rolipram

Summary

Summary: A phosphodiesterase inhibitor with antidepressant properties.

Top Publications

  1. ncbi Persistent improvement in synaptic and cognitive functions in an Alzheimer mouse model after rolipram treatment
    Bing Gong
    The Center for Dementia Research, Nathan Kline Institute for Psychiatric Research, Orangeburg, New York, USA
    J Clin Invest 114:1624-34. 2004
  2. ncbi Inhibitor binding to type 4 phosphodiesterase (PDE4) assessed using [3H]piclamilast and [3H]rolipram
    Yu Zhao
    Department of Pharmacology, University of Tennessee Health Science Center, 874 Union Avenue, Memphis, TN 38163, USA
    J Pharmacol Exp Ther 305:565-72. 2003
  3. ncbi Inhibitory effects of quercetin derivatives on phosphodiesterase isozymes and high-affinity [(3) H]-rolipram binding in guinea pig tissues
    Agnes L F Chan
    Pharmacy Department, Chi Mei Medical Center, 901 Chung Hwa Road, Tainan, 710, Taiwan
    Invest New Drugs 26:417-24. 2008
  4. ncbi PDE4 inhibitors induce emesis in ferrets via a noradrenergic pathway
    A Robichaud
    Department of Pharmacology, Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe Claire, Dorval, Quebec, Canada H9R 4P8
    Neuropharmacology 40:262-9. 2001
  5. ncbi Rolipram attenuates acute oligodendrocyte death in the adult rat ventrolateral funiculus following contusive cervical spinal cord injury
    Christopher M Whitaker
    Kentucky Spinal Cord Injury Research Center, School of Medicine, University of Louisville, Louisville, KY 40292, USA
    Neurosci Lett 438:200-4. 2008
  6. ncbi Quantification of brain phosphodiesterase 4 in rat with (R)-[11C]Rolipram-PET
    Masahiro Fujita
    Molecular Imaging Branch, National Institute of Mental Health, Building 1, Room B3 10, 1 Center Drive, MSC 0135, Bethesda, MD 20892 0135, USA
    Neuroimage 26:1201-10. 2005
  7. ncbi Correlation between emetic effect of phosphodiesterase 4 inhibitors and their occupation of the high-affinity rolipram binding site in Suncus murinus brain
    Ryo Hirose
    Pharmaceutical Research Center, Kyowa Hakko Kogyo Co, Ltd, 1188 Shimotogari, Nagaizumi, Shizuoka, 411 8731, Japan
    Eur J Pharmacol 573:93-9. 2007
  8. ncbi PDE4 inhibitors roflumilast and rolipram augment PGE2 inhibition of TGF-{beta}1-stimulated fibroblasts
    Shinsaku Togo
    Pulmonary and Critical Care Medicine, University of Nebraska Medical Center, Omaha, NE 68198 5885, USA
    Am J Physiol Lung Cell Mol Physiol 296:L959-69. 2009
  9. ncbi Beneficial effects of rolipram in the R6/2 mouse model of Huntington's disease
    Zena DeMarch
    Santa Lucia Foundation IRCCS Hospital at the European Center for Brain Research, Laboratory of Neuroanatomy, Rome, Italy
    Neurobiol Dis 30:375-87. 2008
  10. ncbi Antidepressant- and anxiolytic-like effects of the phosphodiesterase-4 inhibitor rolipram on behavior depend on cyclic AMP response element binding protein-mediated neurogenesis in the hippocampus
    Yun Feng Li
    Department of Behavioral Medicine and Psychiatry, West Virginia University Health Sciences Center, Morgantown, WV 26506 9137, USA
    Neuropsychopharmacology 34:2404-19. 2009

Research Grants

  1. PKA-Hypothermia Bridge: A New Therapeutic Approach for Traumatic Brain Injury
    Larry W Jenkins; Fiscal Year: 2010
  2. HEMORHEOLOGICAL FACTORS IN CEREBRAL ISCHEMIA
    Mark Fisher; Fiscal Year: 2009
  3. Up-regulation of Mucin Gene Transcription-Otitis Media
    Jian dong Li; Fiscal Year: 2010
  4. CRYSTAL STRUCT. OF CYCLIC NUCLEOTIDE PHOSPHODIESTERASE
    Hengming Ke; Fiscal Year: 2003
  5. Effects of Lead on Cortical Development and Plasticity
    MARY A WILSON; Fiscal Year: 2010
  6. Effects of Lead on Cortical Development and Plasticity
    Mary Wilson; Fiscal Year: 2009
  7. Novel A2A Adenosine Agonists in Vascular Protection
    Jayson Rieger; Fiscal Year: 2005
  8. PKA-Hypothermia Bridge: A New Therapeutic Approach for Traumatic Brain Injury
    Larry Jenkins; Fiscal Year: 2009
  9. HEMORHEOLOGICAL FACTORS IN CEREBRAL ISCHEMIA
    Mark J Fisher; Fiscal Year: 2010
  10. HEMORHEOLOGICAL FACTORS IN CEREBRAL ISCHEMIA
    Mark Fisher; Fiscal Year: 2007

Detail Information

Publications228 found, 100 shown here

  1. ncbi Persistent improvement in synaptic and cognitive functions in an Alzheimer mouse model after rolipram treatment
    Bing Gong
    The Center for Dementia Research, Nathan Kline Institute for Psychiatric Research, Orangeburg, New York, USA
    J Clin Invest 114:1624-34. 2004
    ..Here we demonstrate that brief treatment with the phosphodiesterase 4 inhibitor rolipram ameliorates deficits in both long-term potentiation (LTP) and contextual learning in the double-transgenic mice...
  2. ncbi Inhibitor binding to type 4 phosphodiesterase (PDE4) assessed using [3H]piclamilast and [3H]rolipram
    Yu Zhao
    Department of Pharmacology, University of Tennessee Health Science Center, 874 Union Avenue, Memphis, TN 38163, USA
    J Pharmacol Exp Ther 305:565-72. 2003
    Piclamilast is a type 4 phosphodiesterase (PDE4) inhibitor with equal affinity for the high-affinity rolipram binding site (HARBS) and low-affinity rolipram binding site (LARBS)...
  3. ncbi Inhibitory effects of quercetin derivatives on phosphodiesterase isozymes and high-affinity [(3) H]-rolipram binding in guinea pig tissues
    Agnes L F Chan
    Pharmacy Department, Chi Mei Medical Center, 901 Chung Hwa Road, Tainan, 710, Taiwan
    Invest New Drugs 26:417-24. 2008
    b>Rolipram has high (PDE4(H)) and low (PDE4(L)) affinities for phosphodiesterase (PDE)-4, respectively...
  4. ncbi PDE4 inhibitors induce emesis in ferrets via a noradrenergic pathway
    A Robichaud
    Department of Pharmacology, Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe Claire, Dorval, Quebec, Canada H9R 4P8
    Neuropharmacology 40:262-9. 2001
    ..e. 6-(4-pyridylmethyl)-8-(3-nitrophenyl)quinoline, CT-2450 and R-rolipram. It was postulated that PDE4 inhibitors trigger emesis by mimicking the pharmacological actions of alpha(2)-..
  5. ncbi Rolipram attenuates acute oligodendrocyte death in the adult rat ventrolateral funiculus following contusive cervical spinal cord injury
    Christopher M Whitaker
    Kentucky Spinal Cord Injury Research Center, School of Medicine, University of Louisville, Louisville, KY 40292, USA
    Neurosci Lett 438:200-4. 2008
    b>Rolipram, an inhibitor of phosphodiesterase 4 (PDE4) proteins that hydrolyze cAMP, increases axonal regeneration following spinal cord injury (SCI)...
  6. ncbi Quantification of brain phosphodiesterase 4 in rat with (R)-[11C]Rolipram-PET
    Masahiro Fujita
    Molecular Imaging Branch, National Institute of Mental Health, Building 1, Room B3 10, 1 Center Drive, MSC 0135, Bethesda, MD 20892 0135, USA
    Neuroimage 26:1201-10. 2005
    ..Phosphodiesterase 4 (PDE4) catabolizes the second messenger 3', 5'-cyclic adenosine monophosphate and may play a critical role in brain diseases. Our aim was to quantify PDE4 in rats with positron emission tomography (PET)...
