Genomes and Genes
Summary: A group of compounds with the heterocyclic ring structure of benzo(c)pyridine. The ring structure is characteristic of the group of opium alkaloids such as papaverine. (From Stedman, 25th ed)
Publications340 found, 100 shown here
- In vivo imaging of microglial activation with [11C](R)-PK11195 PET in idiopathic Parkinson's diseaseAlexander Gerhard
MRC Clinical Sciences Centre and Division of Neuroscience, Faculty of Medicine, Imperial College, London, UK
Neurobiol Dis 21:404-12. 2006..The absence of significant longitudinal changes suggests that microglia are activated early in the disease process, and levels then remain relatively static, possibly driving the disease via cytokine release...
- Sanguinarine induces apoptosis of HT-29 human colon cancer cells via the regulation of Bax/Bcl-2 ratio and caspase-9-dependent pathwayJun Sik Lee
Heart Research Center of Chonnam National University Hospital, Cardiovascular Research Institute of Chonnam National University, Gwangju 501 757, Korea
Int J Toxicol 31:70-7. 2012..Our results suggest that sanguinarine induces apoptosis of HT-29 human colon cancer cells and may have a potential therapeutic use in the treatment of human colon cancer...
- In-vivo measurement of activated microglia in dementiaA Cagnin
MRC Cyclotron Unit, Imperial College, Faculty of Medicine, Division of Neuroscience and Psychological Medicince, Hammersmith Hospital, London, UK
Lancet 358:461-7. 2001..INTERPRETATION: In-vivo detection of increased [11C](R)-PK11195 binding in Alzheimer-type dementia, including mild and early forms, suggests that microglial activation is an early event in the pathogenesis of the disease...
- Improved prevention of moderately emetogenic chemotherapy-induced nausea and vomiting with palonosetron, a pharmacologically novel 5-HT3 receptor antagonist: results of a phase III, single-dose trial versus dolasetronPeter Eisenberg
California Cancer Care, Greenbrae, California, USA
Cancer 98:2473-82. 2003..The current Phase III trial evaluated the efficacy and safety of palonosetron in preventing acute and delayed CINV after moderately emetogenic chemotherapy...
- Mixed-affinity binding in humans with 18-kDa translocator protein ligandsDavid R J Owen
Division of Experimental Medicine, Imperial College, Hammersmith Hospital, London, United Kingdom
J Nucl Med 52:24-32. 2011....
- Transcriptional activation of the NF-kappaB p65 subunit by mitogen- and stress-activated protein kinase-1 (MSK1)Linda Vermeulen
Department of Molecular Biology, University of Gent VIB, K L Ledeganckstraat 35, B 9000 Gent, Belgium
EMBO J 22:1313-24. 2003..This effect represents, together with phosphorylation of nucleosome components such as histone H3, an essential step leading to selective transcriptional activation of NF-kappaB-dependent gene expression...
- Palonosetron exhibits unique molecular interactions with the 5-HT3 receptorCamilo Rojas
Research and Translational Development, MGI PHARMA INC, 6611 Tributary St, Baltimore, MD 21224 6515, USA
Anesth Analg 107:469-78. 2008..However, these attributes alone are not sufficient to explain the results with palonosetron. We sought to elucidate additional differences among 5-HT(3)-RAs that could help explain the observations in the clinic...
- Evaluation of anticancer activities of benzo[c]phenanthridine alkaloid sanguinarine in oral squamous cell carcinoma cell lineHikari Tsukamoto
Department of Oral and Maxillofacial Surgery, School of Dentistry, Showa University, Ota ku, Tokyo, Japan
Anticancer Res 31:2841-6. 2011..Taken together, these results indicate that sanguinarine is a potential inhibitor of tumorigenesis and suggest that it may be valuable in the development of new anticancer drugs for the treatment of OSCC...
- Sanguinarine induces apoptosis of human osteosarcoma cells through the extrinsic and intrinsic pathwaysHyunjin Park
Cell Biomaterial Biohybrid Systems, Universite de Sherbrooke, Department of Chemical Engineering and Biotechnological Engineering, Canada J1K 2R1
Biochem Biophys Res Commun 399:446-51. 2010..It activated multicaspases, and increased the activities of caspase-8 and caspase-9 in both MG-63 and SaOS-2 cells. These data highlight sanguinarine as a novel potential agent for bone cancer therapy...
- Reference and target region modeling of [11C]-(R)-PK11195 brain studiesFederico E Turkheimer
Division of Neuroscience, Department of Clinical Neuroscience, Imperial College London, London, United Kingdom
J Nucl Med 48:158-67. 2007....
- Development of a tracer kinetic plasma input model for (R)-[11C]PK11195 brain studiesMarc A Kropholler
Department of Nuclear Medicine and PET Research, VU University Medical Center, Amsterdam, The Netherlands
J Cereb Blood Flow Metab 25:842-51. 2005..It was concluded that a two-tissue reversible compartment model with K(1)/k(2) fixed to whole cortex value is optimal for analyzing (R)-[(11)C]PK11195 PET brain studies...
- Promotion of sleep by targeting the orexin system in rats, dogs and humansCatherine Brisbare-Roch
Research and Development, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil, Switzerland
Nat Med 13:150-5. 2007..No signs of cataplexy were observed, in contrast to the rodent, dog or human narcolepsy syndromes. These results open new perspectives for investigating the role of endogenous orexins in sleep-wake regulation...
- Palonosetron triggers 5-HT(3) receptor internalization and causes prolonged inhibition of receptor functionCamilo Rojas
Johns Hopkins University School of Medicine, Brain Science Institute Neurotranslational Center, 6611 Tributary Street, Baltimore, MD 21224 6515, USA
Eur J Pharmacol 626:193-9. 2010..These experiments may provide a pharmacological basis for differences noted in published clinical trials comparing palonosetron to other 5-HT(3) receptor antagonists...
- The many faces of H89: a reviewA Lochner
Dept Biomedical Sciences, Faculty of Health Sciences, University of Stellenbosch, Tygerberg, South Africa
Cardiovasc Drug Rev 24:261-74. 2006..H-89 should be used in conjunction with other PKA inhibitors, such as Rp-cAMPS or PKA analogs...
- Antiproliferative activity of ecteinascidin 743 is dependent upon transcription-coupled nucleotide-excision repairY Takebayashi
Laboratory of Molecular Pharmacology, National Cancer Institute/NIH, Bethesda, Maryland, USA
Nat Med 7:961-6. 2001..We found that Et743 interacts with the transcription-coupled NER machinery to induce lethal DNA strand breaks...
- Imaging microglial activation in Huntington's diseaseYen F Tai
Division of Neuroscience and Psychological Medicine, Hammersmith Hospital, Imperial College London, UK
Brain Res Bull 72:148-51. 2007..Further longitudinal studies are needed to fully elucidate this link...
- Evolution of microglial activation in patients after ischemic stroke: a [11C](R)-PK11195 PET studyAlexander Gerhard
MRC Clinical Sciences Centre and Department of Neuropathology, Faculty of Medicine, Imperial College, London, UK
Neuroimage 24:591-5. 2005..Our data suggest that [11C](R)-PK11195 PET can be used to investigate both the primary lesion and remote pathological changes following Wallerian degeneration...
