نتایج جستجو برای: pyridinyl

تعداد نتایج: 490  

Journal: :The Journal of pharmacology and experimental therapeutics 2002
M Motasim Billah Nicola Cooper Michael Minnicozzi Julie Warneck Peng Wang John A Hey William Kreutner Charles A Rizzo Sidney R Smith Simon Young Richard W Chapman Hazel Dyke Nang-Yang Shih John J Piwinski Francis M Cuss John Montana Ashit K Ganguly Robert W Egan

N-(3,5-Dichloro-1-oxido-4-pyridinyl)-8-methoxy-2-(trifluoromethyl)-5-quinoline carboxamide (SCH 351591) has been identified as a potent (IC(50) = 58 nM) and highly selective type 4 phosphodiesterase (PDE4) inhibitor with oral bioactivity in several animal models of lung inflammation. N-(3,5-Dichloro-4-pyridinyl)-8-methoxy-2-(trifluoromethyl)-5-quinoline carboxamide (SCH 365351), the only signif...

Journal: :The Journal of pharmacology and experimental therapeutics 2015
Sudeshna Ghosh Steven G Kinsey Qing-Song Liu Lenka Hruba Lance R McMahon Travis W Grim Christina R Merritt Laura E Wise Rehab A Abdullah Dana E Selley Laura J Sim-Selley Benjamin F Cravatt Aron H Lichtman

Inhibition of fatty acid amide hydrolase (FAAH) or monoacylglycerol lipase (MAGL), the primary hydrolytic enzymes for the respective endocannabinoids N-arachidonoylethanolamine (AEA) and 2-arachidonylglycerol (2-AG), produces antinociception but with minimal cannabimimetic side effects. Although selective inhibitors of either enzyme often show partial efficacy in various nociceptive models, the...

Journal: :The Journal of pharmacology and experimental therapeutics 2012
Daniel F Manvich Heather L Kimmel Debra A Cooper Leonard L Howell

Antagonists of the serotonin (5-hydroxytryptamine; 5-HT) type 2C receptor (5-HT(2C)R) are being considered as potential pharmacotherapeutics for various affective disorders, but evidence suggests that these compounds enhance the effects of cocaine and related psychostimulants in rodents. However, the effects of selective 5-HT(2C)R antagonists have not been evaluated in nonhuman primates. The pr...

Journal: :Nucleic acids research 1996
Chin-Yi Huang Guixia Bi Paul S. Miller

Homopurine sequences of duplex DNA are binding sites for triplex-forming oligodeoxyribopyrimidines. The interactions of synthetic duplex DNA targets with an oligodeoxyribopyrimidine containing N4-(6-amino-2-pyridinyl)deoxycytidine (1), a nucleoside designed to interact with a single C-G base pair interruption of the purine target tract, was studied by UV melting, circular dichroism spectroscopy...

Journal: :Journal of medicinal chemistry 2006
Jianjun Cheng Ryan Zeidan Swaroop Mishra Aijie Liu Suzie H Pun Rajan P Kulkarni Gregory S Jensen Nathalie C Bellocq Mark E Davis

To understand how chloroquine (CQ) enhances transgene expression in polycation-based, nonviral gene delivery systems, a number of CQ analogues with variations in the aliphatic amino side chain or in the aromatic ring are synthesized and investigated. Our studies indicate that the aliphatic amino moiety of CQ is essential to provide increased gene expression. Further, the enhancements are more d...

Journal: :The Journal of pharmacology and experimental therapeutics 2004
L E O'Dell L H Parsons

Previous work has demonstrated that peripheral serotonin(1B) (5-HT(1B)) receptor agonist administration facilitates the behavioral and neurochemical effects of cocaine. This study used dual probe microdialysis to investigate whether activation of serotonin(1B) (5-HT(1B)) receptors in the ventral tegmental area (VTA) alters the ability of peripherally administered cocaine to elevate dopamine (DA...

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