  7. ncbi Correlation between emetic effect of phosphodiesterase 4 inhibitors and their occupation of the high-affinity rolipram binding site in Suncus murinus brain
    Ryo Hirose
    Pharmaceutical Research Center, Kyowa Hakko Kogyo Co, Ltd, 1188 Shimotogari, Nagaizumi, Shizuoka, 411 8731, Japan
    Eur J Pharmacol 573:93-9. 2007
    We employed an ex vivo [(3)H]rolipram binding experiment to elucidate the mechanism of emetic activity of phosphodiesterase 4 inhibitors...
  8. ncbi PDE4 inhibitors roflumilast and rolipram augment PGE2 inhibition of TGF-{beta}1-stimulated fibroblasts
    Shinsaku Togo
    Pulmonary and Critical Care Medicine, University of Nebraska Medical Center, Omaha, NE 68198 5885, USA
    Am J Physiol Lung Cell Mol Physiol 296:L959-69. 2009
    ..The PDE4 inhibitors roflumilast and rolipram both inhibited fibroblast-mediated contraction of three-dimensional collagen gels and fibroblast chemotaxis ..
  9. ncbi Beneficial effects of rolipram in the R6/2 mouse model of Huntington's disease
    Zena DeMarch
    Santa Lucia Foundation IRCCS Hospital at the European Center for Brain Research, Laboratory of Neuroanatomy, Rome, Italy
    Neurobiol Dis 30:375-87. 2008
    We have previously showed that rolipram, a phosphodiesterase type IV inhibitor, displays a neuroprotective effect in a rat quinolinic acid model of HD [DeMarch Z., Giampa C., Patassini S., Martorana A., Bernardi G. and Fusco F.R...
  10. ncbi Antidepressant- and anxiolytic-like effects of the phosphodiesterase-4 inhibitor rolipram on behavior depend on cyclic AMP response element binding protein-mediated neurogenesis in the hippocampus
    Yun Feng Li
    Department of Behavioral Medicine and Psychiatry, West Virginia University Health Sciences Center, Morgantown, WV 26506 9137, USA
    Neuropsychopharmacology 34:2404-19. 2009
    ..In this study, chronic administration of rolipram (0.31-1.25 mg/kg, 16-23 days) produced antidepressant- and anxiolytic-like effects on behavior in mice...
  11. ncbi Rolipram inhibits leukocyte-endothelial cell interactions in vivo through P- and E-selectin downregulation
    Maria Jesus Sanz
    Department of Pharmacology, Faculty of Medicine, University of Valencia, Spain
    Br J Pharmacol 135:1872-81. 2002
    1. Rolipram, a selective phosphodiesterase (PDE) type 4 inhibitor, was used to characterize leukocyte recruitment mechanisms in models of acute and subacute inflammation...
  12. ncbi Effects of rolipram, pimobendan and zaprinast on ischaemia-induced dysrhythmias and on ventricular cyclic nucleotide content in the anaesthetized rat
    M D Carceles
    University School of Medicine, Department of Anaesthesiology, CSV Arrixaca Hospital, Murcia, Spain
    Eur J Anaesthesiol 20:205-11. 2003
    ..The drugs used were pimobendan, a selective PDE III inhibitor, rolipram, a selective PDE IV inhibitor, and zaprinast, a selective PDE V inhibitor...
  13. ncbi Luteolin, a non-selective competitive inhibitor of phosphodiesterases 1-5, displaced [3H]-rolipram from high-affinity rolipram binding sites and reversed xylazine/ketamine-induced anesthesia
    Ming Chih Yu
    Department of Internal Medicine, Taipei Municipal Wan Fang Hospital, Taiwan
    Eur J Pharmacol 627:269-75. 2010
    ..possible adverse effects, such as nausea, vomiting, and gastric hypersecretion, determined by replacing [(3)H]-rolipram binding and reversing xylazine/ketamine-induced anesthesia...
  14. ncbi Rolipram: a specific phosphodiesterase 4 inhibitor with potential antipsychotic activity
    S J Kanes
    Department of Psychiatry and Center for Neurobiology and Behavior, University of Pennsylvania, Philadelphia, PA 19104, USA
    Neuroscience 144:239-46. 2007
    ..To test this hypothesis, we studied the effect of an acute treatment of rolipram, an inhibitor of type 4 phosphodiesterases that degrade cAMP, on acoustic startle and prepulse inhibition (PPI) ..
  15. ncbi Rolipram-induced elevation of cAMP or chondroitinase ABC breakdown of inhibitory proteoglycans in the extracellular matrix promotes peripheral nerve regeneration
    E Udina
    Division of Physical Medicine and Rehabilitation, Faculty of Medicine and Dentistry, Center for Neurosciences, University of Alberta, Edmonton, Alberta, Canada T6G 2S2
    Exp Neurol 223:143-52. 2010
    ..transected common peroneal (CP) nerve in rats and either elevated cAMP in the axotomized neurons by subcutaneous rolipram, a specific inhibitor of phosphodiesterase IV, and/or promoted degradation of proteoglycans in the distal nerve ..
  16. ncbi Inflammation, mucous cell metaplasia, and Bcl-2 expression in response to inhaled lipopolysaccharide aerosol and effect of rolipram
    Kevin R Smith
    COPD Program, Lovelace Respiratory Research Institute, Albuquerque, NM 87108, USA
    Toxicol Appl Pharmacol 253:253-60. 2011
    ..When rats were treated with the phosphodiesterase-4 (PDE4) inhibitor, rolipram (10mg/kg), prior to exposure to aerosolized LPS neutrophil numbers in the BAL were reduced at 8h but not at 24 or ..
  17. ncbi Effects of rolipram on adult rat oligodendrocytes and functional recovery after contusive cervical spinal cord injury
    E Beaumont
    Kentucky Spinal Cord Injury Research Center, School of Medicine, University of Louisville, Louisville, KY 40292, USA
    Neuroscience 163:985-90. 2009
    ..4 (PDE4) subtypes and that their death was attenuated up to 3 days after contusive cervical SCI when rolipram, a specific inhibitor of PDE4, was administered...
  18. ncbi Improved sensorimotor function by rolipram following focal cerebral ischemia in rats
    Sonja Hätinen
    Department of Neurology, University of Kuopio, Finland
    Restor Neurol Neurosci 26:493-9. 2008
    b>Rolipram, a specific phosphodiesterase 4 inhibitor (PDE4), is suggested to facilitate functional recovery following brain injury by activation of cAMP/CREB pathway...
  19. ncbi Cyclic nucleotide phosphodiesterases and their role in immunomodulatory responses: advances in the development of specific phosphodiesterase inhibitors
    Ana Castro
    Instituto de Química Médica, Juan de la Cierva 3, 28006 Madrid, Spain
    Med Res Rev 25:229-44. 2005
    ..The review also highlights the novel structural classes of PDE4 and PDE7 inhibitors, and the therapeutic potential that combined PDE4/PDE7 inhibitors offer as immunomodulatory agents...
  20. ncbi Comparision of the inotropic effects of levosimendan, rolipram, and dobutamine on human atrial trabeculae
    Coskun Usta
    Department of Pharmacology, Akdeniz University, Medical Faculty, Antalya, Turkey
    J Cardiovasc Pharmacol 44:622-5. 2004
    ..compare the positive inotropic effects of 3 different agents with 3 different mechanisms of actions-levosimendan, rolipram, and dobutamine-on human atrial trabecular muscles...
  21. ncbi Early and late bronchoconstrictions, airway hyper-reactivity, leucocyte influx and lung histamine and nitric oxide after inhaled antigen: effects of dexamethasone and rolipram
    T J Toward
    Division of Pharmacology, Welsh School of Pharmacy, Cardiff University, Cardiff, UK
    Clin Exp Allergy 34:91-102. 2004
    ..to standard anti-asthmatic agents, the steroid, dexamethasone, and a phosphodiesterase-4 (PDE4) inhibitor, rolipram. METHODS: Guinea-pigs were sensitized with ovalbumen (OA) (10 microg plus Al2(OH)3 100 mg, intraperitoneal (i.p...
  22. ncbi Effect of phosphodiesterase inhibitor-4, rolipram, on new bone formations by recombinant human bone morphogenetic protein-2
    H Horiuchi
    Department of Orthopaedic Surgery, Shinshu University School of Medicine, Nagano, Japan
    Bone 30:589-93. 2002
    ..Ten or 20 mg/kg per day of Rolipram, a selective inhibitory agent to phosphodiesterase type 4 (PDE-4), or vehicle, was injected subcutaneously into ..
