phosphinic acids

Summary

Summary: Inorganic or organic derivatives of phosphinic acid, H2PO(OH). They include phosphinates and phosphinic acid esters.

Top Publications

  1. pmc The N domain of human angiotensin-I-converting enzyme: the role of N-glycosylation and the crystal structure in complex with an N domain-specific phosphinic inhibitor, RXP407
    Colin S Anthony
    Division of Medical Biochemistry, Institute of Infectious Diseases and Molecular Medicine, University of Cape Town, Anzio Road, Observatory 7925, South Africa
    J Biol Chem 285:35685-93. 2010
  2. ncbi Roles of the two active sites of somatic angiotensin-converting enzyme in the cleavage of angiotensin I and bradykinin: insights from selective inhibitors
    Dimitris Georgiadis
    Laboratory of Organic Chemistry, Department of Chemistry, University of Athens, Panepistimiopolis, Zografou, Athens, Greece
    Circ Res 93:148-54. 2003
  3. ncbi Effects of electrically coupled inhibitory networks on local neuronal responses to intracortical microstimulation
    Sergejus Butovas
    Hertie Institute for Clinical Brain Research, Department of Cognitive Neurology, University Tübingen, Otfried Müller Str 27, 72076 Tubingen, Germany
    J Neurophysiol 96:1227-36. 2006
  4. pmc RXP 407, a phosphinic peptide, is a potent inhibitor of angiotensin I converting enzyme able to differentiate between its two active sites
    V Dive
    Departement d Etudes et d Ingéniérie des Protéines, Commissariat a l Energie Atomique, CE Saclay, 91191 Gif sur Yvette, France
    Proc Natl Acad Sci U S A 96:4330-5. 1999
  5. ncbi Investigating the domain specificity of phosphinic inhibitors RXPA380 and RXP407 in angiotensin-converting enzyme
    Wendy L Kröger
    Division of Medical Biochemistry, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Observatory, Cape Town 7935, South Africa
    Biochemistry 48:8405-12. 2009
  6. ncbi Metabotropic glutamate receptor 4 novel agonist LSP1-2111 with anxiolytic, but not antidepressant-like activity, mediated by serotonergic and GABAergic systems
    Joanna M Wieronska
    Institute of Pharmacology, Polish Academy of Sciences, 31 343 Krakow, Poland
    Neuropharmacology 59:627-34. 2010
  7. ncbi Development of domain-selective angiotensin I-converting enzyme inhibitors
    Pierre Redelinghuys
    Division of Medical Biochemistry, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Cape Town, South Africa
    Ann N Y Acad Sci 1056:160-75. 2005
  8. pmc Novel mechanism of inhibition of human angiotensin-I-converting enzyme (ACE) by a highly specific phosphinic tripeptide
    Mohd Akif
    Department of Biology and Biochemistry, University of Bath, Claverton Down, Bath BA2 7AY, UK
    Biochem J 436:53-9. 2011
  9. ncbi RXP 407, a selective inhibitor of the N-domain of angiotensin I-converting enzyme, blocks in vivo the degradation of hemoregulatory peptide acetyl-Ser-Asp-Lys-Pro with no effect on angiotensin I hydrolysis
    C Junot
    Commissariat a l Energie Atomique, Service de Pharmacologie et d Immunologie, Gif sur Yvette, France
    J Pharmacol Exp Ther 297:606-11. 2001
  10. ncbi Aldehyde and phosphinate analogs of glutathione and glutathionylspermidine: potent, selective binding inhibitors of the E. coli bifunctional glutathionylspermidine synthetase/amidase
    C H Lin
    Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, 240 Longwood Avenue, Boston, MA 02115, USA
    Chem Biol 4:859-66. 1997

Detail Information

Publications224 found, 100 shown here

  1. pmc The N domain of human angiotensin-I-converting enzyme: the role of N-glycosylation and the crystal structure in complex with an N domain-specific phosphinic inhibitor, RXP407
    Colin S Anthony
    Division of Medical Biochemistry, Institute of Infectious Diseases and Molecular Medicine, University of Cape Town, Anzio Road, Observatory 7925, South Africa
    J Biol Chem 285:35685-93. 2010
    ..0 Å resolution. The Ndom389 structure revealed a hinge region that may contribute to the breathing motion proposed for substrate binding...
  2. ncbi Roles of the two active sites of somatic angiotensin-converting enzyme in the cleavage of angiotensin I and bradykinin: insights from selective inhibitors
    Dimitris Georgiadis
    Laboratory of Organic Chemistry, Department of Chemistry, University of Athens, Panepistimiopolis, Zografou, Athens, Greece
    Circ Res 93:148-54. 2003
    ..Based on these findings, it might be suggested that the gene duplication of ACE in vertebrates may represent a means for regulating the cleavage of Ang I differently from that of BK...
  3. ncbi Effects of electrically coupled inhibitory networks on local neuronal responses to intracortical microstimulation
    Sergejus Butovas
    Hertie Institute for Clinical Brain Research, Department of Cognitive Neurology, University Tübingen, Otfried Müller Str 27, 72076 Tubingen, Germany
    J Neurophysiol 96:1227-36. 2006
    ..Electrical coupling renders evoked cortical inhibition more precise and strong and ensures a uniform spread along the two cardinal axes of neocortical geometry...
  4. pmc RXP 407, a phosphinic peptide, is a potent inhibitor of angiotensin I converting enzyme able to differentiate between its two active sites
    V Dive
    Departement d Etudes et d Ingéniérie des Protéines, Commissariat a l Energie Atomique, CE Saclay, 91191 Gif sur Yvette, France
    Proc Natl Acad Sci U S A 96:4330-5. 1999
    ....
  5. ncbi Investigating the domain specificity of phosphinic inhibitors RXPA380 and RXP407 in angiotensin-converting enzyme
    Wendy L Kröger
    Division of Medical Biochemistry, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Observatory, Cape Town 7935, South Africa
    Biochemistry 48:8405-12. 2009
    ..Taken together, these data advance our understanding regarding the molecular basis for the remarkable ACE domain selectivity exhibited by these inhibitors...
  6. ncbi Metabotropic glutamate receptor 4 novel agonist LSP1-2111 with anxiolytic, but not antidepressant-like activity, mediated by serotonergic and GABAergic systems
    Joanna M Wieronska
    Institute of Pharmacology, Polish Academy of Sciences, 31 343 Krakow, Poland
    Neuropharmacology 59:627-34. 2010
    ..Moreover, the compound was not effective in 5-HT depleted animals. The results of these studies indicate that the GABAergic and serotonergic systems are involved in the potential anxiolytic action of LSP1-2111...
  7. ncbi Development of domain-selective angiotensin I-converting enzyme inhibitors
    Pierre Redelinghuys
    Division of Medical Biochemistry, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Cape Town, South Africa
    Ann N Y Acad Sci 1056:160-75. 2005
    ..This review summarizes the structural basis and recent synthetic chemistry approaches to the development of novel domain-selective inhibitors...