- Structures of three classes of anticancer agents bound to the human topoisomerase I-DNA covalent complexBart L Staker
deCODE BioStructures, 7869 NE Day Road West, Bainbridge Island, Washington 98110, USA
J Med Chem 48:2336-45. 2005..These new X-ray structures explain how very different molecules can stabilize top1-DNA covalent complexes and will aid the rational design of completely novel structural classes of anticancer drugs...
- A randomized, double-blind study to evaluate the efficacy and safety of three different doses of palonosetron versus placebo for preventing postoperative nausea and vomitingKeith A Candiotti
Department of Anesthesiology, University of Miami, Miami, Florida, USA
Anesth Analg 107:445-51. 2008....
- Palonosetron in combination with 1-day versus 3-day dexamethasone for prevention of nausea and vomiting following moderately emetogenic chemotherapy: a randomized, multicenter, phase III trialLuigi Celio
Medical Oncology Unit 2, Fondazione IRCCS Istituto Nazionale dei Tumori, Via Venezian 1, 20133, Milan, Italy
Support Care Cancer 19:1217-25. 2011....
- Hypocretin/orexin contributes to the expression of some but not all forms of stress and arousalTeri M Furlong
School of Medical Sciences, University of New South Wales, NSW 2052, Australia
Eur J Neurosci 30:1603-14. 2009..When it does, hypocretin will at least contribute to the cardiovascular response. The findings are of clinical relevance to some forms of psychological stress...
- Sanguinarine sensitizes human gastric adenocarcinoma AGS cells to TRAIL-mediated apoptosis via down-regulation of AKT and activation of caspase-3Woo Young Choi
Department of Biochemistry, Dongeui University College of Oriental Medicine, Yangjung Dong, Busanjin Gu, Busan 614 714, South Korea
Anticancer Res 29:4457-65. 2009....
- Isolation of the mitochondrial benzodiazepine receptor: association with the voltage-dependent anion channel and the adenine nucleotide carrierM W McEnery
Department of Neuroscience, Johns Hopkins University School of Medicine, Baltimore, MD 21205 2185
Proc Natl Acad Sci U S A 89:3170-4. 1992..VDAC and ADC, outer and inner mitochondrial membrane channel proteins, respectively, together with the 18-kDa subunit, may comprise mBzR at functionally important transport sites at the junction of two mitochondrial membranes...
- 18F-FEAC and 18F-FEDAC: PET of the monkey brain and imaging of translocator protein (18 kDa) in the infarcted rat brainJoji Yui
Molecular Imaging Center, National Institute of Radiological Sciences, Chiba, Japan
J Nucl Med 51:1301-9. 2010....
- Acute effect of palonosetron on electrocardiographic parameters in cancer patients: a prospective studyC Yavas
Department of Radiation Oncology, Konya Training and Research Hospital, Konya, Turkey
Support Care Cancer 20:2343-7. 2012..The acute cardiac effect of palonosteron is unknown. The purpose of this study is to determine acute effects of palonosetron on electrocardiographic (ECG) parameters in cancer patients...
- The interaction of RS 25259-197, a potent and selective antagonist, with 5-HT3 receptors, in vitroE H Wong
Institute of Pharmacology, Palo Alto, California 94303, USA
Br J Pharmacol 114:851-9. 19951. A series of isoquinolines have been identified as 5-HT3 receptor antagonists. One of these, RS 25259-197 [(3aS)-2-[(S)-1-azabicyclo[2.2...
- Imaging glial cell activation with [11C]-R-PK11195 in patients with AIDSDima A Hammoud
Department of Radiology, The Johns Hopkins Medical Institutions, Baltimore, Maryland 21287 2182, USA
J Neurovirol 11:346-55. 2005..The findings of this pilot study support a role for glial cell activation in HAD, and that PET with [11C]-R-PK11195 can detect the concomitants of neuronal damage in individuals infected with HIV...
- Peripheral benzodiazepine receptor ligands reverse apoptosis resistance of cancer cells in vitro and in vivoDidier Decaudin
Department of Hematology, and UMR 147 CNRS, Section de Recherche, Institut Curie, 75005 Paris, France
Cancer Res 62:1388-93. 2002..Peripheral benzodiazepine receptor ligands may therefore act as chemosensitizing agents for the treatment of human neoplasms...
- DNA-binding affinities and sequence selectivity of quaternary benzophenanthridine alkaloids sanguinarine, chelerythrine, and nitidineLi Ping Bai
School of Chinese Medicine, Hong Kong Baptist University, Kowloon Tong
Bioorg Med Chem 14:5439-45. 2006....
- The positron emission tomography ligand DAA1106 binds with high affinity to activated microglia in human neurological disordersSriram Venneti
Department of Pathology, University of Pittsburgh School of Medicine, and Presbyterian University Hospital, Neuropathology Division, Pittsburgh, Pennsylvania 15213, USA
J Neuropathol Exp Neurol 67:1001-10. 2008....
- Palonosetron: in the prevention of nausea and vomitingLily P H Yang
Adis, North Shore, Auckland, New Zealand
Drugs 69:2257-78. 2009..Intravenous palonosetron is a useful alternative to currently recommended agents in PONV prevention...
- An 18-kDa translocator protein (TSPO) polymorphism explains differences in binding affinity of the PET radioligand PBR28David R Owen
Division of Experimental Medicine, Department of Medicine, Imperial College London, Hammersmith Hospital, London, UK
J Cereb Blood Flow Metab 32:1-5. 2012....
- In vivo imaging of microglial activation with [11C](R)-PK11195 PET in corticobasal degenerationAlexander Gerhard
MRC Clinical Sciences Center and Division of Neuroscience, Faculty of Medicine, Imperial College, London, United Kingdom
Mov Disord 19:1221-6. 2004....
- Developmental regulation of protein kinase A expression and activity in Schistosoma mansoniBrett E Swierczewski
Department of Microbiology and Immunology, Uniformed Services University of the Health Sciences, Bethesda, MD, USA
Int J Parasitol 40:929-35. 2010..Taken together, our data suggest that PKA signalling is required for cercarial viability and may play a specific role in the reproductive activity of adult worms...
- Inhibition of Stat3 activation by sanguinarine suppresses prostate cancer cell growth and invasionMeng Sun
Department of Urology, University of California at Davis, Sacramento, California, USA
Prostate 72:82-9. 2012..Sanguinarine, a benzophenanthridine alkaloid derived primarily from the bloodroot plant, was identified previously as a novel inhibitor of survivin that selectively kills prostate cancer cells over "normal" prostate epithelial cells...
- [11C](R)-PK11195 PET imaging of microglial activation in multiple system atrophyA Gerhard
MRC Clinical Sciences Center and Division of Neuroscience, Faculty of Medicine, Imperial College, London, UK
Neurology 61:686-9. 2003..Providing an indicator of disease activity, [11C](R)-PK11195 PET can thus be used to characterize the in vivo neuropathology of MSA...