  23. ncbi The phosphodiesterase type 4 inhibitor, rolipram, enhances glucocorticoid receptor function
    Andrew H Miller
    Department of Psychiatry and Behavioral Sciences, Emory University School of Medicine, 1639 Pierce Dr, Suite 4000, Atlanta, GA 30322, USA
    Neuropsychopharmacology 27:939-48. 2002
    ..Accordingly, we examined GR function in cells treated with rolipram, a phosphodiesterase (PDE) type 4 inhibitor that antagonizes cAMP breakdown...
  24. ncbi Whole-body biodistribution and radiation dosimetry in monkeys and humans of the phosphodiesterase 4 radioligand [(11)C](R)-rolipram: comparison of two-dimensional planar, bisected and quadrisected image analyses
    David R Sprague
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD 20892 2035, USA
    Nucl Med Biol 35:493-500. 2008
    11)C](R)-Rolipram is a selective radioligand for positron emission tomography (PET) imaging of phosphodiesterase 4, an enzyme that metabolizes 3',5'-cyclic adenosine monophosphate...
  25. ncbi The type IV phosphodiesterase inhibitor rolipram induces expression of the cell cycle inhibitors p21(Cip1) and p27(Kip1), resulting in growth inhibition, increased differentiation, and subsequent apoptosis of malignant A-172 glioma cells
    Thomas C Chen
    LAC USC Medical Center, Department of Neurosurgery, Pathology, University of Southern California, 1200 N State St, Suite 5046, Los Angeles, CA 90033, USA
    Cancer Biol Ther 1:268-76. 2002
    ..Therefore, we investigated the effects of rolipram, a drug that has undergone clinical trials as an antidepressant and has also been proposed as a treatment for ..
  26. ncbi Preventive effect of rolipram, a phosphodiesterase 4 enzyme inhibitor, on oxidative renal injury in acute ascending pyelonephritis model in rats
    Sadik Gorur
    Department of Urology, Mustafa Kemal University Faculty of Medicine, Antioch Hatay, Turkey
    Urology 72:743-8. 2008
    To evaluate the effects of rolipram, a phosphodiesterase 4 enzyme inhibitor, on Escherichia coli-induced renal oxidative damage in an acute pyelonephritis (PYN) rat model.
  27. ncbi Genistein, a competitive PDE1-4 inhibitor, may bind on high-affinity rolipram binding sites of brain cell membranes and then induce gastrointestinal adverse effects
    Chung Hong Shih
    Department of Internal Medicine, Taipei Medical University Hospital, Taipei, Taiwan
    Eur J Pharmacol 643:113-20. 2010
    ..3 to 13.7 microM. Genistein (3-300 microM) concentration-dependently displaced 2nM [(3)H]-rolipram bound on high-affinity rolipram binding sites of brain cell membranes...
  28. ncbi Dysregulation of protein kinase a signaling in the aged prefrontal cortex: new strategy for treating age-related cognitive decline
    Brian P Ramos
    Department of Neurobiology, Yale University School of Medicine, New Haven, CT 06510, USA
    Neuron 40:835-45. 2003
    ..These data demonstrate that PKA inhibition, rather than activation, is the appropriate strategy for restoring prefrontal cortical cognitive abilities in the elderly...
  29. ncbi Selective inhibition of purified human phosphodiesterase 4A expressed in yeast cell GL62 by ciclamilast, piclamilast, and rolipram
    Jun Chun Chen
    Respiratory Drugs Research Laboratory of State Food and Drugs Administration of China, Medical School of Zhejiang University, Hangzhou 310031, China
    Acta Pharmacol Sin 25:1171-5. 2004
    ..and investigate the effects of selective phosphodiesterase 4 (PDE4) inhibitors (ciclamilast, piclamilast, and rolipram), selective phosphodiesterase 5 (PDE5) inhibitor zaprinast, and cyclooxygenase (COX) inhibitors (aspirin, ..
  30. ncbi Phosphodiesterase inhibitors: a novel mechanism for receptor-independent antipsychotic medications
    C R Maxwell
    Stanley Center for Experimental Therapeutics in Psychiatry, Division of Neuropsychiatry, Department of Psychiatry, University of Pennsylvania, Philadelphia, PA 19104, USA
    Neuroscience 129:101-7. 2004
    ..This study examines the ability of the phosphodiesterase-4 inhibitor, rolipram, to reverse amphetamine-induced abnormalities in auditory-evoked potentials that are characteristic of ..
  31. ncbi Different regulation of adenylyl cyclase and rolipram-sensitive phosphodiesterase activity on the frontal cortex and hippocampus in learned helplessness rats
    Tetsuji Itoh
    Department of Drug Safety Evaluation, Developmental Research Laboratories, Shionogi and Co, Ltd, 3 1 1, Futaba cho, Toyonaka, Osaka 561 0825, Japan
    Brain Res 991:142-9. 2003
    The present study examined the activities of adenylyl cyclase (AC) and rolipram-sensitive phosphodiesterase (PDE4) on brain regions in learned helplessness rat in order to clarify the cyclic AMP (cAMP) regulation system in the depressive ..
  32. ncbi Rolipram inhibits polarization and migration of human T lymphocytes
    Esther Layseca-Espinosa
    , Facultad de Medicina, ,
    J Invest Dermatol 121:81-7. 2003
    ..skin diseases; however, an overall study on the effects of specific phosphodiesterase inhibitors, such as rolipram on the processes involved in the extravasation of lymphoid cells has not been performed...
  33. ncbi Upregulation of phosphodiesterase-4 in the lung of allergic rats
    Hui-Fang Tang
    Schering-Plough Research Institute, 2015 Galloping Hill Road, K-15-1600, Kenilworth, NJ 07033, USA
    Am J Respir Crit Care Med 171:823-8. 2005
    ..The increases in pulmonary resistance and IL-4 production were both suppressed by the PDE4-selective inhibitor rolipram or the corticosteroid drug dexamethasone...
  34. ncbi Comparison of PDE 4 inhibitors, rolipram and SB 207499 (ariflo), in a rat model of pulmonary neutrophilia
    J Spond
    Schering Plough Research Institute, Kenilworth, New Jersey, USA
    Pulm Pharmacol Ther 14:157-64. 2001
    ..of SB 207499 was evaluated and compared to that of the prototypic type-4 phosphodiesterase (PDE4) inhibitor, rolipram. In dose-response experiments, we found that rats exposed to 10 microg or 100 microg of intratracheal (it) LPS ..
  35. ncbi Phosphodiesterase type 4 isozymes expression in human brain examined by in situ hybridization histochemistry and[3H]rolipram binding autoradiography. Comparison with monkey and rat brain
    S Pérez-Torres
    Department of Neurochemistry, Instituto de Investigaciones Biomédicas de Barcelona, CSIC IDIBAPS, C Rosselló 161, 6a, E 08036, Barcelona, Spain
    J Chem Neuroanat 20:349-74. 2000
    ..mRNAs in the brain of different species by in situ hybridization histochemistry and by autoradiography with [3H]rolipram. We have compared the localization of each isozyme in human brain with that in rat and monkey brain...
  36. ncbi The phosphodiesterase inhibitors pentoxifylline and rolipram suppress macrophage activation and nitric oxide production in vitro and in vivo
    E Beshay
    The Department of Pathology, McGill University, 3775 University Street, Montreal, Quebec, H3A 2B4, Canada
    Clin Immunol 98:272-9. 2001
    We studied the effects of the phosphodiesterase inhibitors pentoxifylline (PTX) and rolipram (ROL) on nitric oxide (NO) production by macrophages and correlated this with cellular cAMP levels. The RAW 264...
  37. ncbi Elastolytic activity and alveolar epithelial type-1 cell damage after chronic LPS inhalation: effects of dexamethasone and rolipram
    Frederick J Johnson
    Division of Pharmacology, Welsh School of Pharmacy, Cardiff University, King Edward VII Avenue, Cathays Park, Cardiff, CF10 3XF, UK
    Toxicol Appl Pharmacol 207:257-65. 2005
    ..The effect of the corticosteroid, dexamethasone, or the phosphodiesterase-4 (PDE4)-inhibitor, rolipram, on these features was studied...