  8. pmc Novel mechanism of inhibition of human angiotensin-I-converting enzyme (ACE) by a highly specific phosphinic tripeptide
    Mohd Akif
    Department of Biology and Biochemistry, University of Bath, Claverton Down, Bath BA2 7AY, UK
    Biochem J 436:53-9. 2011
    ..These features, for the first time, highlight the unusual architecture and flexibility of the active site of C-ACE, which could be further utilized for structure-based design of new C-ACE or vasopeptidase inhibitors...
  9. ncbi RXP 407, a selective inhibitor of the N-domain of angiotensin I-converting enzyme, blocks in vivo the degradation of hemoregulatory peptide acetyl-Ser-Asp-Lys-Pro with no effect on angiotensin I hydrolysis
    C Junot
    Commissariat a l Energie Atomique, Service de Pharmacologie et d Immunologie, Gif sur Yvette, France
    J Pharmacol Exp Ther 297:606-11. 2001
    ..Thus, RXP 407 is the first ACE inhibitor that might be used to control selectively AcSDKP metabolism with no effect on blood pressure regulation...
  10. ncbi Aldehyde and phosphinate analogs of glutathione and glutathionylspermidine: potent, selective binding inhibitors of the E. coli bifunctional glutathionylspermidine synthetase/amidase
    C H Lin
    Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, 240 Longwood Avenue, Boston, MA 02115, USA
    Chem Biol 4:859-66. 1997
    ..In E. coli, the Gsp synthetase is part of a bifunctional enzyme opposed by the hydrolytic Gsp amidase...
  11. pmc Opposing efficacy of group III mGlu receptor activators, LSP1-2111 and AMN082, in animal models of positive symptoms of schizophrenia
    Joanna M Wieronska
    Institute of Pharmacology, Polish Academy of Sciences, 31 343, Krakow, Poland
    Psychopharmacology (Berl) 220:481-94. 2012
    ..Several studies have suggested that modulation of the glutamatergic system via metabotropic glutamate receptors (mGlu) could be a new and efficient way to achieve antipsychotic-like activity...
  12. ncbi On the mechanism of anti-hyperthermic effects of LY379268 and LY487379, group II mGlu receptors activators, in the stress-induced hyperthermia in singly housed mice
    J M Wieronska
    Institute of Pharmacology, Polish Academy of Sciences, Smetna 12, 31 343 Krakow, Poland
    Neuropharmacology 62:322-31. 2012
    ..Therefore, it seems that the antagonism towards GABA(A) receptors, presynaptic 5-HT(1A) and postsynaptic 5-HT(2A/2C) receptors is responsible for the phenomenon. This article is part of a Special Issue entitled 'Anxiety and Depression'...
  13. pmc The GABA B receptor agonist CGP44532 and the positive modulator GS39783 reverse some behavioural changes related to positive syndromes of psychosis in mice
    J M Wieronska
    Department of Neurobiology, Institute of Pharmacology PAS, 31 343 Krakow, Poland
    Br J Pharmacol 163:1034-47. 2011
    ..The GABA(B) receptor antagonists CGP51176 and CGP36742, agonist CGP44532 and positive allosteric modulator GS39783 were studied...
  14. ncbi Electrophysiological and behavioral evidence that modulation of metabotropic glutamate receptor 4 with a new agonist reverses experimental parkinsonism
    Corinne Beurrier
    Institut de Biologie du Developpement de Marseille Luminy, UMR 6216 CNRS Université de la Méditerranée, Marseille, France
    FASEB J 23:3619-28. 2009
    ..Finally, systemic administration of LSP1-2111 counteracts haloperidol-induced catalepsy, opening promising perspectives for the development of antiparkinsonian therapeutic strategies focused on orthosteric mGlu4-receptor agonists...
  15. ncbi Effect of lesogaberan, a novel GABA(B)-receptor agonist, on transient lower oesophageal sphincter relaxations in male subjects
    G E Boeckxstaens
    Academic Medical Center, Amsterdam, The Netherlands
    Aliment Pharmacol Ther 31:1208-17. 2010
    ..Transient lower oesophageal sphincter relaxations (TLESRs) are a major mechanism behind gastro-oesophageal reflux disease (GERD)...
  16. ncbi Synthesis of p-aminophenyl aryl H-phosphinic acids and esters via cross-coupling reactions: elaboration to phosphinic acid pseudopeptide analogues of pteroyl glutamic acid and related antifolates
    Yonghong Yang
    Departments of Medicinal Chemistry and Chemistry, University of Michigan, Ann Arbor, MI 48109 1055, USA
    J Org Chem 72:5748-58. 2007
    The synthesis of suitably protected p-aminophenyl H-phosphinic acids and esters from the corresponding para-substituted aryl halides has been accomplished via the Pd-catalyzed cross-coupling reaction of anilinium hypophosphite, either in ..
  17. pmc Role of ionotropic glutamate receptors in long-term potentiation in rat hippocampal CA1 oriens-lacunosum moleculare interneurons
    Iris Oren
    Institute of Neurology, University College London, London WC1N 3BG, United Kingdom
    J Neurosci 29:939-50. 2009
    ..Glutamatergic synapses on O-LM cells thus behave in a homogeneous manner and exhibit LTP dependent on Ca(2+)-permeable AMPA receptors...
  18. ncbi Effects of lesogaberan on reflux and lower esophageal sphincter function in patients with gastroesophageal reflux disease
    Guy E Boeckxstaens
    Academic Medical Centre, Amsterdam, The Netherlands
    Gastroenterology 139:409-17. 2010
    ....
  19. ncbi Structural determinants of RXPA380, a potent and highly selective inhibitor of the angiotensin-converting enzyme C-domain
    Dimitris Georgiadis
    Laboratory of Organic Chemistry, Department of Chemistry, University of Athens, Panepistimiopolis Zografou, 15771 Athens, Greece
    Biochemistry 43:8048-54. 2004
    ..The structural insights provided by this study should enhance understanding of the factors controlling the selectivity of the two domains of somatic ACE and allow the design of new selective ACE inhibitors...
  20. ncbi (R)-(3-amino-2-fluoropropyl) phosphinic acid (AZD3355), a novel GABAB receptor agonist, inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action
    Anders Lehmann
    AstraZeneca R and D, Molndal, Sweden
    J Pharmacol Exp Ther 331:504-12. 2009
    ..In summary, AZD3355 probably inhibits TLESR through stimulation of peripheral GABA(B) receptors and may offer a potential new approach to treatment of GERD...
  21. ncbi Combined use of selective inhibitors and fluorogenic substrates to study the specificity of somatic wild-type angiotensin-converting enzyme
    Nicolas D Jullien
    CEA, Département d Ingénerie et d Etudes des Protéines, Gif Yvette, France
    FEBS J 273:1772-81. 2006
    ..These results raise concerns about the interpretation of functional studies performed in animals using N-domain and C-domain substrate selectivity data derived only from human ACE...
  22. ncbi Phosphinic acid pseudopeptides analogous to glutamyl-gamma-glutamate: synthesis and coupling to pteroyl azides leads to potent inhibitors of folylpoly-gamma-glutamate synthetase
    N Valiaeva
    Departments of Medicinal Chemistry and Chemistry, University of Michigan, Ann Arbor, Michigan 48109-1055, USA
    J Org Chem 66:5146-54. 2001
    ....
