Research Topics
| J DunlopSummaryAffiliation: Wyeth Research Country: USA Publications
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Detail Information
Publications
Pituitary adenylate cyclase-activating peptide (PACAP) induces differentiation in the neuronal F11 cell line through a PKA-dependent pathwayH Beal McIlvain
Discovery Neuroscience, Wyeth Research, CN 8000 Princeton, NJ 08543, USA
Brain Res 1077:16-23. 2006..PACAP is upregulated in DRG neurons as a result of injury, and F11 cells provide an easily accessible in vitro model for understanding mechanisms underlying PACAP differentiation and neurogenesis...- Validation of DRG-like F11 cells for evaluation of KCNQ/M-channel modulatorsFlora Jow
Discovery Neuroscience, Wyeth Research, Princeton, NJ 08543, USA
Assay Drug Dev Technol 4:49-56. 2006..These findings have led us to conclude that F11 cells can be used as a DRG cell model to evaluate effects of KCNQ/M-channel modulators... - Ligands targeting the excitatory amino acid transporters (EAATs)John Dunlop
Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton NJ 08543, USA
Curr Top Med Chem 6:1897-906. 2006.... - Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels and painJ Dunlop
Neuroscience Discovery, Wyeth Research, Princeton, NJ 08543, USA
Curr Pharm Des 15:1767-72. 2009..This review discusses the evidence implicating a role for HCN channels in pain... - WAY-163909 [(7bR, 10aR)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole], a novel 5-hydroxytryptamine 2C receptor-selective agonist with anorectic activityJohn Dunlop
Discovery Neuroscience, Wyeth Research, Princeton, NJ 08543, USA
J Pharmacol Exp Ther 313:862-9. 2005..4 and 5.19 mg/kg i.p., respectively, consistent with the potential utility of 5-HT(2C) receptor agonists as anti-obesity agents... - Characterization of novel aryl-ether, biaryl, and fluorene aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT2John Dunlop
Discovery Neuroscience, Wyeth Research, Princeton, NJ 08543, USA
Mol Pharmacol 68:974-82. 2005..Taken in combination with its selectivity over ionotropic and metabotropic glutamate receptors, this compound represents a potential tool for the further elucidation of EAAT2 function... - High-throughput electrophysiology: an emerging paradigm for ion-channel screening and physiologyJohn Dunlop
Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton, New Jersey 08543, USA
Nat Rev Drug Discov 7:358-68. 2008.... - Old and new pharmacology: positive allosteric modulation of the alpha7 nicotinic acetylcholine receptor by the 5-hydroxytryptamine(2B/C) receptor antagonist SB-206553 (3,5-dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b']di pyrrole-1(2H)-carboxamide)John Dunlop
Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
J Pharmacol Exp Ther 328:766-76. 2009..This latter observation provides further evidence in support of the potential therapeutic utility of alpha7 nAChR PAMs in schizophrenia... - WAY-855 (3-amino-tricyclo[2.2.1.02.6]heptane-1,3-dicarboxylic acid): a novel, EAAT2-preferring, nonsubstrate inhibitor of high-affinity glutamate uptakeJohn Dunlop
Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
Br J Pharmacol 140:839-46. 2003..WAY-855 represents a novel structure in glutamate transporter pharmacology, and exploration of this structure might provide insights into the discrimination between EAAT2 and other EAAT subtypes... - Glutamate-based therapeutic approaches: targeting the glutamate transport systemJohn Dunlop
Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton, New Jersey 08543, USA
Curr Opin Pharmacol 6:103-7. 2006..In addition, momentum has been gained with the discovery of compounds capable of upregulating the activity of the predominant forebrain glutamate transporter, EAAT2... - In vitro screening strategies for nicotinic receptor ligandsJohn Dunlop
Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
Biochem Pharmacol 74:1172-81. 2007.... - Pharmacological profile of the 5-HT(2C) receptor agonist WAY-163909; therapeutic potential in multiple indicationsJohn Dunlop
Discovery Neuroscience, Wyeth Research, Princeton, NJ 08543, USA
CNS Drug Rev 12:167-77. 2006..Consistent with a potential therapeutic utility in obesity, schizophrenia and depression WAY-163909 was found to have robust dose-dependent effects in animal models of obesity, psychotic-like behavior or depression... - Ion channel screeningJohn Dunlop