  38. ncbi Adenovirus-mediated delivery and expression of a cAMP-dependent protein kinase inhibitor gene to BEAS-2B epithelial cells abolishes the anti-inflammatory effects of rolipram, salbutamol, and prostaglandin E2: a comparison with H-89
    Koremu K Meja
    Thoracic Medicine, National Heart and Lung Institute, Imperial College London, London, United Kingdom
    J Pharmacol Exp Ther 309:833-44. 2004
    ..antagonized MCP-1-induced [(3)H]AA release and enhanced the inhibitory effect of submaximal concentrations of rolipram and 8-bromo-cAMP...
  39. ncbi Three-dimensional structures of PDE4D in complex with roliprams and implication on inhibitor selectivity
    Qing Huai
    Department of Biochemistry and Biophysics and Lineberger Comprehensive Cancer Center, The University of North Carolina, Chapel Hill, Chapel Hill, NC 27599, USA
    Structure 11:865-73. 2003
    ..The crystal structures of the PDE4D2 catalytic domain in complex with (R)- or (R,S)-rolipram suggest that inhibitor selectivity is determined by the chemical nature of amino acids and subtle conformational ..
  40. ncbi Rolipram depresses [(3)H]2-deoxyglucose uptake in mouse brain and heart in vivo
    Megumi Ishikawa
    Department of Medical Physics, School of Allied Health Sciences, Faculty of Medicine, Osaka University, 1 7 Yamadaoka, Suita Shi, Osaka, Japan
    Eur J Nucl Med Mol Imaging 29:1212-5. 2002
    The effects of systemic administration of rolipram, a selective phosphodiesterase type 4 inhibitor, on [(3)H]2-deoxyglucose (DG) uptake in brain and peripheral tissues were examined...
  41. ncbi Goblet cell hyperplasia, airway function, and leukocyte infiltration after chronic lipopolysaccharide exposure in conscious Guinea pigs: effects of rolipram and dexamethasone
    Toby J Toward
    Division of Pharmacology, Welsh School of Pharmacy, Cardiff University, King Edward VII Avenue, Cathays Park, Cardiff CF10 3XF, Wales, UK
    J Pharmacol Exp Ther 302:814-21. 2002
    ..parameters to treatment with the corticosteroid, dexamethasone, or the phosphodiesterase-4 (PDE4) inhibitor, rolipram, was determined...
  42. ncbi Airway function, oedema, cell infiltration and nitric oxide generation in conscious ozone-exposed guinea-pigs: effects of dexamethasone and rolipram
    Toby J Toward
    Division of Pharmacology, Welsh School of Pharmacy, Cardiff University, King Edward VII Avenue, Cathays Park, Cardiff CF10 3XF
    Br J Pharmacol 136:735-45. 2002
    ..15+/-0.05 p.p.m.) and their modification by dexamethasone (20 mg kg(-1)) or the phosphodiesterase-4 inhibitor, rolipram (1 mg kg(-1)), administered (i.p.) 24 and 0...
  43. ncbi Diazepam and rolipram differentially inhibit cyclic AMP-specific phosphodiesterases PDE4A1 and PDE4B3 in the mouse
    J A Cherry
    Department of Psychology and Laboratory of Molecular Neurobiology and Behavior, 64 Cummington Street, Boston University, 02215, Boston, MA, USA
    Biochim Biophys Acta 1518:27-35. 2001
    ..by benzodiazepines, it has not been conclusively demonstrated that members of the class of cyclic AMP-specific, rolipram-inhibitable PDEs (PDE4s) are targets for these drugs...
  44. ncbi Inhibition of the phosphodiesterase 4 (PDE4) enzyme reverses memory deficits produced by infusion of the MEK inhibitor U0126 into the CA1 subregion of the rat hippocampus
    Han Ting Zhang
    Department of Pharmacology, The University of Tennessee Health Science Center, Memphis, TN 38163, USA
    Neuropsychopharmacology 29:1432-9. 2004
    ..It was found that rolipram, a PDE4-selective inhibitor, reversed the amnesic effect in the radial-arm maze test of the MEK inhibitor U0126 ..
  45. ncbi Effects of the phosphodiesterase IV inhibitor rolipram on Th1 and Th2 immune responses in mice
    Kouya Yamaki
    Department of Pharmacology, Kobe Pharmaceutical University, Kobe, Hyogo 658-8558, Japan
    J Pharm Pharmacol 56:877-82. 2004
    The present study was designed to investigate the effect of the phosphodiesterase IV inhibitor rolipram on Th1 and Th2 immune responses in mice...
  46. ncbi Impact of VIP and cAMP on the regulation of TNF-alpha and IL-10 production: implications for rheumatoid arthritis
    Andrew D Foey
    Kennedy Institute of Rheumatology Division, Charing Cross Hospital Campus, Imperial College School of Medicine, London, UK
    Arthritis Res Ther 5:R317-28. 2003
    ..its slight effect on TNF-alpha results from cAMP being rapidly degraded as the phosphodiesterase IV inhibitor, rolipram, rescues cAMP-dependent activation of cAMP response element binding protein...
  47. ncbi Effects of a phosphodiesterase IV inhibitor rolipram on microsphere embolism-induced defects in memory function and cerebral cyclic AMP signal transduction system in rats
    Akira Nagakura
    Department of Pharmacology, Tokyo University of Pharmacy and Life Science, 1432-1, Horinouchi, Hachioji, Tokyo 192-0392, Japan
    Br J Pharmacol 135:1783-93. 2002
    The effects of treatment with rolipram, a specific phosphodiesterase IV inhibitor, on learning and memory function and on the cyclic AMP/PKA/CREB signal transduction system were examined in rats with microsphere embolism (ME)-induced ..
  48. ncbi Airway relaxant and anti-inflammatory properties of a PDE4 inhibitor with low affinity for the high-affinity rolipram binding site
    Christian Martin
    Division of Pulmonary Pharmacology, Research Centre Borstel, Parkallee 22, 23845 Borstel, Germany
    Naunyn Schmiedebergs Arch Pharmacol 365:284-9. 2002
    ..PDE4 has two binding sites for the archetypal PDE4 inhibitor rolipram, and it has been suggested that binding to the high-affinity rolipram binding site (HARBS) is responsible for the ..
  49. ncbi Effects of rolipram, a selective inhibitor of type 4 phosphodiesterase, on lipopolysaccharide-induced uveitis in rats
    Zai Long Chi
    Department of Ophthalmology, Toyama Medical and Pharmaceutical University, Sugitani, Toyama, Japan
    Invest Ophthalmol Vis Sci 45:2497-502. 2004
    To investigate effects of rolipram, an inhibitor of type 4 phosphodiesterase, on lipopolysaccharide (LPS)-induced uveitis in Wistar rats.
  50. ncbi The antidepressant and antiinflammatory effects of rolipram in the central nervous system
    J Zhu
    Division of Geriatric Medicine, Department of Clinical Neuroscience, Karolinska Institutet, Huddinge Hospital, S 141 86 Stockholm, Sweden
    CNS Drug Rev 7:387-98. 2001
    b>Rolipram is a selective inhibitor of phosphodiesterases (PDE) IV, especially of the subtype PDE IVB. These phosphodiesterases are responsible for hydrolysis of the cyclic nucleotides cAMP and cGMP, particularly in nerve and immune cells...
  51. ncbi Modulation of corneal endothelial hydration control mechanisms by Rolipram
    C G Wigham
    Department of Optometry and Vision Sciences, Cardiff University, UK
    Pflugers Arch 440:866-70. 2000
    ..To resolve this question, the effects of Rolipram, a cAMP phosphodiesterase inhibitor, on endothelial physiology were determined. Addition of 0...
  52. ncbi Acute rolipram/thalidomide treatment improves tissue sparing and locomotion after experimental spinal cord injury
    Guido C Koopmans
    Department of Anesthesiology, Academic Hospital Maastricht, Maastricht, 6200 AZ, The Netherlands
    Exp Neurol 216:490-8. 2009
    ..In the present investigation, the ability of rolipram and thalidomide (FDA approved drugs) to reduce secondary tissue degeneration and improve motor function was ..
  53. ncbi Increasing synaptic noradrenaline, serotonin and histamine enhances in vivo binding of phosphodiesterase-4 inhibitor (R)-[11C]rolipram in rat brain, lung and heart
    Celia M Lourenco
    PET Centre, Centre for Addiction and Mental Health, 250 College St, Toronto, Ontario, Canada M5T 1R8
    Life Sci 79:356-64. 2006
    ..PDE4 expression and activity are modulated by agents affecting cAMP levels. The selective PDE4 inhibitor (R)-rolipram labeled with C-11 was tested in vivo in rats to analyze changes in PDE4 levels following drug treatments that ..