- Inhibition of lipopolysaccharide-induced cyclooxygenase-2, tumor necrosis factor-alpha and [Ca2+]i responses in human microglia by the peripheral benzodiazepine receptor ligand PK11195Hyan B Choi
Department of Pharmacology and Therapeutics, Division of Neurology, Faculty of Medicine, The University of British Columbia, 2176 Health Sciences Mall, Vancouver, British Columbia, Canada V6T 1Z3
J Neurochem 83:546-55. 2002....
- Palonosetron plus dexamethasone versus granisetron plus dexamethasone for prevention of nausea and vomiting during chemotherapy: a double-blind, double-dummy, randomised, comparative phase III trialMitsue Saito
Department of Breast Oncology, Juntendo University Hospital, Tokyo, Japan
Lancet Oncol 10:115-24. 2009....
- Comparative evaluation of the translocator protein radioligands 11C-DPA-713, 18F-DPA-714, and 11C-PK11195 in a rat model of acute neuroinflammationFabien Chauveau
CEA, DSV, I2BM, LIME, Orsay, France
J Nucl Med 50:468-76. 2009....
- Double-blind, randomised, controlled study of the efficacy and tolerability of palonosetron plus dexamethasone for 1 day with or without dexamethasone on days 2 and 3 in the prevention of nausea and vomiting induced by moderately emetogenic chemotherapyM Aapro
Division of Oncology, Institut Multidisciplinaire d Oncologie, Clinique de Genolier, Genolier, Switzerland
Ann Oncol 21:1083-8. 2010..We evaluated the possibility to reduce the total dose of corticosteroids when palonosetron, a long-acting second-generation 5-hydroxytryptamine-3 (5-HT(3)) receptor antagonist, is used...
- Novel indenoisoquinolines NSC 725776 and NSC 724998 produce persistent topoisomerase I cleavage complexes and overcome multidrug resistanceSmitha Antony
Laboratory of Molecular Pharmacology, National Cancer Institute, NIH, Bethesda, MD 20892 4255, USA
Cancer Res 67:10397-405. 2007..These gamma-H2AX foci were detectable at pharmacologically relevant doses for up to 24 h and thus could be used as biomarkers for clinical trials (phase 0)...
- Imaging brain inflammation with [(11)C]PK11195 by PET and induction of the peripheral-type benzodiazepine receptor after transient focal ischemia in ratsSantiago Rojas
Department of Brain Ischemia and Neurodegeneration, Institut d Investigacions Biomèdiques de Barcelona IIBB Consejo Superior de Investigaciones Científicas CSIC, Institut d Investigacions Biomediques August Pi i Sunyer IDIBAPS, Barcelona, Spain
J Cereb Blood Flow Metab 27:1975-86. 2007..These results show cellular heterogeneity in the level of PBR expression, supporting that PBR is not a simple marker of inflammation, and that the extent of [(11)C]PK11195 binding depends on intrinsic features of the inflammatory cells...
- Altered subcellular distribution of MSK1 induced by glucocorticoids contributes to NF-kappaB inhibitionIlse M E Beck
Laboratory of Eukaryotic Gene Expression and Signal Transduction, Department of Molecular Biology, Gent University, Gent, Belgium
EMBO J 27:1682-93. 2008..These findings unveil a novel aspect within the GR-mediated NF-kappaB-targeting anti-inflammatory mechanism...
- Evaluation of methods for generating parametric (R-[11C]PK11195 binding imagesAlie Schuitemaker
Department of Nuclear Medicine and PET Research, VU University Medical Centre, Amsterdam, The Netherlands
J Cereb Blood Flow Metab 27:1603-15. 2007..In pathological conditions with reduced flow rates or large variations in blood volume, the basis function method is preferred because it produces less bias and is more precise...
- Involvement of benzodiazepine receptors in neuroinflammatory and neurodegenerative diseases: evidence from activated microglial cells in vitroH Wilms
Klinik fur Neurologie, Christian Albrechts Universitat zu Kiel, Niemannsweg 147, 24105 Kiel, Germany
Neurobiol Dis 14:417-24. 2003..These findings link the in vivo data of elevated PBR levels in neurodegenerative/-inflammatory diseases to a functional role and opens up possible therapeutic intervention targeting the PBR in microglia...
- Sanguinarine-dependent induction of apoptosis in primary effusion lymphoma cellsAzhar R Hussain
Human Cancer Genomic Research, King Fahad National Center for Children s Cancer and Research, Biological and Medical Research, Riyadh 11211, Saudi Arabia
Cancer Res 67:3888-97. 2007....
- Novel reference region model reveals increased microglial and reduced vascular binding of 11C-(R)-PK11195 in patients with Alzheimer's diseaseGiampaolo Tomasi
Department of Information Engineering, University of Padova, Padova, Italy
J Nucl Med 49:1249-56. 2008....
- Visualising microglial activation in vivoRichard B Banati
Department of Neuropathology, Charing Cross Hospital, Imperial College School of Medicine, and MRC Clinical Sciences Centre PET Neurology, Hammersmith Hospital, London, United Kingdom
Glia 40:206-17. 2002....
- Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the ratChristine Dugovic
Neuroscience, Johnson and Johnson PRD, 3210 Merryfield Row, San Diego, CA 92121, USA
J Pharmacol Exp Ther 330:142-51. 2009..In addition, it is suggested that simultaneous inhibition of OX1R attenuates the sleep-promoting effects mediated by selective OX2R blockade, possibly correlated with dopaminergic neurotransmission...
- [11C]-DPA-713 and [18F]-DPA-714 as new PET tracers for TSPO: a comparison with [11C]-(R)-PK11195 in a rat model of herpes encephalitisJanine Doorduin
Department of Nuclear Medicine and Molecular Imaging, University Medical Center Groningen, University of Groningen, 9700 RB Groningen, The Netherlands
Mol Imaging Biol 11:386-98. 2009..In this study, we evaluated the PET tracers [(11)C]-DPA-713 and [(18)F]-DPA-714 as agents for imaging of activated microglia in a rat model of herpes encephalitis...
- The indenoisoquinoline noncamptothecin topoisomerase I inhibitors: update and perspectivesYves Pommier
Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, Maryland 20892, USA
Mol Cancer Ther 8:1008-14. 2009..We discuss the use of γ-H2AX as a pharmacodynamic biomarker for the clinical development of the indenoisoquinolines...
- Synthesis of substituted isoquinolines utilizing palladium-catalyzed α-arylation of ketonesTimothy J Donohoe
Department of Chemistry, University of Oxford, Chemistry Research Laboratory, Mansfield Road, Oxford OX1 3TA, United Kingdom
Proc Natl Acad Sci U S A 109:11605-8. 2012..palladium-catalyzed α-arylation and cyclization reactions provides a general approach to an array of isoquinolines and their corresponding N-oxides...