Neuroscience Discovery Research and Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
Comb Chem High Throughput Screen 11:514-22. 2008.... - Pharmacological characterization of threo-3-methylglutamic acid with excitatory amino acid transporters in native and recombinant systemsS Eliasof
Neurocrine Biosciences Inc, San Diego, California, USA Wyeth Neuroscience, Wyeth-Ayerst Research, Princeton, New Jersey, USA
J Neurochem 77:550-7. 2001..Thus, T3MG represents a pharmacological tool for the study of not only the predominant EAAT2 subtype but also the EAAT4 subtype highly expressed in cerebellum... - Acid sensing ion channel (ASIC) inhibitors exhibit anxiolytic-like activity in preclinical pharmacological modelsJason M Dwyer
Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ, 08543 8000, USA
Psychopharmacology (Berl) 203:41-52. 2009..Of particular interest is ASIC1a, which is located in areas associated with fear and anxiety behaviors. Recent reports suggest a role for ASIC1a in preclinical models of fear conditioning and anxiety... - The pharmacological profile of L-glutamate transport in human NT2 neurones is consistent with excitatory amino acid transporter 2J Dunlop
CNS Disorders, Wyeth Ayerst Research, Princeton, NJ 08543 8000, USA
Eur J Pharmacol 360:249-56. 1998.... - Rb+ efflux through functional activation of cardiac KCNQ1/minK channels by the benzodiazepine R-L3 (L-364,373)Flora Jow
Discovery Neuroscience, Wyeth Research, Princeton, NJ 08543, USA
Assay Drug Dev Technol 4:443-50. 2006..In addition, the assay also can be used for evaluation of possible long-QT liability during cardiac selectivity of new chemical entities... - Substrate exchange properties of the high-affinity glutamate transporter EAAT2J Dunlop
Wyeth Neuroscience, Wyeth Ayerst Research, Princeton, New Jersey 08543, USA
J Neurosci Res 66:482-6. 2001..The estimate of drug induced [3H] efflux with the cloned EAAT2 transporter represents a convenient biochemical assay for the discrimination of substrate and non-substrate inhibitors of the EAAT2 subtype... - Validation of a medium-throughput electrophysiological assay for KCNQ2/3 channel enhancers using IonWorks HTFlora Jow
Discovery Neuroscience, Wyeth Research, Princeton, New Jersey 08543 8000, USA
J Biomol Screen 12:1059-67. 2007..The authors found that there was a very good correlation (R(2) > 0.9) between the 2 assays, thus demonstrating the highly predictive nature of the IonWorks assay... - A novel method for patch-clamp automationD Vasilyev
Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543 8000, USA
Pflugers Arch 452:240-7. 2006..This system represents an efficient method for patch-clamp automation without the need for a complex and expensive electrophysiological set-up for cell visualization... - Impaired spinal cord glutamate transport capacity and reduced sensitivity to riluzole in a transgenic superoxide dismutase mutant rat model of amyotrophic lateral sclerosisJohn Dunlop
Neuroscience, Wyeth Research, Princeton, New Jersey 08543-8000, USA
J Neurosci 23:1688-96. 2003.... - Synthesis and 5-hydroxytryptamine (5-HT) activity of 2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5-(6H)ones and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoxalinesG S Welmaker
Medicinal Chemistry, Chemical Sciences, Wyeth Ayerst Research, Princeton, NJ 08543, USA
Bioorg Med Chem Lett 10:1991-4. 2000..Compound 21R inhibited food intake over 2 h in fasted, male Sprague Dawley rats with ED50 values of 2 mg/kg (i.p.) and 10 mg/kg (p.o.)... - Full and partial agonist activity of C-terminal cholecystokinin peptides at the cloned human CCK-A receptor expressed in Chinese hamster ovary cellsJ Dunlop
Wyeth Ayerst Research, Princeton, NJ 08540, USA
Peptides 18:865-8. 1997..These results demonstrate that CCK-8S represents the minimum ligand requirement for both high affinity and full agonist activity at the human CCK-A receptor subtype... - Characterization of 5-HT1A receptor functional coupling in cells expressing the human 5-HT1A receptor as assessed with the cytosensor microphysiometerJ Dunlop
Wyeth Ayerst Research, CNS Disorders, Princeton, New Jersey 08543, USA
J Pharmacol Toxicol Methods 40:47-55. 1998..The evaluation of 5-HT1A ligands using the microphysiometer, which represents a very distinct indice of 5-HT1A receptor function compared with the cAMP assay, results in a different profile of functional activity... - YM022 [(R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo-5-phenyl-1H-1,4- benzodiazepin-3-yl]-3-(3-methylphenyl)urea]: an irreversible cholecystokinin type-B receptor antagonistJ Dunlop