  54. ncbi Chronic lipopolysaccharide exposure on airway function, cell infiltration, and nitric oxide generation in conscious guinea pigs: effect of rolipram and dexamethasone
    T J Toward
    Division of Pharmacology, Welsh School of Pharmacy, Cardiff University, Cardiff, United Kingdom
    J Pharmacol Exp Ther 298:298-306. 2001
    ..The effect of the corticosteroid, dexamethasone, or phosphodiesterase-4 (PDE4) inhibitor, rolipram, on these features was studied...
  55. ncbi Cellular mechanisms underlying prostaglandin-induced transient cAMP signals near the plasma membrane of HEK-293 cells
    Thomas C Rich
    Department of Pharmacology, College of Medicine and Center for Lung Biology, University of South Alabama, Mobile, AL 36688, USA
    Am J Physiol Cell Physiol 292:C319-31. 2007
    ..Following pretreatment with rolipram (a PDE4 inhibitor), H89 had little or no effect on near-membrane or total cAMP levels...
  56. ncbi Beneficial effects of rolipram in a quinolinic acid model of striatal excitotoxicity
    Zena DeMarch
    Laboratory of Neuroanatomy, Santa Lucia Foundation IRCCS at the European Center for Brain Research, Via del Fosso Fiorano 64, 00143 Rome, Italy
    Neurobiol Dis 25:266-73. 2007
    ..The phosphodiesterase type IV inhibitor rolipram increases CREB phosphorylation. Such drug has a protective effect in global ischaemia and embolism in rats...
  57. ncbi The PDE4 inhibitor rolipram reverses object memory impairment induced by acute tryptophan depletion in the rat
    K Rutten
    Department of Psychiatry and Neuropsychology, Brain and Behavior Institute, Maastricht University, Universiteitssingel 50, 6200 MD, Maastricht, The Netherlands
    Psychopharmacology (Berl) 192:275-82. 2007
    The selective type IV phosphodiesterase inhibitor, rolipram, has been shown to improve long-term memory and can reverse the cholinergic deficit caused by scopolamine. However, the underlying mechanisms of action of rolipram remain obscure.
  58. ncbi Characterization of five different proteins produced by alternatively spliced mRNAs from the human cAMP-specific phosphodiesterase PDE4D gene
    G B Bolger
    Department of Veterans Affairs Medical Center, 151M, and Huntsman Cancer Institute, Department of Oncologic Sciences and Department of Medicine Hematology Oncology University of Utah Health Sciences Center, Salt Lake City, UT 84148, USA
    Biochem J 328:539-48. 1997
    ..two isoforms (HSPDE4D4 and HSPDE4A5) encoded by the human PDE4D gene, one of four genes that encode cAMP-specific rolipram-inhibited 3',5'-cyclic nucleotide phosphodiesterases (type IVPDEs; PDE4 family)...
  59. ncbi Difference in preventive effects between the phosphodiesterase iv inhibitor rolipram and anti-arthritic drugs on antigen-induced arthritis in mice
    Kouya Yamaki
    Department of Pharmacology, Kobe Pharmaceutical University, Kobe, Hyogo, Japan
    Immunol Invest 36:131-45. 2007
    The efficacy of the phosphodiesterase (PDE) IV inhibitor rolipram on antigen-induced arthritis (AIA) in mice was evaluated in comparison with clinically used anti-arthritic drugs...
  60. ncbi The human cyclic AMP-specific phosphodiesterase PDE-46 (HSPDE4A4B) expressed in transfected COS7 cells occurs as both particulate and cytosolic species that exhibit distinct kinetics of inhibition by the antidepressant rolipram
    E Huston
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, IBLS, Wolfson Link Building, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom
    J Biol Chem 271:31334-44. 1996
    ..encoding the human cyclic AMP-specific PDE4A phosphodiesterase PDE-46 (HSPDE4A4B) led to the expression of a rolipram-inhibited PDE4 activity, which contributed approximately 96% of the total COS cell PDE activity...
  61. ncbi A low-Km, rolipram-sensitive, cAMP-specific phosphodiesterase from human brain. Cloning and expression of cDNA, biochemical characterization of recombinant protein, and tissue distribution of mRNA
    M M McLaughlin
    Department of Gene Expression Sciences, SmithKline Beecham Pharmaceuticals, King of Prussia, Pennsylvania 19406
    J Biol Chem 268:6470-6. 1993
    ..of the expected kinetic characteristics for a PDE IV, including sensitivity to the isozyme-selective inhibitor rolipram (Ki = 0.085 microM)...
  62. ncbi Selective PDE inhibitors rolipram and sildenafil improve object retrieval performance in adult cynomolgus macaques
    K Rutten
    Department of Neuroscience, School for Mental Health and Neuroscience, Maastricht University, Universiteitssingel 50, PO Box 616, 6200 MD Maastricht, The Netherlands
    Psychopharmacology (Berl) 196:643-8. 2008
    ..However, studies evaluating the effects of PDE inhibition on prefrontal cortex-dependent cognition and in monkeys are rare...
  63. ncbi Combined medication of lovastatin with rolipram suppresses severity of experimental autoimmune encephalomyelitis
    Ajaib S Paintlia
    Darby Children s Research Institute, Medical University of South Carolina, USA
    Exp Neurol 214:168-80. 2008
    ..Another drug, rolipram (phosphodiesterase-4 inhibitor) ameliorates the clinical severity of EAE via induction of various anti-..
  64. ncbi Effects of rolipram on the elevated plus-maze test in rats: a preliminary study
    J S Silvestre
    Department of Pharmacology, Research Centre, Almirall Prodesfarma, Barcelona, Spain
    J Psychopharmacol 13:274-7. 1999
    The objective of the present study was to assess the behavioural effects of rolipram, a specific cAMP phosphodiesterase (PDE4) inhibitor, in the elevated plus-maze (EPM) test in rats...
  65. ncbi Phosphodiesterase-4 influences the PKA phosphorylation status and membrane translocation of G-protein receptor kinase 2 (GRK2) in HEK-293beta2 cells and cardiac myocytes
    Xiang Li
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, IBLS, Wolfson Link Building, University of Glasgow, University Avenue, Glasgow G12 8QQ, Scotland, UK
    Biochem J 394:427-35. 2006
    ..when cAMP-specific PDE4 (phosphodiesterase-4) activity is selectively inactivated, either chemically with rolipram or by siRNA (small interfering RNA)-mediated knockdown of PDE4B and PDE4D...
  66. ncbi Mitogen-activated protein kinase-mediated reinforcement of hippocampal early long-term depression by the type IV-specific phosphodiesterase inhibitor rolipram and its effect on synaptic tagging
    Sheeja Navakkode
    Department of Neurophysiology, Leibniz Institute for Neurobiology, D-39118 Magdeburg, Germany
    J Neurosci 25:10664-70. 2005
    b>Rolipram, a selective inhibitor of cAMP-specific phosphodiesterase 4 (PDE4), has been shown to reinforce an early form of long-term potentiation (LTP) to a long-lasting LTP (late LTP)...
  67. ncbi Inhibition of cyclic AMP phosphodiesterase (PDE4) reverses memory deficits associated with NMDA receptor antagonism
    H T Zhang
    Department of Pharmacology and Therapeutics, Louisiana State University Medical Center, Shreveport, LA 71130, USA
    Neuropsychopharmacology 23:198-204. 2000
    b>Rolipram, a selective inhibitor of type 4 cyclic AMP phosphodiesterase (PDE4), completely reversed the amnesic effects of MK-801 on working and reference memory (F[4,64] = 11.10; p <.0001 and F[4,64] = 2.53; p <...
  68. ncbi Effects of rolipram on scopolamine-induced impairment of working and reference memory in the radial-arm maze tests in rats
    H T Zhang
    Department of Pharmacology and Therapeutics, Louisiana State University Medical Center, Shreveport 71130, USA
    Psychopharmacology (Berl) 150:311-6. 2000
    b>Rolipram, a selective inhibitor of cyclic AMP-specific phosphodiesterase (PDE4), has been shown to enhance scopolamine-induced impairment of working memory...