- Differential induction of topoisomerase I-DNA cleavage complexes by the indenoisoquinoline MJ-III-65 (NSC 706744) and camptothecin: base sequence analysis and activity against camptothecin-resistant topoisomerases ISmitha Antony
Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute NIH, 37 Convent Drive, Bethesda, MD 20892 4255, USA
Cancer Res 63:7428-35. 2003..This study shows the specific molecular interactions of MJ-III-65 with top1 and demonstrates that MJ-III-65 is a potentially useful top1 inhibitor that enhances and traps top1 cleavage sites not sensitive to CPTs...
- Isoquinoline synthesis via rhodium-catalyzed oxidative cross-coupling/cyclization of aryl aldimines and alkynesNicolas Guimond
Centre for Catalysis Research and Innovation, Department of Chemistry, University of Ottawa, 10 Marie Curie, Ottawa, Canada K1N 6N5
J Am Chem Soc 131:12050-1. 2009..This process affords 3,4-disubstituted isoquinolines in good yield and high regioselectivity...
- Agonists and antagonists induce different palonosetron dissociation rates in 5-HT₃A and 5-HT₃AB receptorsSarah C R Lummis
Department of Biochemistry, University of Cambridge, Tennis Court Road, Cambridge CB2 1QW, UK
Neuropharmacology 73:241-6. 2013....
- On the binding of indeno[1,2-c]isoquinolines in the DNA-topoisomerase I cleavage complexXiangshu Xiao
Department of Medicinal Chemistry and Molecular Pharmacology and the Purdue Cancer Center, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, Indiana 47907, USA
J Med Chem 48:3231-8. 2005....
- Optimization of supervised cluster analysis for extracting reference tissue input curves in (R)-[(11)C]PK11195 brain PET studiesMaqsood Yaqub
Department of Nuclear Medicine and PET Research, VU University Medical Center, Amsterdam, The Netherlands
J Cereb Blood Flow Metab 32:1600-8. 2012..Incorporation of V(b) within RPM, together with SVCA4, appears to be the method of choice for analyzing cerebral (R)-[(11)C]PK11195 neurodegeneration studies...
- Salsolinol, a tetrahydroisoquinoline-derived neurotoxin, induces oxidative modification of neurofilament-L protection by histidyl dipeptidesJung Hoon Kang
Department of Genetic Engineering, Cheongju University, Cheongju 360 764, Korea
BMB Rep 45:114-9. 2012..Both compounds also inhibited the generation of •OH induced by salsolinol. The results indicated that carnosine and related compounds may prevent salsolinol-mediated NF-L modification via free radical scavenging...
- Orexins depolarize rostral ventrolateral medulla neurons and increase arterial pressure and heart rate in rats mainly via orexin 2 receptorsShang Cheng Huang
Graduate Institute of Medical Sciences, College of Medicine, Taipei Medical University, Taipei, Taiwan
J Pharmacol Exp Ther 334:522-9. 2010..We concluded that orexins directly excite RVLM neurons, which include bulbospinal vasomotor neurons, and regulate cardiovascular function mainly via the OX(2)R, with a smaller contribution from the OX(1)R...
- Efficacy of palonosetron (PAL) compared to other serotonin inhibitors (5-HT3R) in preventing chemotherapy-induced nausea and vomiting (CINV) in patients receiving moderately or highly emetogenic (MoHE) treatment: systematic review and meta-analysisTobias Engel Ayer Botrel
Rua Tranquillo Prosperi, 143, Campinas, Sao Paulo, 13084 778, Brazil
Support Care Cancer 19:823-32. 2011..25 mg with other 5-HT(3)R in patients receiving moderately or highly emetogenic (MoHE) chemotherapy...
- The binding orientation of a norindenoisoquinoline in the topoisomerase I-DNA cleavage complex is primarily governed by pi-pi stacking interactionsYunlong Song
Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue Cancer Center, Purdue University, West Lafayette, IN 47907, USA
J Phys Chem B 112:9484-9. 2008....
- The antiemetic 5-HT3 receptor antagonist Palonosetron inhibits substance P-mediated responses in vitro and in vivoCamilo Rojas
the Brain Science Institute, Johns Hopkins University School of Medicine, 855 N Wolfe Street, Suite 270, Baltimore, MD 21205, USA
J Pharmacol Exp Ther 335:362-8. 2010....
- TSPO over-expression increases motility, transmigration and proliferation properties of C6 rat glioma cellsMariarosa Rechichi
Dipartimento di Morfologia Umana e Biologia Applicata, University of Pisa, Via Volta 4, Pisa, Italy
Biochim Biophys Acta 1782:118-25. 2008..These findings suggest that the use of TSPO ligands as chemotherapeutic agents could be effective on aggressive tumor cells with a high TSPO expression level...
- The potential anticancer agent PK11195 induces apoptosis irrespective of p53 and ATM status in chronic lymphocytic leukemia cellsAntonio F Santidrian
Departament de Ciències Fisiològiques II, IDIBELL Universitat de Barcelona, L Hospitalet de Llobregat, Spain
Haematologica 92:1631-8. 2007..Primary chronic lymphocytic leukemia (CLL) cells overexpress TSPO. The aim of this study was to examine the effects of PK11195 on CLL cells. Table 1. Characteristics of the patients with chronic lymphocytic leukemia...
- Inhibition of poly adenosine diphosphate-ribose polymerase decreases hepatocellular carcinoma growth by modulation of tumor-related gene expressionRosa Quiles-Perez
San Cecilio University Hospital, Granada, Spain
Hepatology 51:255-66. 2010..05)...
- SPM analysis of parametric (R)-[11C]PK11195 binding images: plasma input versus reference tissue parametric methodsAlie Schuitemaker
Department of Nuclear Medicine and PET Research, VU University Medical Centre, P O Box 7057, 1081 MB Amsterdam, The Netherlands
Neuroimage 35:1473-9. 2007..Vd images could only demonstrate differences in (R)-[11C]PK11195 binding when analysed with proportional scaling due to intersubject variation in K1/k2 (blood-brain barrier transport and non-specific binding)...
- Widespread and prolonged increase in (R)-(11)C-PK11195 binding after traumatic brain injuryHedy Folkersma
Neurosurgical Center Amsterdam, VU University Medical Center, Amsterdam, The Netherlands
J Nucl Med 52:1235-9. 2011..Our objective was to measure (R)-(11)C-PK11195 binding as an indirect marker of neuronal damage after traumatic brain injury (TBI)...
- Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERBDouglas Kojetin
ACS Chem Biol 6:131-4. 2011..Thus, SR8278 represents a unique chemical tool for probing REV-ERB function and may serve as a point for initiation of further optimization to develop REV-ERB antagonists with the ability to explore circadian and metabolic functions...
- Design, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domainMuriel Billamboz
Laboratoire de Chimie Organique et Macromoléculaire, UMR CNRS 8009, Universite de Lille 1, 59655 Villeneuve d Ascq, France
J Med Chem 51:7717-30. 2008..Unfortunately, all tested compounds exhibited high cellular cytotoxicity in cell culture which limits their applications as antiviral agents...