  23. ncbi Functional conservation of the active sites of human and Drosophila angiotensin I-converting enzyme
    D Coates
    School of Biology, University of Leeds, Leeds LS2 9JT, UK
    Biochemistry 39:8963-9. 2000
    ..The conservation of ACE enzymes with distinct active sites in the evolution of both vertebrate and invertebrate species provides further evidence that these two kinds of active sites have different physiological functions...
  24. ncbi Computer-aided optimization of phosphinic inhibitors of bacterial ureases
    Stamatia Vassiliou
    Department of Bioorganic Chemistry, Faculty of Chemistry, Wrocław University of Technology, Wrocław, Poland
    J Med Chem 53:5597-606. 2010
    ..The designed compounds represent a competitive reversible class of urease inhibitors. The most potent, N-methyl-aminomethyl-P-hydroxymethylphosphinic acid, displayed K(i) = 360 nM against P. vulgaris enzyme...
  25. ncbi Potent inhibition of human folylpolyglutamate synthetase by a phosphinic acid mimic of the tetrahedral reaction intermediate
    John J McGuire
    Grace Cancer Drug Center, Roswell Park Cancer Institute, Elm and Carlton Streets, Buffalo, NY 14263, USA
    Biochem Pharmacol 65:315-8. 2003
    ..Because of its exceedingly high potency as an FPGS inhibitor, MTX-phosphinate represents a lead structure from which cell-permeable analogs may be developed to test the hypothesis that FPGS inhibition is therapeutically efficacious...
  26. pmc Prodrug forms of N-[(4-deoxy-4-amino-10-methyl)pteroyl]glutamate-gamma-[psiP(O)(OH)]-glutarate, a potent inhibitor of folylpoly-gamma-glutamate synthetase: synthesis and hydrolytic stability
    Yan Feng
    Department of Medicinal Chemistry, University of Michigan, Ann Arbor, Michigan 48109 1055, USA
    J Med Chem 49:770-88. 2006
    ..H-phosphinic acids derived from N-Cbz vinyl glycine esters were converted to the desired pseudopeptides by Michael addition to ..
  27. pmc A stereoselective synthesis of phosphinic acid phosphapeptides corresponding to glutamyl-gamma-glutamate and incorporation into potent inhibitors of folylpoly-gamma-glutamyl synthetase
    David M Bartley
    Departments of Medicinal Chemistry and Chemistry, University of Michigan, Ann Arbor, MI 48109 1055, USA
    J Org Chem 70:6757-74. 2005
    ....
  28. ncbi Phosphinic peptides as zinc metalloproteinase inhibitors
    V Dive
    Départment d Ingénierie et d Etudes des Protéines DIEP, CEA, CE Saclay, 91191, Gif Yvette Cedex, France
    Cell Mol Life Sci 61:2010-9. 2004
    ..Specific properties of the inhibitors produced in recent years are reviewed, supporting the notion that phosphinic pseudo-peptides are useful tools for studying the structural and functional biology of zinc proteases...
  29. ncbi The structure of testis angiotensin-converting enzyme in complex with the C domain-specific inhibitor RXPA380
    Hazel R Corradi
    Department of Biology and Biochemistry, University of Bath, Claverton Down, Bath BA2 7AY, United Kingdom
    Biochemistry 46:5473-8. 2007
    ..The characterization of the extended active site and the binding of a potent C-domain-selective inhibitor provide the first structural data for the design of truly domain-specific pharmacophores...
  30. ncbi Nucleus-specific abnormalities of GABAergic synaptic transmission in a genetic model of absence seizures
    Thomas Bessaïh
    Neurobiologie des Processus Adaptatifs, UMR 7102 CNRS, Universite Pierre et Marie Curie Paris 6, 9 Quai St Bernard, 75252 Paris Cedex 05, France
    J Neurophysiol 96:3074-81. 2006
    ....
  31. ncbi 5-Hydroxytryptamine 1B receptors mediate presynaptic inhibition of monosynaptic IPSC in the rat dorsolateral septal nucleus
    Toshimasa Matsuoka
    Department of Physiology, Kurume University School of Medicine, 67 Asahi Machi, Kurume 830 0011, Japan
    Neurosci Res 48:229-38. 2004
    ..These results suggest that activation of presynaptic 5-HT1B receptors depresses the release of GABA via a pertussis toxin (PTX)-sensitive G-protein in the rat DLSN...
  32. ncbi Distinct properties of presynaptic group II and III metabotropic glutamate receptor-mediated inhibition of perforant pathway-CA1 EPSCs
    Marco Capogna
    Medical Research Council, Anatomical Neuropharmacology Unit, Mansfield Road, Oxford OX1 3TH, UK
    Eur J Neurosci 19:2847-58. 2004
    ..Groups II and III mGluRs are segregated at the presynaptic terminal, and there are distinct differences between the properties of the presynaptic inhibition mediated by these two groups of receptors...
  33. ncbi Distinct properties of functional KCC2 expression in immature mouse hippocampal neurons in culture and in acute slices
    Stanislav Khirug
    Department of Biological and Environmental Sciences, University of Helsinki, Helsinki, Finland
    Eur J Neurosci 21:899-904. 2005
    ....
  34. ncbi GABAergic modulation of the activity of globus pallidus neurons in primates: in vivo analysis of the functions of GABA receptors and GABA transporters
    Adriana Galvan
    Department of Neurology, Emory University, Atlanta, GA 30322, USA
    J Neurophysiol 94:990-1000. 2005
    ....
  35. ncbi Modulation of the components of the rat dark-adapted electroretinogram by the three subtypes of GABA receptors
    Anna Möller
    Department of Physiology, University of Iceland IS 101 Reykjavik, Iceland
    Vis Neurosci 20:535-42. 2003
    ..OPs are modified by stimulation of GABAa receptors, and the a- and b-waves by stimulation of all GABA receptor subtypes...
  36. ncbi The spinal GABAergic system is a strong modulator of burst frequency in the lamprey locomotor network
    David E Schmitt
    Nobel Inst for Neurophysiology, Dept of Neuroscience, Karolinska Institutet, SE 17177 Stockholm, Sweden
    J Neurophysiol 92:2357-67. 2004
    ..It is not required for burst generation, but acts as a powerful modulator...
  37. ncbi Mechanism of GABA receptor-mediated inhibition of spontaneous GABA release onto cerebellar Purkinje cells
    Victoria L Harvey
    Department of Pharmacology, University College London, Gower Street, London WC1E 6BT, UK
    Eur J Neurosci 20:684-700. 2004
    ..Together, these results suggest that GABA(B) inhibition occurs downstream of Ca(2+) influx and may be mediated, in part, by an inhibition of the vesicular release mechanism...
  38. ncbi Presynaptic NMDA autoreceptors facilitate axon excitability: a new molecular target for the anticonvulsant gabapentin
    Luz M Suárez
    Servicio de Neurobiologia, Dpto de Investigación, Hospital Ramon y Cajal, Ctra de Colmenar Km 9, Madrid 28034, Spain
    Eur J Neurosci 21:197-209. 2005
    ..These findings suggest that sodium entry through presynaptic NMDA-R channels facilitates axon excitability. The interaction of gabapentin with this newly described mechanism might contribute to its therapeutic benefits...