  69. ncbi Rolipram reverses scopolamine-induced and time-dependent memory deficits in object recognition by different mechanisms of action
    K Rutten
    Department of Psychiatry and Neuropsychology, Brain and Behaviour Institute, Maastricht University, PO Box 616, 6200 MD Maastricht, The Netherlands
    Neurobiol Learn Mem 85:132-8. 2006
    In this study, the effect of the selective phosphodiesterase type 4 (PDE4) inhibitor rolipram on memory performance was investigated using the object recognition task. First, three doses of rolipram (0.01, 0.03 or 0...
  70. ncbi Phosphodiesterase 4 inhibitors, rolipram and diazepam block the adaptive changes observed during morphine withdrawal in the heart
    Ana González Cuello
    Department of Pharmacology, University School of Medicine, 30100 Murcia, Spain
    Eur J Pharmacol 570:1-9. 2007
    In this study, we investigated whether morphine dependence was inhibited by phosphodiesterase (PDE) 4 inhibitors rolipram and diazepam, since a role for the cyclic AMP systems in the development of morphine dependence was reported...
  71. ncbi Synthesis and biological evaluation of neutrophilic inflammation inhibitors
    Olga Bruno
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Genova, Viale Benedetto XV, Genova 3 16132, Italy
    Farmaco 59:223-35. 2004
    ..they also inhibited selectively the human PDE4 enzyme, although they are less potent than the reference compound Rolipram. We report here synthesis, biological studies and some SAR considerations concerning the above mentioned compounds...
  72. ncbi Rolipram, a phosphodiesterase 4 inhibitor, prevented cancellous and cortical bone loss by inhibiting endosteal bone resorption and maintaining the elevated periosteal bone formation in adult ovariectomized rats
    W Yao
    Radiobiology Division, University of Utah School of Medicine, Salt Lake City, Utah 84108, USA
    J Musculoskelet Neuronal Interact 7:119-30. 2007
    ..b>Rolipram is a selective PDE4 inhibitor reported to have anti-inflammatory effects and used in the treatment of asthma and ..
  73. ncbi Effects of rolipram on induction of action potential bursts in central snail neurons
    Chia-Hsien Lin
    Department of Pharmacology, College of Medicine, National Taiwan University, No.1, Sec.1, Jen-Ai Road, Taipei, Taiwan
    Exp Neurol 194:384-92. 2005
    Effects of rolipram, a selective inhibitor of phosphodiesterases (PDE) IV, on induction of action potential bursts were studied pharmacologically on the RP4 central neuron of the giant African snail (Achatina fulica Ferussac)...
  74. ncbi Forskolin-induced LTP in the CA1 hippocampal region is NMDA receptor dependent
    Nikolai Otmakhov
    Brandeis University, Volen Center for Complex Systems, Waltham, Massachusetts 02454, USA
    J Neurophysiol 91:1955-62. 2004
    ..of Sp-cAMPS or a combination of the adenylyl cyclase activator, forskolin, and the phosphodiesterase inhibitor, rolipram. Under our conditions, cLTP was induced but only if inhibition was reduced...
  75. ncbi Modulation of the cAMP signaling pathway after traumatic brain injury
    Coleen M Atkins
    Department of Neurological Surgery, University of Miami Miller School of Medicine, Miami, FL 33101, USA
    Exp Neurol 208:145-58. 2007
    ..a phosphodiesterase (PDE) IV inhibitor would improve outcome after TBI, we treated animals intraperitoneally with rolipram (0.3 or 3.0 mg/kg) 30 min prior to TBI, and then once per day for 3 days...
  76. ncbi The role of VASP in regulation of cAMP- and Rac 1-mediated endothelial barrier stabilization
    N Schlegel
    Institute of Anatomy and Cell Biology, University of Wurzburg, Wurzburg, Germany
    Am J Physiol Cell Physiol 294:C178-88. 2008
    ..We tested whether VASP is involved in the endothelium-stabilizing effects of cAMP or Rac 1. Forskolin and rolipram (F/R) to increase cAMP and cytotoxic necrotizing factor 1 (CNF-1) to activate Rac 1 were equally efficient to ..
  77. ncbi Impact of cAMP on the T-cell response to type II collagen
    Patricia Ozegbe
    The Kennedy Institute of Rheumatology Division, Imperial College London, UK
    Immunology 111:35-40. 2004
    ..DBA/1 mice were cultured in the presence of type II collagen plus one of five different cAMP-elevating agents: rolipram, forskolin, prostaglandin E2, 8-bromo-cAMP, or cholera toxin...
  78. ncbi Epac/Rap1 pathway regulates microvascular hyperpermeability induced by PAF in rat mesentery
    R H Adamson
    Physiology and Membrane Biology, School of Medicine, University of California at Davis, Davis, CA 95616, USA
    Am J Physiol Heart Circ Physiol 294:H1188-96. 2008
    ..Our results indicate that increased permeability in intact microvessels by acute inflammatory agents such as PAF is the result of the decreased effectiveness of the Epac/Rap1 pathway modulation of cell-cell adhesion...
  79. ncbi Basal nitric oxide modulates vascular effects of a peptide activating protease-activated receptor 2
    Carla Cicala
    Department of Experimental Pharmacology, University of Naples Federico II, Via Domenico Montesano 49, 80131 Naples, Italy
    Cardiovasc Res 60:431-7. 2003
    ....
  80. ncbi An investigation into the effect of the type IV phosphodiesterase inhibitor rolipram in the modulation of glutamate release from rat prefrontocortical nerve terminals
    Su Jane Wang
    School of Medicine, Fu Jen Catholic University, Hsin Chuang, Taipei Hsien, Republic of China
    Synapse 59:41-50. 2006
    The present study was conducted to explore the influence of rolipram, a specific inhibitor of the phosphodiesterase type 4 (PDE4) isoform, on glutamate release in the rat prefrontal cortex, using isolated nerve terminal (synaptosome) ..
  81. ncbi Cyclic-AMP-dependent proliferation of a human osteoblast cell line (HOS cells) induced by hydroxyapatite: effect of exogenous nitric oxide
    Wihaskoro Sosroseno
    School of Dentistry, AIMST University, Semeling, Bedong 08100, Kedah Darul Aman, Malaysia
    Acta Biomed 79:110-6. 2008
    ..The aim of the present study was to test the hypothesis that exogenous NO may up-regulate the proliferation of hydroxyapatite (HA)-induced HOS cells via the cyclic-AMP-protein kinase A (PKA) pathway...
  82. ncbi Chemoresistant KM12C colon cancer cells are addicted to low cyclic AMP levels in a phosphodiesterase 4-regulated compartment via effects on phosphoinositide 3-kinase
    David G McEwan
    The Beatson Institute for Cancer Research, Cancer Research UK Beatson Laboratories, Glasgow, United Kingdom
    Cancer Res 67:5248-57. 2007
    ..cyclase activator forskolin together with the specific cyclic AMP (cAMP) phosphodiesterase-4 (PDE4) inhibitor rolipram, but not the cAMP phosphodiesterase-3 (PDE3) inhibitor cilostamide, causes profound growth arrest of ..
  83. ncbi Interaction between the antidepressant-like behavioral effects of beta adrenergic agonists and the cyclic AMP PDE inhibitor rolipram in rats
    Han Ting Zhang
    Department of Pharmacology, The University of Tennessee Health Science Center, 874 Union Avenue, Memphis, TN 38163, USA
    Psychopharmacology (Berl) 182:104-15. 2005
    ..However, it is not known if PDE4 is associated with beta adrenergic receptors in the mediation of antidepressant-like effects...
  84. ncbi Mitigation of stress-induced gastric mucosal lesions by a specific type IV phosphodiesterase inhibitor
    Sayuri Kato
    Department of Internal Medicine 1, Akita University School of Medicine, 1 1 1 Hondo, Akita 010 8543, Japan
    Dig Dis Sci 52:711-6. 2007
    ..In the present study, we examined the effect of a specific PDE4 inhibitor (rolipram) on stress-induced gastric mucosal lesions...
  85. ncbi Multiple signalling pathways involved in beta2-adrenoceptor-mediated glucose uptake in rat skeletal muscle cells
    Julia Nevzorova
    Department of Pharmacology, PO Box 13E, Monash University, Victoria 3800, Australia
    Br J Pharmacol 147:446-54. 2006
    ..The PDE4 inhibitor, rolipram (10 microM), increased cAMP accumulation to zinterol or forskolin, and sensitised the GU response to zinterol, ..