Biochemistry Laboratory, Wyeth Research UK Ltd, Maidenhead
Biochem Pharmacol 54:81-5. 1997..Thus, YM022 behaves as an irreversible antagonist, whilst its structural analogue L-365,260 exhibits properties consistent with a competitive antagonist... - CCK receptor antagonistsJ Dunlop
CNS Disorders, Wyeth Ayerst Research, Princeton, NJ 08543, USA
Gen Pharmacol 31:519-24. 1998..5. L-365,260 behaves in a manner consistent with that of a competitive antagonist and both L-740,093 and YM022 behave as insurmountable CCK-B receptor antagonists in vitro... - Pharmacological characterization of a Chinese hamster ovary cell line transfected with the human CCK-B receptor geneJ Dunlop
Biochemistry Laboratory, Wyeth Research UK Ltd, Taplow, Maidenhead
Neuropeptides 30:359-63. 1996..This cell line provides a powerful new tool for the evaluation and development of novel ligands acting at the human CCK-B receptor subtype... - 5-HT2C receptor agonists as an innovative approach for psychiatric disordersSharon Rosenzweig-Lipson
Wyeth Discovery Neuroscience, Princeton, New Jersey 08543, USA
Drug News Perspect 20:565-71. 2007..The current review highlights the underlying complexities of this area and provides the rationale for using 5-HT(2C) agonists in the treatment of both schizophrenia and depressive disorders... - Development of an improved IP(1) assay for the characterization of 5-HT(2C) receptor ligandsJean Y Zhang
Department of Neuroscience, Wyeth Research, 865 Ridge Road, Monmouth Junction, NJ 08852, USA
Assay Drug Dev Technol 8:106-13. 2010..78) than with values determined by radioactive IP(1) method (R(2) = 0.64). Our study shows that the HTRF FRET-based assay detects IP(1) with good sensitivity and may be streamlined for high-throughput (HTS) applications... - Neuronal nicotinic acetylcholine receptors - targets for the development of drugs to treat cognitive impairment associated with schizophrenia and Alzheimer's diseaseSimon N Haydar
Chemical Sciences, Wyeth Research, Princeton, NJ 08543, USA
Curr Top Med Chem 10:144-52. 2010.... - A novel high-throughput screening assay for HCN channel blocker using membrane potential-sensitive dye and FLIPRDmitry V Vasilyev
Discovery Neuroscience, Wyeth Research, Princeton, New Jersey 08543 8000, USA
J Biomol Screen 14:1119-28. 2009..The reported HTS-compatible HCN channel blocker assay can serve as a tool in drug discovery in the pursuit of HCN channel isoform-selective small molecules that could be used in the development of clinically relevant compounds... - Antidepressant-like effects of the novel, selective, 5-HT2C receptor agonist WAY-163909 in rodentsSharon Rosenzweig-Lipson
Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
Psychopharmacology (Berl) 192:159-70. 2007..Activation of one or more of the serotonin (5-HT) receptors may play a role in mediating the antidepressant effects of SSRIs... - SAR and biological evaluation of SEN12333/WAY-317538: Novel alpha 7 nicotinic acetylcholine receptor agonistSimon N Haydar
Chemical Sciences and Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton, NJ 08543 8000, USA
Bioorg Med Chem 17:5247-58. 2009..The SAR and biological evaluation of this series of compounds are discussed... - Development of a scintillation proximity assay binding method for the human 5-hydroxytryptamine 6 receptor using intact cellsTikva Carrick
Neuroscience Discovery Research, Wyeth Research, Princeton, NJ 08543, USA
Anal Biochem 381:27-32. 2008..81+/-0.017, make the SPA format amenable to automation and higher throughput; hence, this assay can be a viable alternative to the more labor-intensive filtration and centrifugation methods... - Amiloride is neuroprotective in an MPTP model of Parkinson's diseaseRobert L Arias
Wyeth Discovery Neuroscience, Princeton, New Jersey 08543 8000, USA
Neurobiol Dis 31:334-41. 2008..These findings represent the first experimental evidence of a potential role for ASICs in the pathogenesis of Parkinson's disease... - hERG (KCNH2 or Kv11.1) K+ channels: screening for cardiac arrhythmia riskMark R Bowlby
Neuroscience Discovery, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
Curr Drug Metab 9:965-70. 2008.... - WAY-100635 antagonist-induced plasticity of 5-HT receptors: regulatory differences between a stable cell line and an in vivo native systemXavier Z Khawaja