  39. ncbi Intraglomerular inhibition: signaling mechanisms of an olfactory microcircuit
    Gabe J Murphy
    Neuroscience Graduate Program and Department of Neuroscience, University of California, San Diego, La Jolla, California 92093 0608, USA
    Nat Neurosci 8:354-64. 2005
    ..Ca(2+) spikes in periglomerular cells are evoked by powerful excitatory inputs from a single principal cell, and glutamate release from the dendrites of single principal neurons activates a large ensemble of periglomerular cells...
  40. ncbi Pharmacology of GABAC receptors: responses to agonists and antagonists distinguish A- and B-subtypes of homomeric rho receptors expressed in Xenopus oocytes
    Yi Pan
    Department of Ophthalmology and Visual Sciences, University of Illinois College of Medicine, 1855 West Taylor Street, Chicago, IL 60612, USA
    Neurosci Lett 376:60-5. 2005
    ..These results indicate that, in addition to the characteristic response properties identified previously, there is a pattern of pharmacological reactions that further distinguishes the A- and B-subtypes of GABA rho receptor...
  41. ncbi GABAB receptor antagonist-mediated antidepressant-like behavior is serotonin-dependent
    David A Slattery
    Neuroscience Research, Novartis Institutes for BioMedical Research WSJ 386 344, Novartis, Basel, CH 4002, Switzerland
    J Pharmacol Exp Ther 312:290-6. 2005
    ..Together, these data demonstrate that GABA(B) receptor antagonists via an interaction with the serotonergic system display antidepressant-like properties and therefore represent a novel approach for the treatment of depression...
  42. ncbi Synaptic depolarizing GABA Response in adults is excitatory and proconvulsive when GABAB receptors are blocked
    Joshua T Kantrowitz
    Department of Physiology and Pharmacology, SUNY Downstate Medical Center, Brooklyn, NY 11203, USA
    J Neurophysiol 93:2656-67. 2005
    ..We show here that GABA(B) receptors exert control over the synaptic depolarizing GABA response and that block of GABA(B) receptors makes the depolarizing GABA response excitatory and proconvulsive...
  43. ncbi Cortical injury affects short-term plasticity of evoked excitatory synaptic currents
    Huifang Li
    Department of Neurology and Neurological Sciences, Room M016, 300 Pasteur Dr, Stanford, CA 94305 5122, USA
    J Neurophysiol 93:146-56. 2005
    ..Results are compatible with an increase in the probability of transmitter release at excitatory synapses in undercut cortex due to functional changes in presynaptic terminals...
  44. ncbi GABAB receptors in the medial septum/diagonal band slice from 16-25 day rat
    Z Henderson
    School of Biomedical Sciences, Worsley Building, University of Leeds, Leeds LS2 9JT, UK
    Neuroscience 132:789-800. 2005
    ..These results suggest that GABA(B) receptors modulate rather than generate rhythmic activity in the MS/DB, and that this modulatory effect occurs via receptors located on presynaptic terminals...
  45. pmc Anticonvulsant enaminones depress excitatory synaptic transmission in the rat brain by enhancing extracellular GABA levels
    Samuel B Kombian
    Department of Applied Therapeutics, Faculty of Pharmacy, Kuwait University, PO Box 24923, Safat 13110, Kuwait
    Br J Pharmacol 145:945-53. 2005
    ..Our data suggest that anticonvulsant enaminones cause EPSC depression by enhancing extracellular GABA levels possibly through the inhibition of either GABA reuptake or GABA-T enzyme, or both...
  46. ncbi Enaminones and norepinephrine employ convergent mechanisms to depress excitatory synaptic transmission in the rat nucleus accumbens in vitro
    Samuel B Kombian
    Department of Applied Therapeutics, Faculty of Pharmacy, Health Sciences Centre, Kuwait University, PO Box 24923, Safat 13110, Kuwait
    Eur J Neurosci 24:2781-8. 2006
    ....
  47. ncbi Effects of mu-opioid receptor modulation on GABAB receptor synaptic function in hippocampal CA1
    A Rory McQuiston
    Department of Anatomy and Neurobiology, Virginia Commonwealth University Medical Center, Richmond, Virginia 23298, USA
    J Neurophysiol 97:2301-11. 2007
    ..Therefore MOR suppresses GABA(B) synaptic hyperpolarizations in all layers of CA1 and most effectively facilitates excitatory activity in CA1 output layers...
  48. ncbi Characterization of the glycinergic input to bipolar cells of the mouse retina
    Elena Ivanova
    Department Neuroanatomy, Max Planck Institute for Brain Research, Frankfurt Main, Germany
    Eur J Neurosci 23:350-64. 2006
    ..Thus, different bipolar cell types receive kinetically fast glycinergic inputs, preferentially mediated by GlyRs composed of alpha1 and beta subunits...
  49. ncbi Functional evidence for GABA as modulator of the contractility of the longitudinal muscle in mouse duodenum: role of GABA(A) and GABA(C) receptors
    Maria Grazia Zizzo
    Dipartimento di Biologia Cellulare e dello Sviluppo, Laboratorio di Fisiologia generale, Universita di Palermo, Viale delle Scienze, 90128 Palermo, Italy
    Neuropharmacology 52:1685-90. 2007
    ....
  50. ncbi Dual GABAergic synaptic response of fast excitation and slow inhibition in the medial habenula of rat epithalamus
    Uhnoh Kim
    Department of Neurosurgery and Interdisciplinary Neuroscience Program, College of Medicine, Pennsylvania State University, Hershey, PA 17033 0850, USA
    J Neurophysiol 98:1323-32. 2007
    ..Our study demonstrates that the dual activation of GABAergic excitation and inhibition through GABA A Rs and GABA B Rs generates distinct temporal patterns of cell firing that alter the cellular output in an activity-dependent manner...
  51. pmc GABA(B) receptor modulation of feedforward inhibition through hippocampal neurogliaform cells
    Christopher J Price
    Medical Research Council Anatomical Neuropharmacology Unit, Oxford OX1 3TH, United Kingdom
    J Neurosci 28:6974-82. 2008
    ..The NGFC-CA1 pyramidal cell connection therefore provides a unique and subtle mechanism to shape the integration time domain for signals arriving via a major excitatory input to CA1 pyramidal cells...
  52. ncbi Activation of presynaptic GABA(A) receptors induces glutamate release from parallel fiber synapses
    Brandon M Stell
    Laboratoire de Physiologie Cérébrale, Unité de Formation et de Recherche Biomédicale, Universite Paris Descartes, 75006 Paris, France
    J Neurosci 27:9022-31. 2007
    ..From these data, we conclude that GABA(A)Rs located on parallel fibers depolarize parallel fiber terminals beyond the threshold for Na+ channel activation and thereby induce glutamate release onto MLIs and Purkinje cells...
  53. ncbi Enantioselective actions of 4-amino-3-hydroxybutanoic acid and (3-amino-2-hydroxypropyl)methylphosphinic acid at recombinant GABA(C) receptors
    Tina Hinton
    The Adrien Albert Laboratory of Medicinal Chemistry, Department of Pharmacology, The University of Sydney, NSW 2006, Australia
    Bioorg Med Chem Lett 18:402-4. 2008
    ..These studies highlight the different stereochemical requirements for the hydroxy group in these analogues at GABA(A), GABA(B) and GABA(C) receptors...