  86. ncbi Cyclic AMP-mediated regulation of the resting membrane potential in myelin-forming oligodendrocytes in the isolated intact rat optic nerve
    Sally Bolton
    School of Pharmacy and Biomedical Sciences, University of Portsmouth, St Michael's Building, White Swan Road, Portsmouth PO1 2DT, UK
    Exp Neurol 202:36-43. 2006
    ..In contrast, inhibition of cAMP specific phosphodiesterase with rolipram had no significant effect on the oligodendroglial RMP or the cAMP-mediated hyperpolarization...
  87. ncbi Lixazinone stimulates mitogenesis of Madin-Darby canine kidney cells
    Jingfei Cheng
    Renal Pathophysiology Laboratory, Department of Laboratory Medicine and Pathology, Mayo Clinic College of Medicine, Rochester, Minnesota 55905, USA
    Exp Biol Med (Maywood) 231:288-95. 2006
    ..Pharmacologic agents that stimulate PDE3 activity may provide the basis for new therapies directed toward reducing cystogenesis in patients with PKD...
  88. ncbi Behaviour of [11C]R(-)- and [11C]S(+)-rolipram in vitro and in vivo, and their use as PET radiotracers for the quantificative assay of PDE4
    Christine A Parker
    GlaxoSmithKline, ACCI Addenbrooke s Hospital, Hills Road, Cambridge, CB2 2GG, UK
    Synapse 55:270-9. 2005
    ..b>Rolipram is a selective PDE4 inhibitor which exists in two enantiomeric forms, R(-) and S(+)...
  89. ncbi Cyclic AMP-phosphodiesterases inhibitor improves sodium excretion in rats with cirrhosis and ascites
    Mina Ahloulay
    , INSERM U-481, , 92118 Clichy, France
    Liver Int 25:403-9. 2005
    ..Moroever, the effects on renal function of the intravenous administration of cAMP and rolipram, a powerful and specific cAMP-PDE4 inhibitor, were evaluated...
  90. ncbi The induction of cyclic nucleotide phosphodiesterase 4 gene (PDE4D) impairs memory in a water maze task
    Mauro Giorgi
    Department of Basic and Applied Biology, University of L Aquila, Via Vetoio, località Coppito, 67100 L Aquila, Italy
    Behav Brain Res 154:99-106. 2004
    ..post-training administration of cyclic nucleotide phosphodiesterase (PDE) inhibitors, DC-TA 46 and rolipram, were tested using a visible/hidden-platform water maze task...
  91. ncbi Compartmentalization of cAMP-dependent signaling by phosphodiesterase-4D is involved in the regulation of vasopressin-mediated water reabsorption in renal principal cells
    Eduard Stefan
    Leibniz Institut fur Molekulare Pharmakologie, Berlin, Germany
    J Am Soc Nephrol 18:199-212. 2007
    ..The selective PDE4 inhibitor rolipram increases AKAP-tethered PKA activity on AQP2-bearing vesicles and enhances the AQP2 shuttle and thereby the ..
  92. ncbi In resting COS1 cells a dominant negative approach shows that specific, anchored PDE4 cAMP phosphodiesterase isoforms gate the activation, by basal cyclic AMP production, of AKAP-tethered protein kinase A type II located in the centrosomal region
    Angela McCahill
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, IBLS, Wolfson Link Building, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Cell Signal 17:1158-73. 2005
    ..in resting COS1 cells and this activity increases when cells are treated with the selective PDE4 inhibitor, rolipram. Point mutation of a critical, conserved aspartate residue in the catalytic site of long PDE4A4, PDE4B1, PDE4C2 ..
  93. ncbi Time-dependent involvement of cAMP and cGMP in consolidation of object memory: studies using selective phosphodiesterase type 2, 4 and 5 inhibitors
    Kris Rutten
    Department of Psychiatry and Neuropsychology, Brain and Behavior Institute, EURON, Maastricht University, 6200 MD Maastricht, The Netherlands
    Eur J Pharmacol 558:107-12. 2007
    ..memory enhancing properties of three selective phosphodiesterase inhibitors (PDE-I) vardenafil (PDE5-I), rolipram (PDE4-I) and BAY 60-7550 (PDE2-I) in the object recognition task...
  94. ncbi In vivo selective binding of (R)-[11C]rolipram to phosphodiesterase-4 provides the basis for studying intracellular cAMP signaling in the myocardium and other peripheral tissues
    Miran Kenk
    Cardiac PET Centre, Division of Cardiology, University of Ottawa Heart Institute, Ottawa, Ontario, Canada K1Y 4W7
    Nucl Med Biol 34:71-7. 2007
    ..PDE4 activity and expression are regulated by cAMP levels, suggesting that measurement of PDE4 provides an index of intracellular cAMP signaling...
  95. ncbi Cyclic nucleotide second messengers (cAMP and cGMP) play a central role in signal transduction and regulation of mesenteric postcapillary fluid leak
    Terry J Chong
    UCSF East Bay Surgery Department, Alameda Country Medical Center, Oakland, CA 94602, USA
    J Trauma 59:302-6; discussion 306-7. 2005
    ..The purposes of this series of experiments are to determine microvascular permeability under the following conditions: 1) reduced cGMP levels, 2) elevated cGMP levels, 3) reduced cAMP levels, and 4) elevated cAMP levels...
  96. ncbi Activation and induction of cyclic AMP phosphodiesterase (PDE4) in rat pulmonary microvascular endothelial cells
    Bing Zhu
    Department of Pharmacology, University of South Alabama College of Medicine, Mobile, AL 36688, USA
    Biochem Pharmacol 68:479-91. 2004
    Regulation of the rolipram-sensitive cAMP-specific phosphodiesterase 4 (PDE4) gene family was studied in rat pulmonary microvascular endothelial cells (RPMVECs)...
  97. ncbi Paradoxical cAMP-induced lung endothelial hyperpermeability revealed by Pseudomonas aeruginosa ExoY
    Sarah L Sayner
    Center for Lung Biology, University of South Alabama, College of Medicine, Mobile, AL 36688, USA
    Circ Res 95:196-203. 2004
    ..These findings collectively illustrate a previously unrecognized mechanism of hyperpermeability induced by rises in cytosolic cAMP...
  98. ncbi Increased levels of cyclic adenosine monophosphate contribute to the hyporesponsiveness of mast cells in alloxan diabetes
    Emiliano O Barreto
    Laboratory of Inflammation, Physiology and Pharmacodynamics Department, Oswaldo Cruz Institute, Oswaldo Cruz Foundation, Av. Brasil, no 4365, Manguinhos, Rio de Janeiro, CEP 21045-900, Brazil
    Int Immunopharmacol 4:755-62. 2004
    ..Incubation of normal mast cells with selective inhibitors of phosphodiesterase type 4 (PDE 4) rolipram, NCS 613 and RP 73401, or the cell permeable analogue N6-2'-O-dibutyryladenosine 3':5'-cyclic monophosphate (db ..
  99. ncbi Alpha1-antitrypsin, old dog, new tricks. Alpha1-antitrypsin exerts in vitro anti-inflammatory activity in human monocytes by elevating cAMP
    Sabina M Janciauskiene
    Department of Clinical Sciences, University Hospital Malmo, Lund University, SE 20502 Malmo, Sweden
    J Biol Chem 282:8573-82. 2007
    ..necrosis factor-alpha and interleukin-10 was enhanced when the catabolism of cAMP was blocked by the phosphodiesterase inhibitor rolipram. These effects were still observed with modified forms of AAT lacking protease inhibitor activity.
  100. ncbi Phosphoinositide 3-kinase is involved in Xenopus and Labrus melanophore aggregation
    Tony P M Andersson
    Division of Pharmacology, Department of Medicine and Care, Faculty of Health Sciences, Linkoping University, SE 581 85 Linkoping, Sweden
    Cell Signal 15:1119-27. 2003
    ..In Xenopus aggregation, we suggest that melatonin stimulation of the Mel1c receptor via G(beta gamma) activates PI3-K that, directly or indirectly via MAPK, activates PDE...
  101. ncbi Regulation of the cAMP-elevating effects of isoproterenol and forskolin in cardiac myocytes by treatments that cause increases in cAMP
    Hong Cui
    Department of Pharmacology MC 868, School of Medicine, University of Illinois at Chicago, 835 S Wolcott Avenue, Chicago, IL 60612, USA
    Biochem Biophys Res Commun 307:119-26. 2003
    ....

Research Grants72

  1. PKA-Hypothermia Bridge: A New Therapeutic Approach for Traumatic Brain Injury
    Larry W Jenkins; Fiscal Year: 2010
    ..To this end, we found that the activation of PKA activity with Rolipram, (a type IV phosphodiesterase inhibitor [PDE4] which increases cAMP levels and PKA activation) and reduced ..