Neuroscience, Wyeth Research, Princeton, New Jersey, USA
J Neurochem 98:134-45. 2006..This suggests that an antagonist can influence 5-HT(1A) receptor recycling in vitro differently to in vivo regulatory conditions... - Characterization of the 5-HT6 receptor coupled to Ca2+ signaling using an enabling chimeric G-proteinJean Y Zhang
Neuroscience Discovery Research, Wyeth Research, CN-8000, Princeton, NJ 08543-8000, USA
Eur J Pharmacol 472:33-8. 2003.... - Evaluation of FLIPR Calcium 3 Assay Kit--a new no-wash fluorescence calcium indicator reagentYingxin Zhang
Neuroscience Discovery Research, Wyeth Research, Princeton, NJ 08543, USA
J Biomol Screen 8:571-7. 2003..Our results validate Calcium 3 as a compelling alternative to FLUO-4 in the choice of fluorescent dye reagent for studying G-protein-coupled receptors, providing the advantage of a homogenous, no-wash assay format... - Cycloalkyl[b][1,4]benzodiazepinoindoles are agonists at the human 5-HT2C receptorAnnmarie L Sabb
Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543 8000, USA
Bioorg Med Chem Lett 14:2603-7. 2004..In addition, WAY-629 was active in vivo in a rat model of feeding behavior. An SAR study based on WAY-629 led to compound 11 (K(i) 13 nM, E(max) 102%)... - Validation of an atomic absorption rubidium ion efflux assay for KCNQ/M-channels using the ion Channel Reader 8000Kewei Wang
Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
Assay Drug Dev Technol 2:525-34. 2004..By measuring the supernatant only, the throughput of ICR8000 in an eight-point titration is estimated to be 40 compounds per day, which is suitable for a secondary confirmation assay... - Synthesis and biological activities of aryl-ether-, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT-2Alexander Greenfield
Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
Bioorg Med Chem Lett 15:4985-8. 2005..Compound (16) represents one of the most potent (IC50=85+/-5 nM) and selective inhibitors of EAAT-2 identified to date... - Distinct functional profiles of aripiprazole and olanzapine at RNA edited human 5-HT2C receptor isoformsJean Y Zhang
Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
Biochem Pharmacol 71:521-9. 2006..5-HT2C agonism may also underlie the minimal weight gain seen with aripiprazole... - Direct inhibition of Ih by analgesic loperamide in rat DRG neuronsDmitry V Vasilyev
Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543 8000, USA
J Neurophysiol 97:3713-21. 2007..Because I(h) channels are involved in pain processing, loperamide-induced inhibition of I(h) channels could provide an additional molecular mechanism for its analgesic action... - Antiobesity-like effects of the 5-HT2C receptor agonist WAY-161503Sharon Rosenzweig-Lipson
Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543 8000, USA
Brain Res 1073:240-51. 2006.... - Ligand dependency of 5-hydroxytryptamine 2C receptor internalizationBrian D Schlag
Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
J Pharmacol Exp Ther 310:865-70. 2004..These results were confirmed by confocal microscopy. They demonstrate that the 5-HT2C receptor is internalized by incubation with agonists and partial agonists but not with inverse agonists or neutral antagonists... - A cog in cognition: how the alpha 7 nicotinic acetylcholine receptor is geared towards improving cognitive deficitsSteven C Leiser
Discovery Neuroscience, Wyeth Research, Princeton, NJ 08543, United States
Pharmacol Ther 122:302-11. 2009..This review will focus on the recent work highlighting the role of alpha7 in cognition and cognitive processes... - Ion channel screening plates: design, construction, and maintenanceScott C Mayer
Chemical Sciences, Pfizer Global Research and Development, Princeton, New Jersey 08543, USA
Assay Drug Dev Technol 8:504-11. 2010.... - Properties of excitatory amino acid transport in the human U373 astrocytoma cell lineJ Dunlop
CNS Disorders, Wyeth Ayerst Research, Princeton, NJ 08543 8000, USA
Brain Res 839:235-42. 1999..In conclusion, the Na(+)-dependent high-affinity L-glutamate transport into human U373 astrocytoma cells appears to be mediated predominantly by the EAAT3 subtype... - The JNK pathway amplifies and drives subcellular changes in tau phosphorylationJ Vogel
Discovery Neuroscience, Wyeth Research, CN8000, Princeton, NJ 08543, USA