  54. ncbi Influence of positive allosteric modulators on GABA(B) receptor coupling in rat brain: a scintillation proximity assay characterisation of G protein subtypes
    Clotilde Mannoury La Cour
    Psychopharmacology Department, Institut de Recherche Servier, Croissy sur Seine, France
    J Neurochem 105:308-23. 2008
    ..PAMs more markedly enhanced efficacy of coupling to Go versus Gi(1/3). It will be of interest to confirm these observations employing complementary techniques and to evaluate their potential therapeutic significance...
  55. ncbi Regulation of synaptic input to hypothalamic presympathetic neurons by GABA(B) receptors
    Q Chen
    Department of Anesthesiology, Pennsylvania State University College of Medicine, Hershey, PA 17033, USA
    Neuroscience 142:595-606. 2006
    ..This presynaptic action of GABA(B) receptors is mediated by the N-ethylmaleimide-sensitive G(i/o) proteins, but independent of voltage-gated Ca2+ and K+ channels...
  56. ncbi Hippocampal partial kindling decreased hippocampal GABAB receptor efficacy and wet dog shakes in rats
    L Stan Leung
    Department of Physiology and Pharmacology, University of Western Ontario, London, Ontario, Canada N6A5C1
    Behav Brain Res 173:274-81. 2006
    ....
  57. pmc Cellular and behavioral interactions of gabapentin with alcohol dependence
    Marisa Roberto
    Committee on the Neurobiology of Addictive Disorders, Pearson Center for Alcoholism and Addiction Research, The Scripps Research Institute, La Jolla, California 92037, USA
    J Neurosci 28:5762-71. 2008
    ....
  58. ncbi Distinct mechanisms of presynaptic inhibition at GABAergic synapses of the rat substantia nigra pars compacta
    Michela Giustizieri
    Centro Europeo di Ricerca sul Cervello Fondazione Santa Lucia Istituto di Ricovero e Cura a Carattere Scientifico, Via del Fosso di Fiorano, 64, 00143 Rome, Italy
    J Neurophysiol 94:1992-2003. 2005
    ..These results indicate that group III mGluRs depress GABA release to DA neurons of the SNc through inhibition of presynaptic VDCCs, while presynaptic GABA(B) receptors directly impair transmitter exocytosis...
  59. ncbi Mechanisms contributing to the exacerbated epileptiform activity in hippocampal slices expressing a C-terminal truncated GABA(B2) receptor subunit
    Sébastien J Thuault
    Neurology and GI CEDD, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Epilepsy Res 65:41-51. 2005
    ....
  60. ncbi Nicotine-induced switch in the nicotinic cholinergic mechanisms of facilitation of long-term potentiation induction
    Yoshihiko Yamazaki
    Department of Neurobiology and Behavior, University of California, Irvine, CA 92697 4550, USA
    Eur J Neurosci 22:845-60. 2005
    ..These ACh-independent mechanisms probably contribute to the nicotine-induced cognitive enhancement observed in the presence of cholinergic deficits, such as those in Alzheimer's disease patients...
  61. ncbi An NMDA receptor/nitric oxide cascade is involved in cerebellar LTD but is not localized to the parallel fiber terminal
    Jung Hoon Shin
    Department of Neuroscience, The Johns Hopkins University School of Medicine, Baltimore, MD 21205, USA
    J Neurophysiol 94:4281-9. 2005
    ..These results are consistent with the hypothesis that an NMDA receptor/NO cascade involved in cerebellar LTD is localized to interneurons rather than parallel fibers...
  62. ncbi Independent roles of calcium and voltage-dependent potassium currents in controlling spike frequency adaptation in lateral amygdala pyramidal neurons
    E S Louise Faber
    Queensland Brain Institute, University of Queensland, Brisbane, QLD 4072, Australia
    Eur J Neurosci 22:1627-35. 2005
    ..This dual mechanism of controlling firing patterns is unique to lateral amygdala neurons and is likely to contribute to the very low levels of firing seen in lateral amygdala neurons in vivo...
  63. ncbi Evidence for a functional role of GABA receptors in the rat mature hippocampus
    Anniina Alakuijala
    Institute of Biotechnology, PO Box 56, FI 00014 University of Helsinki, Finland
    Eur J Neurosci 23:514-20. 2006
    ..The lack of GABA(C) receptor activation by less intensive stimulation under control conditions suggests that these receptors are extrasynaptic and activated via spillover of synaptically released GABA...
  64. ncbi GABA(B) receptor-activation inhibits GABAergic synaptic transmission in parvocellular neurones of rat hypothalamic paraventricular nucleus
    X Liu
    Department of Basic Neuroscience, University Medical Centre, Geneva, Switzerland
    J Neuroendocrinol 18:177-86. 2006
    ..Activation of these receptors causes disinhibition of parvocellular neurosecretory and nonendocrine paraventricular neurones...
  65. ncbi Concentration-dependent effects of anticonvulsant enaminone methyl 4-(4'-bromophenyl)aminocyclohex-3-en-6-methyl-2-oxo-1-oate on neuronal excitability in vitro
    K V V Ananthalakshmi
    Department of Applied Therapeutics, Faculty of Pharmacy, Kuwait University, P O Box 24923, Safat 13110, Kuwait
    Neuroscience 141:345-56. 2006
    ..These two actions of methyl 4-(4'-bromophenyl)aminocyclohex-3-en-6-methyl-2-oxo-1-oate on neuronal excitability would have therapeutic implications in future clinical use of enaminones as anticonvulsants in seizure disorders...
  66. ncbi Origins of GABA(A) and GABA(B) receptor-mediated responses of globus pallidus induced after stimulation of the putamen in the monkey
    Hitoshi Kita
    Department of Anatomy and Neurobiology, College of Medicine, University of Tennessee, Memphis, Tennessee 38163, USA
    J Neurosci 26:6554-62. 2006
    ....
  67. ncbi Developmental decrease in short-term facilitation at Schaffer collateral synapses in hippocampus is mGluR1 sensitive
    Haley E Speed
    Department of Neurobiology, Civitan International Research Center, University of Alabama at Birmingham, Birmingham, AL, USA
    J Neurophysiol 99:799-813. 2008
    ....
  68. ncbi Cloning and functional expression of GABA(B) receptors from Drosophila
    M Mezler
    Bayer AG, Agricultural Centre, Molecular Target Research, Geb 6240, Alfred Nobel Strasse 50, 40789 Monheim, Germany
    Eur J Neurosci 13:477-86. 2001
    ..The pharmacology of the coexpressed D-GABA(B)R1/2 receptor was different from the mammalian GABA(B)Rs: e.g. baclofen, an agonist of mammalian GABA(B)Rs, showed no effect...
  69. ncbi Spontaneous epileptiform activity mediated by GABA(A) receptors and gap junctions in the rat hippocampal slice following long-term exposure to GABA(B) antagonists
    Marylka Uusisaari
    University of Helsinki, Department of Biosciences, Division of Animal Physiology, PO Box 65 Viikinkaari 1, Finland
    Neuropharmacology 43:563-72. 2002
    ..These data suggest that enhanced GABAergic activity with functional interneuronal connectivity via gjs is sufficient to trigger epileptiform activity in the absence of ionotropic glutamatergic transmission...