- Salsolinol produces reinforcing effects in the nucleus accumbens shell of alcohol-preferring (P) ratsZachary A Rodd
Indiana University School of Medicine, Institute of Psychiatric Research, 791 Union Drive, Indianapolis, IN 46202 4887, USA
Alcohol Clin Exp Res 27:440-9. 2003....
- ET-743: the US experience in sarcomas of soft tissuesGeorge D Demetri
Center for Sarcoma and Bone Oncology, Dana Farber Cancer Institute, Harvard Medical School, Boston, Massachusetts, USA
Anticancer Drugs 13:S7-9. 2002..There were no treatment-associated deaths. In conclusion, ET-743 is an active chemotherapeutic agent that can induce objective responses and clinical benefit in a subset of patients with metastatic or advanced soft-tissue sarcoma...
- Antisense RNA-mediated suppression of benzophenanthridine alkaloid biosynthesis in transgenic cell cultures of California poppySang Un Park
Department of Biological Sciences, University of Calgary, Calgary, Alberta, Canada T2N 1N4
Plant Physiol 128:696-706. 2002..These data provide new insight into the metabolic engineering of benzophenanthridine alkaloid pathways...
- Phosphorylation of glycogen synthase kinase-3 and stimulation of T-cell factor signaling following activation of EP2 and EP4 prostanoid receptors by prostaglandin E2Hiromichi Fujino
Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, Tucson, Arizona 85721 0207, USA
J Biol Chem 277:2614-9. 2002..This is the first indication of a fundamental difference in the signaling potential of EP(2) and EP(4) prostanoid receptors...
- Novel phosphorylation of aquaporin-5 at its threonine 259 through cAMP signaling in salivary gland cellsTakahiro Hasegawa
Dept of Molecular Oral Physiology, Institute of Health Biosciences, The Univ of Tokushima Graduate School, Japan
Am J Physiol Cell Physiol 301:C667-78. 2011..These results suggest that AQP5 is phosphorylated at its Thr259 by PKA through cAMP, but not Ca(2+), signaling pathways, and that this phosphorylation does not contribute to AQP5 trafficking in the salivary gland cells...
- Long-term trans-synaptic glial responses in the human thalamus after peripheral nerve injuryR B Banati
Peripheral Neuropathy Unit, MRC Clinical Sciences Centre, Imperial College Faculty of Medicine, Hammersmith Hospital, London, UK
Neuroreport 12:3439-42. 2001..Our findings support the view that long-term rearrangement of cortical representational maps is significantly determined within the thalamus...
- Sanguinarine (pseudochelerythrine) is a potent inhibitor of NF-kappaB activation, IkappaBalpha phosphorylation, and degradationM M Chaturvedi
Cytokine Research Section, Department of Molecular Oncology, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
J Biol Chem 272:30129-34. 1997..Overall, our results demonstrate that sanguinarine is a potent suppressor of NF-kappaB activation and it acts at a step prior to IkappaBalpha phosphorylation...
- Differential effects of the dual orexin receptor antagonist almorexant and the GABA(A)-α1 receptor modulator zolpidem, alone or combined with ethanol, on motor performance in the ratMichel A Steiner
CNS Pharmacology, Actelion Pharmaceuticals Ltd, Allschwil, Switzerland
Neuropsychopharmacology 36:848-56. 2011....
- Induction of conditioned place preference and dopamine release by salsolinol in posterior VTA of rats: involvement of μ-opioid receptorsLucía Hipólito
Departament de Farmàcia i Tecnologia Farmacèutica, Universitat de Valencia, Avda Vicente Andres Estelles s n, 46100 Burjassot, Spain
Neurochem Int 59:559-62. 2011..The local pretreatment with β-FNA, an antagonist of MORs, prevented this increase, supporting our hypothesis on the involvement of MORs in the Sal-derived effects...
- Cyclooxygenase 2 rescues LNCaP prostate cancer cells from sanguinarine-induced apoptosis by a mechanism involving inhibition of nitric oxide synthase activityJacob Huh
Department of Medicine and Free Radical Research Center, Medical College of Wisconsin, 8701 Watertown Plank Road, Milwaukee, WI 53266, USA
Cancer Res 66:3726-36. 2006....
- Orexin receptor antagonism, a new sleep-promoting paradigm: an ascending single-dose study with almorexantP Hoever
Department of Clinical Pharmacology, Actelion Pharmaceuticals Ltd, Allschwil, Switzerland
Clin Pharmacol Ther 87:593-600. 2010..Population pharmacokinetic/pharmacodynamic modeling suggested that doses of ~500 mg almorexant and 10 mg zolpidem are equivalent with respect to subjectively assessed alertness...
- Positron emission tomography imaging of neuroinflammationAnnachiara Cagnin
Department of Neuroscience, University of Padova, Via Giustiniani 5, 35128, Padova, Italy
Neurotherapeutics 4:443-52. 2007....
- Anti-emetic effect of ondansetron and palonosetron in thyroidectomy: a prospective, randomized, double-blind studyY E Moon
Department of Anaesthesiology and Pain Medicine, Seoul St Mary s Hospital, Catholic University College of Medicine, Seoul, Republic of Korea
Br J Anaesth 108:417-22. 2012..This study compared the effects of i.v. ondansetron and palonosetron administered at the end of surgery in preventing postoperative nausea and vomiting (PONV) in high-risk patients receiving i.v. PCA after thyroidectomy...
- Palonosetron: a second-generation 5-hydroxytryptamine receptor antagonistRudolph M Navari
Indiana University School of Medicine, Notre Dame Cancer Institute, South Bend, IN 46617, USA
Future Oncol 2:591-602. 2006..Future studies may consider the use of palonosetron with current and other new agents and in other clinical settings, such as bone marrow transplantation and radiation therapy...
- Neuropathological imaging: in vivo detection of glial activation as a measure of disease and adaptive change in the brainRichard B Banati
Molecular Neuropsychiatry, Department of Neuropathology, Charing Cross Hospital, Imperial College School of Medicine, London, UK
Br Med Bull 65:121-31. 2003..Systematic attempts are now undertaken, using positron emission tomography and a ligand with relative selectivity for activated microglia, to develop generic imaging tools for a cellular in vivo neuropathology...
- Sanguinarine causes cell cycle blockade and apoptosis of human prostate carcinoma cells via modulation of cyclin kinase inhibitor-cyclin-cyclin-dependent kinase machineryVaqar Mustafa Adhami
Department of Dermatology, University of Wisconsin Medical Science Center, 1300 University Avenue, Madison, WI 53706, USA
Mol Cancer Ther 3:933-40. 2004..These results suggest that sanguinarine may be developed as an agent for the management of prostate cancer...
- PET imaging with [11C]PBR28 can localize and quantify upregulated peripheral benzodiazepine receptors associated with cerebral ischemia in ratMasao Imaizumi
Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 1, Room B3 10, 1 Center Drive, MSC 0135, Bethesda, MD 20892 0135, USA
Neurosci Lett 411:200-5. 2007..In this first study to demonstrate neuroinflammation in vivo with small animal PET, [11C]PBR28 had adequate sensitivity to localize and quantify the associated increase in PBRs...
- Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918M Maliepaard
Division of Experimental Therapy, The Netherlands Cancer Institute, 1066 CX Amsterdam, The Netherlands
Clin Cancer Res 7:935-41. 2001..This observation may have important clinical implications for future development of novel camptothecins...
- Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonistsPari Malherbe
F Hoffmann La Roche Ltd, Bldg 69 333, CH 4070 Basel, Switzerland
Mol Pharmacol 76:618-31. 2009..The electrophysiology data suggest that OX(2) might be more important than OX(1) in mediating the effect of orexin-A on slow-firing of VTA dopaminergic neurons...
- Positron emission tomography imaging of peripheral benzodiazepine receptor binding in human immunodeficiency virus-infected subjects with and without cognitive impairmentClayton A Wiley
Department of Pathology, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania, USA
J Neurovirol 12:262-71. 2006....
- An active protein kinase A (PKA) is involved in meiotic arrest of rat growing oocytesMichal Kovo
Department of Biological Regulation, The Weizmann Institute of Science, Rehovot, 76100 Israel
Reproduction 132:33-43. 2006....
- MSK activation and physiological rolesJ Simon C Arthur
MRC Protein Phosphorylation Unit, College of Life Sciences, University of Dundee, Dundee, DD1 5EH, UK
Front Biosci 13:5866-79. 2008..The physiological roles of MSKs still remain to be completely determined, however recent work has suggested a role for MSKs in neuronal synaptic plasticity and in regulating cytokine production in the innate immune system...
- Topoisomerase I levels in the NCI-60 cancer cell line panel determined by validated ELISA and microarray analysis and correlation with indenoisoquinoline sensitivityThomas D Pfister
Laboratory of Human Toxicology and Pharmacology, Applied Developmental Research Support Directorate, Science Applications International Corporation Frederick Inc, National Cancer Institute Frederick, Frederick, MD 21702, USA
Mol Cancer Ther 8:1878-84. 2009....
- The Ca2+/calmodulin-dependent protein kinase kinases are AMP-activated protein kinase kinasesRebecca L Hurley
Departments of Medicine and Biochemistry, Dartmouth Medical School and the Department of Biological Sciences, Dartmouth College, Hanover, NH 03755, USA
J Biol Chem 280:29060-6. 2005..These data indicate that the CaMKKs function in intact cells as AMPKKs, predicting wider roles for these kinases in regulating AMPK activity in vivo...
- Synergy of Pancratistatin and Tamoxifen on breast cancer cells in inducing apoptosis by targeting mitochondriaPeter Siedlakowski
Department of Chemistry and Biochemistry, University of Windsor, Windsor, Ontario, Canada
Cancer Biol Ther 7:376-84. 2008....
- Comparison of [(11)C]-(R)-PK 11195 and [(11)C]PBR28, two radioligands for translocator protein (18 kDa) in human and monkey: Implications for positron emission tomographic imaging of this inflammation biomarkerWilliam C Kreisl
Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD, USA
Neuroimage 49:2924-32. 2010..This study asked two questions: (1) What is the cause of non-binding to PBR28? and (2) Why has this phenomenon not been reported using [(11)C]-(R)-PK 11195?..
- PalonosetronM Asif A Siddiqui
Adis International Limited, Mairangi Bay, Auckland, New Zealand
Drugs 64:1125-32; discussion 1133-4. 2004..Intravenous palonosetron was generally well tolerated in clinical trials, with few adverse events being treatment related. Palonosetron had no significant effect on the corrected QT interval or laboratory parameters...
- Morphinans and isoquinolines: acetylcholinesterase inhibition, pharmacophore modeling, and interaction with opioid receptorsDaniela Schuster
Department of Pharmaceutical Chemistry, Institute of Pharmacy, University of Innsbruck and Center for Molecular Biosciences Innsbruck CMBI, Innrain 52a c, A 6020 Innsbruck, Austria
Bioorg Med Chem 18:5071-80. 2010..The most active compounds were biochemically tested for their activity on mu, delta, and kappa opioid receptors...
- Mitogen- and stress-activated kinase 1-mediated histone H3 phosphorylation is crucial for cell transformationHong Gyum Kim
The Hormel Institute, University of Minnesota, Austin, MN 55912, USA
Cancer Res 68:2538-47. 2008..Thus, MSK1 is required for tumor promoter-induced cell transformation through its phosphorylation of histone H3 at Ser(10) and AP-1 activation...
- Total synthesis of the N,C-coupled naphthylisoquinoline alkaloids ancistrocladinium A and B and related analoguesGerhard Bringmann
Institute of Organic Chemistry, University of Wurzburg, Am Hubland, D 97074 Wurzburg, Germany
J Am Chem Soc 132:1151-8. 2010..Its general applicability was shown by the preparation of the sterically even more congested, as yet unnatural N,3'- and N,1'-coupled analogues, ancistrocladinium C (5) and D (6)...
- Syntheses and antitumor targeting G1 phase of the cell cycle of benzoyldihydroisoquinolines and related 1-substituted isoquinolinesAlmudena Bermejo
Departamento de Farmacologia, Laboratorio de Farmacognosia, Universidad de Valencia, 46100 Burjassot, Spain
J Med Chem 45:5058-68. 2002..iii) Regarding the influence of the benzoylic moiety, both the unsubstituted (13, 8, 9, 11, 1, and 6) and the 3'-monosubstituted (22, 21, 20, and 19) compounds were more potent than compounds with other substitutions...
- Two activated stages of microglia and PET imaging of peripheral benzodiazepine receptors with [(11)C]PK11195 in ratsFumitaka Ito
Department of Radiology, Fujita Health University, Kutsukake, Toyoake, Aichi, Japan
Ann Nucl Med 24:163-9. 2010..We evaluated whether [(11)C]PK11195 PET can indicate differences of microglial activation between no treatment and lipopolysaccharide (LPS) treatment in a rat artificial injury model of brain inflammation...
- Synthesis of Medicinally Important HeterocyclesRICHARD LAROCK; Fiscal Year: 2007..affords very high yields of a wide variety of halogen-, sulfur- and selenium-substituted benzothiophenes, isoquinolines, benzofurans, and isocoumarins under exceptionally mild reaction conditions...
- Pilot-Scale Heterocyclic and Carbocyclic Libraries for High Throughout ScreeningRICHARD LAROCK; Fiscal Year: 2009..coumarins, isocoumarins, phthalides, pyrones, 2-quinolones, pyridines, isoquinolin-1-ones, isoindolin-1-ones, isoquinolines, carbolines, isoindolo[2,1-a]indoles, carbazoles, dibenzofurans and various other heterocycles, plus indenones,..
- BENZODIAZEPINE DERIVED CARBORANES FOR N CAPTURE THERAPYJOHN NEUMEYER; Fiscal Year: 1992..The initial objective of the Phase I effort will be the synthesis of several boron-containing isoquinolines structurally related to PK 11195 and their evaluation against malignant glioma cells, U251 human glioblastoma...