Neuropharmacology 57:539-50. 2009..Together these data provide novel insights into the JNK pathway and a high resolution perspective on how this pathway influences tau phosphorylation and dynamics in neurons... - Functional calcium coupling with the human metabotropic glutamate receptor subtypes 2 and 4 by stable co-expression with a calcium pathway facilitating G-protein chimera in Chinese hamster ovary cellsDianne Kowal
Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
Biochem Pharmacol 66:785-90. 2003.... - The C-terminus of Gi family G-proteins as a determinant of 5-HT(1A) receptor couplingDianne Kowal
Wyeth Research, Neuroscience Discovery Research, CN-8000, Princeton, NJ 08543-8000, USA
Biochem Biophys Res Commun 294:655-9. 2002..These results indicate the C-terminus of Gi3 as an important determinant for coupling to the 5-HT(1A) receptor, while the reduced functional agonist activities suggest additional motifs participate in receptor/G-protein coupling... - Screening of immunophilin ligands by quantitative analysis of neurofilament expression and neurite outgrowth in cultured neurons and cellsDanni Liu
Neuroscience Discovery Research, Wyeth Research, Princeton, NJ 08543, United States
J Neurosci Methods 163:310-20. 2007..Taken together, these results demonstrate the potential utility of the neurofilament ELISA and Cellomics ArrayScan platform to efficiently quantify neurotrophic effects of immunophilin ligands on cultured neurons and cell lines... - The role of transmembrane helix 5 in agonist binding to the human H3 receptorAlbert J Uveges
Wyeth Neurosciences, Princeton, New Jersey 08543, USA
J Pharmacol Exp Ther 301:451-8. 2002..These observations suggest that the agonist receptor complexes formed by these three different H3 agonists are not conformationally equivalent... - Novel pharmacological activity of loperamide and CP-339,818 on human HCN channels characterized with an automated electrophysiology assayYan T Lee
Discovery Neuroscience, Wyeth Research, CN 8000, Princeton, NJ 08543 8000, United States
Eur J Pharmacol 581:97-104. 2008.... - Serotonin mechanisms in heart valve disease II: the 5-HT2 receptor and its signaling pathway in aortic valve interstitial cellsJie Xu
Cardiology Research Laboratory, Children's Hospital of Philadelphia, Philadelphia, Pennsylvania, USA
Am J Pathol 161:2209-18. 2002..Thus, major 5-HT Erk 1/2 signaling beyond that controlled by 5-HT(2)Rs must involve other serotonin receptor types and/or secondary signaling events... - A conservative, single-amino acid substitution in the second cytoplasmic domain of the human Serotonin2C receptor alters both ligand-dependent and -independent receptor signalingKelly A Berg
Department of Pharmacology 7764, University of Texas Health Science Center, 7703 Floyd Curl Drive, San Antonio, TX 78229, USA
J Pharmacol Exp Ther 324:1084-92. 2008.... - Role of the GLT-1 subtype of glutamate transporter in glutamate homeostasis: the GLT-1-preferring inhibitor WAY-855 produces marginal neurotoxicity in the rat hippocampusJulie V Selkirk
Neurosciences Department, Neurocrine Biosciences Inc, 12970 El Camino Real, San Diego, CA 92130, USA
Eur J Neurosci 21:3217-28. 2005.... - mGlu4 potentiation of K(2P)2.1 is dependant on C-terminal dephosphorylationStuart M Cain
Strathclyde Institute of Pharmacy and Biomedical Sciences, The University of Strathclyde, 27 Taylor Street, Glasgow G4 0NR, UK
Mol Cell Neurosci 37:32-9. 2008..1 activity through a reduction in C-terminal phosphorylation, which represents a novel mechanism by which group III mGlu receptors may regulate cell excitability and synaptic activity... - Functional properties of alpha7 nicotinic acetylcholine receptors co-expressed with RIC-3 in a stable recombinant CHO-K1 cell lineRenza Roncarati
Discovery Research, Siena Biotech S p A, Siena, Italy
Assay Drug Dev Technol 6:181-93. 2008..This recombinant cell system is useful for characterization of alpha7 nAChRs and to study the mechanism of action of chemical modulators, in particular the detection of PAMs capable of slowing receptor desensitization kinetics... - glaikit is essential for the formation of epithelial polarity and neuronal developmentJohn Dunlop
Medical Research Council, Centre for Developmental Neurobiology, 4th Floor, New Hunts House, Guys Campus, King s College London, London SE1 1UL, United Kingdom
Curr Biol 14:2039-45. 2004..A mutation in the human homolog of gkt causes the neurodegenerative disease spinocerebellar ataxia with neuropathy (SCAN1), making it possible that a failure of membrane protein localization is a cause of this disease...