  2. HEMORHEOLOGICAL FACTORS IN CEREBRAL ISCHEMIA
    Mark Fisher; Fiscal Year: 2009
    ..the in vivo role of PDE4 and PDE4D in the brain microvascular response to endotoxin, using rats pretreated with rolipram and mice null for PDE4D...
  3. Up-regulation of Mucin Gene Transcription-Otitis Media
    Jian dong Li; Fiscal Year: 2010
    ..preliminary studies indicate that MKP-1 itself is further negatively controlled by phosphodiesterase 4B (PDE4B);Rolipram, a specific inhibitor of PDE4 that has been already in late phase III clinical trial for asthma and COPD, ..
  4. CRYSTAL STRUCT. OF CYCLIC NUCLEOTIDE PHOSPHODIESTERASE
    Hengming Ke; Fiscal Year: 2003
    ..including (1) the catalytic domain of PDE4B, (2) the catalytic domain of PDE4B complexed with the inhibitors rolipram and iodonated cAMP, (3) full length PDE4D and its complexes with the inhibitors rolipram and denbufylline and (4) ..
  5. Effects of Lead on Cortical Development and Plasticity
    MARY A WILSON; Fiscal Year: 2010
    ..be blocked by the NMDA antagonist dextromethorphan, inhibition of Ras with FPT III, or inhibition of PDE4 with rolipram, 3) to determine whether postnatal lead exposure increases or decreases phosphorylation of CREB, ERK1/2 or CaMKIV ..
  6. Effects of Lead on Cortical Development and Plasticity
    Mary Wilson; Fiscal Year: 2009
    ..be blocked by the NMDA antagonist dextromethorphan, inhibition of Ras with FPT III, or inhibition of PDE4 with rolipram, 3) to determine whether postnatal lead exposure increases or decreases phosphorylation of CREB, ERK1/2 or CaMKIV ..
  7. Novel A2A Adenosine Agonists in Vascular Protection
    Jayson Rieger; Fiscal Year: 2005
    ..combined used of two synergistic anti-inflammatory compounds, ATL146e, an agonist of A2A adenosine receptors, and rolipram, a type IV phosphodiesterase (PDE) inhibitor, loaded into a proprietary nanoporous stent coating, inhibits stent ..
  8. PKA-Hypothermia Bridge: A New Therapeutic Approach for Traumatic Brain Injury
    Larry Jenkins; Fiscal Year: 2009
    ..To this end, we found that the activation of PKA activity with Rolipram, (a type IV phosphodiesterase inhibitor [PDE4] which increases cAMP levels and PKA activation) and reduced ..
  9. HEMORHEOLOGICAL FACTORS IN CEREBRAL ISCHEMIA
    Mark J Fisher; Fiscal Year: 2010
    ..the in vivo role of PDE4 and PDE4D in the brain microvascular response to endotoxin, using rats pretreated with rolipram and mice null for PDE4D...
  10. HEMORHEOLOGICAL FACTORS IN CEREBRAL ISCHEMIA
    Mark Fisher; Fiscal Year: 2007
    ..the in vivo role of PDE4 and PDE4D in the brain microvascular response to endotoxin, using rats pretreated with rolipram and mice null for PDE4D...
  11. Cyclic Nucleotide Regulation in Traumatic Brain Injury
    W Dalton Dietrich; Fiscal Year: 2009
    ..In other models of CMS injury, the phosphodiesterase (PDE) IV inhibitor rolipram, which prevents the degradation of cAMP, improves neuronal survival, axonal regeneration, and decreases ..
  12. Cyclic Nucleotide Regulation in Traumatic Brain Injury
    W DALTON DALTON DIETRICH; Fiscal Year: 2010
    ..In other models of CMS injury, the phosphodiesterase (PDE) IV inhibitor rolipram, which prevents the degradation of cAMP, improves neuronal survival, axonal regeneration, and decreases ..
  13. Regulation of CXCR4 by cognate and non-cognate ligands
    Elias Lolis; Fiscal Year: 2010
    ..in the glioblastoma mouse model required an increase on cAMP and that the cAMP phosphodiesterase inhibitor rolipram had similar therapeutic effects as CXCR4 antagonism due to an increase in cAMP...
  14. APOPTOSIS IN NORMAL AND MALIGNANT LYMPHOCYTES
    Adam Lerner; Fiscal Year: 2003
    ..CLL cells contained PDE4B transcript, protein and enzymatic activity. Inhibition of PDE4 by rolipram raised cAMP levels and induced apoptosis in CLL cells in a dose dependent fashion that required 48 hours to ..
  15. Phosphodiesterase-inhibitors, vascular integrity and SCI
    Raymond Grill; Fiscal Year: 2009
    ..We propose to determine whether acute treatment with 2 PDE-ls, a specific PDE4a-inhibitor called rolipram and a non- selective PDE-I known as pentoxifylline reduce protein extravasation following SCI; protecting the ..
  16. Phosphodiesterase-inhibitors, vascular integrity and SCI
    Raymond J Grill; Fiscal Year: 2010
    ..We propose to determine whether acute treatment with 2 PDE-ls, a specific PDE4a-inhibitor called rolipram and a non- selective PDE-I known as pentoxifylline reduce protein extravasation following SCI;protecting the BSCB ..
  17. Phosphodiesterase-inhibitors, vascular integrity and SCI
    Raymond Grill; Fiscal Year: 2007
    ..We propose to determine whether acute treatment with 2 PDE-ls, a specific PDE4a-inhibitor called rolipram and a non- selective PDE-I known as pentoxifylline reduce protein extravasation following SCI; protecting the ..
  18. LPS-PEPTIDE INTERACTION IN BLADDER INFLAMMATION
    Ricardo Saban; Fiscal Year: 2003
    ..cystitis and that treatment with a proteosome inhibitor (lactacystin) or phosphodiestase 4 inhibitor (rolipram) blocks both the expression of NF-kB genes and inflammation...
  19. Cyclic AMP-mediated apoptosis in lymphoid malignancies
    Adam Lerner; Fiscal Year: 2009
    Inhibitors of type 4 cAMP phosphodiesterase (PDE4) such as rolipram-induced apoptosis in B cell chronic lymphocytic leukemia, even in the absence of exogenous pharmacologic agents that activate adenylate cyclase such as the diterpene ..
  20. Exploring the role of Phosphodiesterase 4A in axonal regeneration
    Benjamin Sachs; Fiscal Year: 2007
    ..Indeed, rolipram, an inhibitor of type four phosphodiesterases (PDE4s), the enzymes responsible for cAMP degradation, has been ..
  21. NEUROPSYCHOPHARMACOLOGY OF CYCLIC AMP PDE INHIBITORS
    JAMES O DONNELL; Fiscal Year: 2002
    ..inhibitors in rats in two behavioral tasks, behavior maintained under a DRL 72-sec schedule and a two-lever rolipram drug discrimination procedure, with their inhibition of recombinant rat PDE4A, PDE4B, PDE4C, and PDE4D...
  22. NEUROPSYCHOPHARMACOLOGY OF CYCLIC AMP PDE INHIBITORS
    JAMES O DONNELL; Fiscal Year: 2007
    Inhibitors of Type 4 cyclic AMP phosphodiesterase (PDE4), such as rolipram, produce both antidepressant-like and memory-enhancing effects in preclinical models...
  23. EFFICIENT SYNTHESIS OF BIOACTIVE GAMMA LACTAMS
    KYUNG JUNG; Fiscal Year: 2005
    ..Our synthetic targets encompass lactacystin, pramanicin, statine, rolipram, epolactaene, and kainic acid...
  24. Pathology and Biology of Neurodegenerative Disease
    Michael Shelanski; Fiscal Year: 2007
    The demonstration that the drugs rolipram and forskalin reverse the inhibition of LTP induced by alpha beta in hippocampal slices and that exposure of cultured hippocampal neurons to alpha beta causes changes in expression of genes ..
  25. Axon Regenration: Synergistic Actions of the MAPK and Cyclic AMP Pathways
    Damien Pearse; Fiscal Year: 2009
    ..a one-time injection of cAMP into the cord above and below the implant, and a two-week subcutaneous infusion of Rolipram induced substantial growth of serotonergic fibers into the implant and beyond into the cord caudal to the implant...