- MITOCHONDRIA, PESTICIDES, ISOQUINOLINES AND PARKINSON'SHoward Strahlendorf; Fiscal Year: 2001..or by increasing the vulnerability of these neurons to selective detrimental effects of naturally occurring isoquinolines (IsoQ), specifically 1,2,3,4, tetrahydroisoquinoline (TIQ) and salsolinol (SAL)...
- Topoisomerase I-directed Anticancer DrugsLeroy Liu; Fiscal Year: 2004..g. indolocarbazoles, nitidines, saintopin, morpholinyl doxorubicin, aclacinomycin A, indeno[1,2-c]isoquinolines, nogalamycin, actinomycin D, protoberberines, dibenzo[c,h]cinnolines, 2-phenylbenzimidazoles and ..
- ANTHRACYCLINES FROM ISOQUINOLINESRICHARD FRANCK; Fiscal Year: 1992..The biological activity of the C-glycosides will provide important information about the requirements for cytotoxicity and cardiotoxicity of the parent compounds...
- Enabling Technologies for Combinatorial ChemistryK Nicolaou; Fiscal Year: 2005..abstract_text> ..
- Morphine/NMDA interactions: Antinociceptive and discriminative stimulus effectsBRADFORD FISCHER; Fiscal Year: 2007..Findings from these experiments may have important clinical implications, and may lead to new pharmacotherapeutic strategies in the treatment of pain and drug abuse. [unreadable] [unreadable] [unreadable]..
- Imaging of Serotonin Transporters in DepressionRAMIN PARSEY; Fiscal Year: 2005..These goals will be met by a combination of didactic I course work and supervision. ..
- TOTAL SYNTHESIS OF AZADIRACHTINK Nicolaou; Fiscal Year: 2008..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
- Biological Predictors of Response to AntidepressantsRamin V Parsey; Fiscal Year: 2010..Our overall goal is to reduce the trial and error associated with finding an effective antidepressant by using data from pre-treatment quantification of 5-HT1A receptors and 5-HTT to guide antidepressant treatment selection. ..
- Escalating Cocaine Self-Administration: NMDA MechanismsRichard Allen; Fiscal Year: 2003..abstract_text> ..
- Molecular Target Focused Discovery of Anticancer DrugsGeorge R Pettit; Fiscal Year: 2010....
- SYNTHESIS OF ANTICANCER AGENTSK C Nicolaou; Fiscal Year: 2010..abstract_text> ..
- TOTAL SYNTHESIS OF NATURAL PRODUCTSK Nicolaou; Fiscal Year: 2002..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
- DESIGN OF INHIBITORS OF EPINEPHRINE BIOSYNTHESISGARY GRUNEWALD; Fiscal Year: 2005..These inhibitors will be the first pharmacological tools available to help determine the function(s) of Epi in the CNS. This project is ripe and ready to burst forth with important new results. ..
- Molecular Target Focused Discovery of Anticancer DrugsGEORGE PETTIT; Fiscal Year: 2007..In summary, the proposed research will be sharply aimed at the discovery and very rapid development of new anticancer drugs for the NCI programs direct at improving human cancer treatments. ..
- TOTAL SYNTHESIS OF APOPTOLIDINK Nicolaou; Fiscal Year: 2004..The proposed work is expected to have significant impact in the area of cancer chemotherapy and should provide enabling technologies and tools for biology and medicine. ..
- New Methodology for Indole Alkaloid SynthesesKen S Feldman; Fiscal Year: 2010..The use of a new variant of the Pummerer reaction to control both oxidation level and reaction site within the indole nucleus forms the basis of this chemistry. ..
- Alkynyliodonium Salts and Derived Diyls in SynthesisKen Feldman; Fiscal Year: 2009..abstract_text> ..
- COCAINE: A STUDY OF THE BIOCHEMICAL MECHANISM OF ACTIONFrank Carroll; Fiscal Year: 2007..abstract_text> ..
- Screen for Mycobacterium Tuberculosis (RMI)E White; Fiscal Year: 2005..tuberculosis. 3) To study the effect of these novel inhibitors on the pantothenate pathway in M. smegmatis. 4) To co-crystallize these compounds with pantothenate synthetase to study their mode of binding ..
- PET Imaging MDMA NeurotoxicityUna McCann; Fiscal Year: 2006..g., dementia, Parkinsonism, depression/anxiety). In addition, the proposed 18FDG studies will address the question of if MDMA exposure leads to altered brain function at the most fundamental level, glucose utilization. ..
- METHODOLOGY FOR THE SYNTHESIS OF NITROGEN HETEROCYCLESPhilip Magnus; Fiscal Year: 2007..The synthetic intermediates, particularly as they more closely resemble the natural products, will be screened to assess biological activity. [unreadable] [unreadable]..
- NOVEL PHARMACOTHERAPY FOR TREATMENT OF COCAINE ADDICTIONFrank Carroll; Fiscal Year: 2008..abstract_text> ..
- Design and Development of Pharmacotherapies for Treating Stimulant AbuseFrank Ivy Carroll; Fiscal Year: 2010..3) To continue on a limited basis our development of selected 3-phenyltropane analogs as second-generation pharmacotherapies to treat cocaine addiction. ..
- Northeast Under/Grad Research Organization for NeuroscienceCheryl Frye; Fiscal Year: 2008..Both of these outcomes are congruous with the Public Health Service's mission to ensure that there is a resource of well-trained scientists and health-care providers in the United States. [unreadable] [unreadable] [unreadable]..
- SYNTHESIS OF ANTIBIOTICSAndrew G Myers; Fiscal Year: 2010..In addition, we will undertake basic studies to explore the feasibility of a novel macropolycyclization route to produce the new class of antibiotics known as the pyrrocidines. ..
- Chemical and Biological Studies on Biaryl PhenolicsKen Feldman; Fiscal Year: 2005..The search for selective 20S proteosome inhibitors among the Ntn-type proteases will be advanced by these investigations. ..
- NOVEL PHARMACOTHERAPIES FOR COCAINE DEPENDENCEFrank Carroll; Fiscal Year: 2001..An ideal candidate compound would not only have efficacy in the preclinical models but would be safe, orally active, and potent, would not show tolerance or sensitization, and if abusable, would be less so than cocaine. ..
- SYNTHESIS OF DIAZONAMIDESPhilip Magnus; Fiscal Year: 2004..Part of the synthetic studies will involve the generation of persistent radical intermediates that should add to pi-deficient heterocycles and form the key central hindered bond present in the diazonamides. ..
- Novel antioxidant catalyst for transplant rejectionPrakash Jagtap; Fiscal Year: 2003..Phase II funding would support pharamcokinetic, toxicology, and pharmacodynamic studies required for IND submission and FDA-sanctioned clinical Phase I trials. ..
- Novel PARS inhibitor for therapy of colitisPrakash Jagtap; Fiscal Year: 2002..These studies will provide the foundation for clinical testing, commercial development, and first market entry of an ultrapotent PARS inhibitor for therapy of IBD. PROPOSED COMMERCIAL APPLICATION: NOT AVAILABLE ..