  70. ncbi GABAergic modulation of primary gustatory afferent synaptic efficacy
    Andrew A Sharp
    Department of Cellular and Structural Biology, University of Colorado Health Sciences Center, Denver, Colorado 80262, USA
    J Neurobiol 52:133-43. 2002
    ..The mechanism of action of GABA(B) receptors suggests a presynaptic locus of action for that receptor...
  71. ncbi Comparison of receptive field expansion produced by GABA(B) and GABA(A) receptor antagonists in raccoon primary somatosensory cortex
    S A Chowdhury
    Department of Physiology and Biophysics, Dalhousie University, Halifax, Nova Scotia, Canada B3H 4H7
    Exp Brain Res 144:114-21. 2002
    ..These results indicate that both GABA(B) and GABA(A) receptors play a role in shaping the normal receptive fields in somatosensory cortex...
  72. pmc Regulation of muscarinic acetylcholine receptor-mediated synaptic responses by GABA(B) receptors in the rat hippocampus
    R A Morton
    MRC Centre for Synaptic Plasticity, University of Bristol, University Walk, Bristol BS8 1TD, UK
    J Physiol 535:757-66. 2001
    ..The mechanism of inhibition may involve both pre- and postsynaptic elements...
  73. ncbi Recombinant GABA(B) receptors formed from GABA(B1) and GABA(B2) subunits selectively inhibit N-type Ca(2+) channels in NG108-15 cells
    Alison Easter
    Division of Neuroscience Pharmacology, Medical School, University of Birmingham, Edgbaston, Birmingham, B15 2TT, UK
    Eur J Pharmacol 440:17-25. 2002
    ..In fact, in differentiated NG108-15 cells, the recombinant GABA(B) receptors couple only to N-type Ca(2+) channels...
  74. pmc Differential ontogeny of GABA(B)-receptor-mediated pre- and postsynaptic modulation of GABA and glycine transmission in respiratory rhythm-generating network in mouse
    W Zhang
    Centre of Physiology and Pathophysiology, University of Gottingen, 37073 Gottingen, Germany
    J Physiol 540:435-46. 2002
    ..GABA(B)-receptor-mediated presynaptic modulation develops with a longer postnatal latency, and becomes predominant within the first postnatal week...
  75. ncbi GABA(B) presynaptic inhibition has an in vivo time constant sufficiently rapid to allow modulation at theta frequency
    Bradley J Molyneaux
    Department of Psychology, Program in Neuroscience, Boston University, 64 Cummington Street, Boston, MA 02215, USA
    J Neurophysiol 87:1196-205. 2002
    ..This heterosynaptic depression was significantly reduced by local infusion of the GABA(B) receptor antagonist CGP55845A...
  76. ncbi Contribution of GABA(A) and GABA(B) receptors to thalamic neuronal activity during spontaneous absence seizures in rats
    R Staak
    Institute of Physiology, Medical School, Otto-von-Guericke University, 39120 Magdeburg, Germany
    J Neurosci 21:1378-84. 2001
    ..This conclusion is in support of the view that the two subtypes of GABA receptors play a differential role in fast (5-10 Hz) and slow (3 Hz) spike-wave paroxysms observed during absence seizures...
  77. ncbi In vivo modulation of ventral tegmental area dopamine and glutamate efflux by local GABA(B) receptors is altered after repeated amphetamine treatment
    M Giorgetti
    Department of Neuroscience, FUHS The Chicago Medical School, North Chicago, IL 60064 3095, USA
    Neuroscience 109:585-95. 2002
    ..This is the first demonstration, in an intact animal, that drugs of abuse alter GABA(B) receptor transmission in the ventral tegmental area...
  78. ncbi Pre- and postsynaptic inhibition mediated by GABA(B) receptors in cerebellar inhibitory interneurons
    Puah Mann-Metzer
    Department of Neurobiology, Institute of Life Sciences and the Interdisciplinary Center for Neuronal Computation, Hebrew University, Jerusalem 91904, Israel
    J Neurophysiol 87:183-90. 2002
    ..These can serve a modulatory role as well as participating in shaping the temporal interactions between consecutive inputs...
  79. ncbi GABAC receptor sensitivity is modulated by interaction with MAP1B
    D Billups
    Laboratory for Molecular Cell Biology, Department of Pharmacology, University College London, London, WC1E 6BT, United Kingdom
    J Neurosci 20:8643-50. 2000
    ..Thus, anchoring to the cytoskeleton lowers the sensitivity of GABA(C) receptors and provides a likely site for functional modulation of GABA(C) receptor-mediated inhibition...
  80. ncbi The ATP-mediated fast current of rat dorsal root ganglion neurons is a novel effector for GABA(B) receptor activation
    Elena Sokolova
    Biophysics Sector and INFM Unit, International School for Advanced Studies SISSA, Via Beirut 4, 34014 Trieste, Italy
    Neurosci Lett 338:181-4. 2003
    ..It is suggested that, on nociceptive DRG neurons, GABA produced slow inhibition of P2X(3) receptors via metabotropic GABA(B) receptors...
  81. ncbi Electrophysiological characterization of "giant" cells in stratum radiatum of the CA3 hippocampal region
    N Savic
    Neuroscience Programme and Istituto Nazionale Fisica della Materia Unit, International School for Advanced Studies SISSA, 34014 Trieste, Italy
    J Neurophysiol 85:1998-2007. 2001
    ..We conclude that CA3 giant cells represent a particular class of hippocampal neuron located in st. radiatum that shares only some morphological and physiological properties with principal cells...
  82. ncbi GABAC receptors in the rat superior colliculus and pretectum participate in synaptic neurotransmission
    Mathias Boller
    Department of Zoology and Neurobiology, Ruhr University, D 44780 Bochum, Germany
    J Neurophysiol 89:2035-45. 2003
    ..We conclude that GABA(C) receptors are, at least partially, located synaptically in SC and pretectal neurons in the rat, which indicates a direct function of this receptor type for synaptic processing in both structures...
  83. ncbi Presynaptic and postsynaptic GABAA receptors in rat suprachiasmatic nucleus
    M A Belenky
    Department of Cell and Animal Biology Institute of Life Sciences, Hebrew University of Jerusalem, Jerusalem 91904, Israel
    Neuroscience 118:909-23. 2003
    ..Our results thus show that GABA(A) receptors are widely distributed in the SCN and may subserve both pre- and postsynaptic roles in controlling the mammalian circadian clock...
  84. ncbi Lamina-specific differences in GABA(B) autoreceptor-mediated regulation of spontaneous GABA release in rat entorhinal cortex
    Sarah J Bailey
    Department of Physiology and MRC Synaptic Plasticity Centre, School of Medical Sciences, University of Bristol, University Walk, BS8 1TD, Bristol, UK
    Neuropharmacology 46:31-42. 2004
    ..This demonstrates that GABA(B) autoreceptors are tonically activated by synaptically released GABA in layer V, and this may partly explain the lower level of spontaneous GABA release in the deep layer...
  85. pmc Regulation of EPSPs by the synaptic activation of GABAB autoreceptors in rat hippocampus
    C H Davies
    Department of Pharmacology, University of Edinburgh, UK
    J Physiol 496:451-70. 1996
    ..regulation of AMPA and NMDA receptor-mediated EPSPs during various patterns of synaptic activation caused by the dynamic changes in GABA-mediated synaptic inhibition, which are orchestrated by GABAA autoreceptors in a frequency-dependent..
  86. ncbi Effects of intrahippocampal injection of GABAergic drugs on memory retention of passive avoidance learning in rats
    M R Zarrindast
    Department of Pharmacology, School of Medicine, Tehran University of Medical Sciences, Tehran, Iran
    J Psychopharmacol 16:313-9. 2002
    ..Atropine decreased memory retention by itself and potentiated the response of muscimol and baclofen. It is concluded that GABAA and GABAB receptor activation may be involved in the impairment of memory retention...
  87. ncbi Analysis of gamma-aminobutyric acid-mediated responses in the pulmonary vascular bed of the cat
    Alan D Kaye
    Department of Anesthesiology, Texas Tech University Health Sciences, 3601 4th Street, Room 1C282, Lubbock, TX 79430, USA
    Anesth Analg 99:758-63, table of contents. 2004
    ..Further, SKF-97541-induced vasodepression is mediated or modulated by an ATP-sensitive K(+) channel...
  88. pmc Antitussive effects of GABAB agonists in the cat and guinea-pig
    D C Bolser
    Schering Plough Research Institute, Kenilworth, NJ 07033 0539
    Br J Pharmacol 110:491-5. 1993
    ..v.) and 3-aminopropylphosphonic acid (3 mg kg-1, i.v.).6. We show that baclofen and 3-APPi have antitussive effects in the guinea-pig and cat and these effects are mediated by GABAB receptors...
  89. pmc GABAB receptor-positive modulators: enhancement of GABAB receptor agonist effects in vivo
    Wouter Koek
    Department of Psychiatry, University of Texas Health Science Center, San Antonio, TX 78229 3900, USA
    J Pharmacol Exp Ther 335:163-71. 2010
    ..Taken together, the results provide further evidence of pharmacologically distinct GABA(B) receptor subtypes, possibly allowing for a more selective therapeutic interference with the GABA(B) system...
  90. ncbi Effects of GABA(B) receptor agents on cocaine priming, discrete contextual cue and food induced relapses
    Małgorzata Filip
    Laboratory of Drug Addiction Pharmacology, Department of Pharmacology, Institute of Pharmacology, Polish Academy of Sciences, 31 343 Krakow, 12 Smetna, Poland
    Eur J Pharmacol 571:166-73. 2007
    ....
  91. ncbi Cholinergic inhibition of neocortical pyramidal neurons
    Allan T Gulledge
    Division of Neuroscience, John Curtin School of Medical Research, Australian National University, Canberra, Australia
    J Neurosci 25:10308-20. 2005
    ..These data demonstrate that acetylcholine can directly inhibit the output of neocortical pyramidal neurons...
  92. ncbi Pharmacological and autoradiographic studies on the pathophysiological role of GABA(B) receptors in the dystonic hamster: pronounced antidystonic effects of baclofen after striatal injections
    S E Sander
    Institute of Pharmacology and Toxicology, Faculty of Veterinary Medicine, Freie Universitat Berlin, Koserstr 20, 14195 Berlin, Germany
    Neuroscience 162:423-30. 2009
    ..In view of the absence of striatal changes in GABA(B) binding, the strong antidystonic effect of baclofen after its striatal microinjection is probably related to a suppression of a pathophysiologically increased synaptic activity...
  93. ncbi Kynurenic acid blocks nicotinic synaptic transmission to hippocampal interneurons in young rats
    Trevor W Stone
    Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8Q, UK
    Eur J Neurosci 25:2656-65. 2007
    ....
  94. ncbi Characterization of the antiabsence effects of SCH 50911, a GABA-B receptor antagonist, in the lethargic mouse, gamma-hydroxybutyrate, and pentylenetetrazole models
    D A Hosford
    Department of Medicine Neurology, Duke University, Duke University Medical Center, Durham, North Carolina, USA
    J Pharmacol Exp Ther 274:1399-403. 1995
    ..These findings suggest that antiabsence activity may be a defining feature of GABAB receptor antagonists and provide a rationale for pursuing clinical trials of GABAB receptor antagonists in human patients with absence seizures...
  95. pmc Structure of malonic acid-based inhibitors bound to human neutrophil collagenase. A new binding mode explains apparently anomalous data
    H Brandstetter
    Max Planck Institut fur Biochemie, Abteilung Strukturforschung, Martinsried, Germany
    Protein Sci 7:1303-9. 1998
    ..Various classes of MMP inhibitors, including hydroxamic acids, phosphinic acids, and thiols, have been previously described...
  96. pmc GABA(B) receptor modulators potentiate baclofen-induced depression of dopamine neuron activity in the rat ventral tegmental area
    Ying Chen
    Eli Lilly and Co Ltd, Erl Wood Manor, Sunninghill Road, Windlesham, Surrey GU20 6PH
    Br J Pharmacol 144:926-32. 2005
    ..This finding suggests a therapeutic potential for GABA(B) potentiators for the treatment of diseases associated with a hyperfunctional mesocorticolimbic system...
  97. ncbi Gamma-aminobutyric acidB (GABAB)-receptor mediation of different in vivo effects of gamma-butyrolactone
    Mauro A M Carai
    CNR Institute of Neuroscience, Cagliari, Italy
    J Pharmacol Sci 106:199-207. 2008
    ..Vice versa, NCS-382 failed to exert any antagonistic or protective effect. These results suggest that the in vivo GBL effects tested in the present study are mediated by activation of the GABA(B) receptor...
  98. ncbi GABAergic system and imipramine-induced impairment of memory retention in rats
    M R Zarrindast
    Department of Pharmacology, Tehran University of Medical Science and Department of Biology, Shaheed Beheshti University, Tehran, Iran
    Eur Neuropsychopharmacol 14:59-64. 2004
    ..It is concluded that the GABA(B) receptor mechanism is involved in memory impairment induced by imipramine...
  99. pmc Behavioral effects of gamma-hydroxybutyrate, its precursor gamma-butyrolactone, and GABA(B) receptor agonists: time course and differential antagonism by the GABA(B) receptor antagonist 3-aminopropyl(diethoxymethyl)phosphinic acid (CGP35348)
    Wouter Koek
    Department of Psychiatry, University of Texas Health Science Center at San Antonio, 7703 Floyd Curl Drive, Mail Code 7792, San Antonio, TX 78229 3900, USA
    J Pharmacol Exp Ther 330:876-83. 2009
    ..A better understanding of the similarities and differences between these mechanisms, and their involvement in the therapeutic effects of GHB and baclofen, could lead to more effective medications with fewer adverse effects...
  100. ncbi Bis[2-(3-carboxyphenoxy)carbonylethyl]phosphinic acid (m-BCCEP): a novel affinity cross-linking reagent for the beta-cleft modification of human hemoglobin
    Hongyi Cai
    Laboratory for Drug Design and Synthesis, Department of Chemistry and Biochemistry, University of Maryland Baltimore County, 1000 Hilltop Circle, Baltimore, MD 21250, USA
    Bioconjug Chem 21:1494-507. 2010
    ..19 Torr) assayed under identical conditions. The measured Hill coefficient value of 1.91 of the m-BCCEP-modified Hb product points to the reasonable retainment of oxygen-binding cooperativity after the cross-link formation...