- PARS inhibitor for cardiac allotransplantationPrakash Jagtap; Fiscal Year: 2002..Global markets are estimated at $400 million. Current market entrants such as cyclosporine A and FK506, have substantial toxicity. Funding of SBIR Phases I and II would allow for market entry in 4 years. ..
- Gene expression associated with the CNS reinforcing act*ZACHARY RODD HENRICKS; Fiscal Year: 2003..The results of the proposed project will provide valuable information on neuronal systems and receptors within the extended amygdala involved in mediating the rewarding properties of alcohol. ..
- Sleep and Nocturnal Endocrine Function in MDMA UserUna McCann; Fiscal Year: 2007..Results from the proposed studies will help better define the functional consequences of MDMA exposure in humans, and could shed light on the roles of 5-HT and DA in sleep and nocturnal endocrine function. ..
- A Method To Study Membrane Protein StructureGuido Zampighi; Fiscal Year: 2003....
- TRPV1 Expressing Sensory Afferents in Postoperative PainTimothy Brennan; Fiscal Year: 2009..A separate pathway, likely an A-fiber mediated pathway, is sufficient to transmit the enhanced mechanical responses. ..
- GAP JUNCTIONAL COMMUNICATIONS IN WOUND HEALINGH Ehrlich; Fiscal Year: 2009..abstract_text> ..
- NITROGEN HETEROCYCLES: METABOLIC EFFECTS AND TOXICITYRaymond F Novak; Fiscal Year: 2010....
- Inflammation in obesity: Modulation by Weight LossParesh Dandona; Fiscal Year: 2009..abstract_text> ..
- VASOMOTOR CONTROL OF DESCENDING VASA RECTATHOMAS PALLONE; Fiscal Year: 2003....
- ROLE OF IMMUNE RESPONSIVENESS AND HIV ENCEPHALOPATHYClayton Wiley; Fiscal Year: 2001..These data will help design means of identifying subjects at risk for the development of CNS disease and help design therapies for arresting HIV encephalitis. ..
- MDMA Neurotoxicity in Nonhuman PrimatesGeorge Ricaurte; Fiscal Year: 2005..abstract_text> ..
- TEMPLATE POLYMERIZATIONKENNETH SHEA; Fiscal Year: 2002..This latter application will utilize a fluorescent signal to report the binding event. Finally we have proposed a study designed to get at how binding sites are created during the polymerization process. ..
- Mechanisms of HIV-Induced PNS Disease: The SIV Macaque ModelJoseph Mankowski; Fiscal Year: 2009..The goal of these comprehensive, integrated studies of HIV sensory neuropathy in our novel SIV primate model is to advance the understanding of HIV-SN pathogenesis to foster new therapeutic approaches. ..
- Agilent 5973 GC/MS SystemGARY MOLANDER; Fiscal Year: 2002..Our current lack of such instrumentation negatively affects the ability to carry out many of these studies. This critical capability, in the form of an instrument for everyday analysis, is urgently needed. ..
- Motor Systems Supporting Pavlovian ConditioningTerry Crow; Fiscal Year: 2008..These studies will help to elucidate general principles underlying the organization of polysensory neural systems generating behavior and their modification by learning. ..
- MOLECULAR MECHANISMS OF SCHWANN CELL MYELINATIONBruce Trapp; Fiscal Year: 2008....
- Xenobiotics and Breast Epithelial Cell-ECM SignalingRaymond Novak; Fiscal Year: 2005..The results of this proposal will provide novel information regarding chemical-mediated effects in breast epithelial cells and seminal data on fundamental cellular changes in human proliferative breast disease. ..
- REGULATION OF THE STEROIDOGENIC ACUTE REGULATORY PROTEINBarbara Clark; Fiscal Year: 2005..This will ultimately lead to a better understanding of potential developmental or disease states that result from aberrant over- or under-expression of StAR in a cell-specific manner. ..
- Partner of Under-Represented Scientists United for EducLINDA DYKSTRA; Fiscal Year: 2005..The Graduate School and individual doctoral granting departments at UNC-Chapel Hill will provide matching funds to promote the success of the program. ..
- Botanicals from Central America for MenopauseGail Mahady; Fiscal Year: 2005..Successful validation and standardization of traditional plant-based medicines used to treat menopause has great significance not only for the women of Central America but the rest of the world as well. ..
- 2004 TERATOLOGY SOCIETY MEETINGS: TRAVEL FOR STUDENTSThomas Knudsen; Fiscal Year: 2004..Funds to help support and encourage student-fellow attendance at the Teratology Society 2004 meeting will enhance the quality of the meeting and the experience of the student attendees. ..
- Overcoming Barriers to Early Phase Clinical TrialsBruce Chabner; Fiscal Year: 2004....
- Red Blood Cell Adhesion in Sickle Cell DiseaseCHERYL HILLERY; Fiscal Year: 2005..Thus, we expect that information derived from this proposal will lead to new therapeutic approaches for the treatment of vaso-occlusion in SS-D. ..
- ALVEOLAR TYPE II CELL GROWTH IN INJURYRANDOLPH HASTINGS; Fiscal Year: 2003..The project will evaluate the potential use of PTHrP-related therapeutic interventions that might speed or improve recovery following silica-induced lung injury. ..
- Reactive Oxygen Species American Society of Nephrology Fall 2007THOMAS PALLONE; Fiscal Year: 2007..Attendance of young scientists insures that the information will be translated into future studies that elucidate the role of ROS in kidney diseases and treatment thereof. [unreadable] [unreadable] [unreadable]..
- 2003 TERATOLOGY SOCIETY MEETINGS: TRAVEL FOR STUDENTSThomas Knudsen; Fiscal Year: 2003..Funds to help support and encourage student-fellow attendance at the Teratology Society 2003 meeting will enhance the quality of the meeting and the experience of the student attendees. ..
- Stem Cell-Seeded ECM Scaffolds for NeurotransplantationMICHELLE LAPLACA; Fiscal Year: 2004..abstract_text> ..
- RETINOID REGULATION OF BLOOD VESSEL FORMATIONKaren Hirschi; Fiscal Year: 2004..We will also specifically investigate the role(s) of retinoic acid and TGF-Â¿ signaling in the control of endothelial cell maturation and growth, as a direct extension of our previous work. ..
- Cyclic AMP signaling in cardiac myocytesTHOMAS RICH; Fiscal Year: 2007..g., protenoid, beta1-,or beta2-adrenergic receptors) or inhibit phosphodiesterase (PDE) will shed new light on the physiologic functions of these enzymes and their relation to cardiac function. ..
- Antipsychotic Actions in Models of NMDA HypofunctionGary Duncan; Fiscal Year: 2007..unreadable] [unreadable]..
- Development of cAMP Biosensor, High Content Imaging, and Functional GLP-1R aSSAYSPhilip LoGrasso; Fiscal Year: 2010....
- TRANSPORT BY OCULAR EPITHELIAL CELLSMORTIMER CIVAN; Fiscal Year: 2005..abstract_text> ..