  101. ncbi Synthesis of α-carboxyphosphinopeptides derived from norleucine
    Jan Picha
    Institute of Organic Chemistry and Biochemistry, v v i, Academy of Sciences of the Czech Republic, Flemingovo namesti 2, 166 10, Prague 6, Czech Republic
    Amino Acids 39:1265-80. 2010
    ....

Research Grants25

  1. Enantioselective Synthesis of Phosphinate Derivatives
    John Cong Gui Zhao; Fiscal Year: 2012
    ..Additionally, this research also offers an excellent opportunity for training the students from the underrepresented groups in the cutting-edge area of organocatalysis. ..
  2. RATIONAL DRUG DESIGN BASED ON CHEMICAL MECHANISMS
    JAMES COWARD; Fiscal Year: 2005
    ..5. Complete the stereoselective synthesis of (2S) 3.3-difluoroglutamic acid and its incorporation into appropriate gammaglutamyl peptides for use in mechanistic studies of GH and FPGS catalysis. ..
  3. H-Phosphinic Acids in the Preparation of Active Organophosphorus Compounds
    Jean Luc Montchamp; Fiscal Year: 2008
    This proposal aims at the development of H-phosphinic acids (RP(O)(OH)H) as synthetic intermediates for the preparation of biologically-active phosphorus-containing compounds...
  4. Neuropharmacology of GHB discrimination
    Wouter Koek; Fiscal Year: 2010
    ..Increased knowledge about the activation and modulation of GABAB systems will help to develop effective approaches to treating sleep-, drug abuse-, and other CNS disorders. ..
  5. Discriminative Stimulus Effects of Alcohol in Mice
    Wouter Koek; Fiscal Year: 2007
    ..This future research will increase our understanding of risk factors for alcoholism and drug abuse and will help the development of effective approaches to prevention and treatment. [unreadable] [unreadable] [unreadable]..
  6. Epidemiologic Case-control Study of Barrett's Esophagus
    Nicholas Shaheen; Fiscal Year: 2005
    ..Finally, by comparing subjects with Barrett's to controls with reflux, and controlling for severs of reflux, the impact of a Barrett's diagnosis on quality of life and psychological stress may be seen. ..
  7. The Perception of Cancer Risk in Patients with Barrett's Esophagus
    Nicholas Shaheen; Fiscal Year: 2007
    ..The resultant study application will assess health-related quality of life, health-related anxiety and healthcare utilization as outcomes. [unreadable] [unreadable]..
  8. FOLYLPOLYGLUTAMATE SYNTHETASE IN CANCER CHEMOTHERAPY
    John McGuire; Fiscal Year: 2003
    ..This may explain why high-level resistance to pulse MTX can occur in the absence of a large decrease in total FPGS activity or a rise in glutamyl hydrolase activity. ..
  9. Enhancement of methotrexate uptake in childhood ALL
    John McGuire; Fiscal Year: 2009
    ..If successful, this research could provide a way to increase the effectiveness of methotrexate, a key drug used in treating childhood acute lymphoblastic leukemia, and thus increase the cure rate in this disease. ..
  10. Cannabinoids and Central Neuronal Activity
    Paul Schweitzer; Fiscal Year: 2005
    ..abstract_text> ..
  11. Synaptic Transmission, Plasticity and Integration in the Subthalamic Nucleus
    Mark D Bevan; Fiscal Year: 2010
    ..abstract_text> ..
  12. MOP Receptor Effects on the Hippocampal CA1 Network
    ADAM MCQUISTON; Fiscal Year: 2008
    ..The results from these studies will provide important information regarding MOP receptor-induced changes in network activity and may possibly lead to the development of treatments for opioid addiction. ..
  13. Serotonin Receptor Subtypes: Regulation and Interaction
    JULIE HENSLER; Fiscal Year: 2008
    ..Studies of the regulation of 5-HT1A receptor function may have important implications for our understanding the role of this receptor in the therapeutic action of drugs used to treat mental illness [unreadable] [unreadable]..
  14. MICROBIAL METABOLISM OF REDUCED PHOSPHORUS COMPOUNDS
    WILLIAM METCALF; Fiscal Year: 2008
    ..unreadable] [unreadable]..
  15. Cue-Reactivity and Alcohol Self-Dosing
    Elise Weerts; Fiscal Year: 2003
    ..This research will additionally provide important information on the behavioral processes underlying conditioned responses to drug-related cues in animals which may be relevant to cue-reactivity and drug-taking in humans. ..
  16. MORPHOLOGIC BASIS FOR CENTRAL VESTIBULAR INHIBITION
    GAY HOLSTEIN; Fiscal Year: 2002
    ....
  17. 5HT transporter & 1A receptor function in BDNF mice
    JULIE HENSLER; Fiscal Year: 2007
    ..Region-specific and age-dependent changes in BDNF protein levels will be determined in selected brain regions of wild-type and BDNF () mice (Aim #3). [unreadable] [unreadable] [unreadable]..
  18. Altered Function of a GABA-A receptor epilepsy mutation
    Mathew Jones; Fiscal Year: 2007
    ..abstract_text> ..
  19. GABA Modulation of Cocaine & Heroin Self-Administration
    David Roberts; Fiscal Year: 2003
    ..The degree to which either IP or intracerebral injections of baclofen affect heroin self-administration will also be assessed. ..
  20. Behavioral Pharmacology and GHB Physical Dependence
    Elise M Weerts; Fiscal Year: 2010
    ..Physical dependence in the context of self-injection of GHB, GBL and 1,4-BD will also be evaluated. These studies will provide critical information on the behavioral pharmacology and dependence-producing effects of GHB. ..
  21. Alcohol Sensitivity and PET Derived Measures of Opioid Activity
    Elise M Weerts; Fiscal Year: 2010
    ..The results of the proposed research will increase our understanding of to the relationship between individual variability in the opioid system and subjective sensitivity to alcohol. ..
  22. Alcohol Modulation of Cerebellar Synaptic Currents
    William Proctor; Fiscal Year: 2006
    ..The combination of our proposed and ongoing genetic studies may aid the identification of more sensitive drug targets and the development of novel drugs for rational therapeutic approaches to alcoholism. ..
  23. Studies on the role of GABA in Cocaine Addiction
    Elise Weerts; Fiscal Year: 2005
    ..The results of these studies will increase our understanding of the role of GABA in the behavioral effects of cocaine and may lead to the development of better medications for the treatment of cocaine addiction. ..
  24. Chemoanatomic bases for peripheral vestibular function
    GAY HOLSTEIN; Fiscal Year: 2007
    ..The proposed research is unique, and will have direct bearing on the development of more effective therapeutic interventions, both medicinal and device-oriented, for peripheral vestibular disorders. [unreadable] [unreadable] [unreadable]..
  25. Functional Recovery of Sensory Input to Olfactory Bulb
    DALE WACHOWIAK; Fiscal Year: 2009
    ..This work could potentially yield insight into treatment strategies for these and other syndromes related to inappropriate neuronal connections. ..