Discovery of 1-(2,4-Dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a Potential Peripheral Cannabinoid-1 Receptor Inverse Agonist

Discovery of 1-(2,4-Dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a Potential Peripheral Cannabinoid-1 Receptor Inverse Agonist

Fast food nation! The title compound (pictured) was identified as a potential peripheral CB1‐acting antagonist based on its negative central effects in CB1R agonist‐induced hypothermia and analgesia models, and low brain exposure as indicated by the blood‐to‐plasma ratio. This compound represents a...

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Veröffentlicht in:ChemMedChem 2010-09, Vol.5 (9), p.1439-1443
Hauptverfasser: Hung, Ming-Shiu, Chang, Chun-Ping, Li, Ting-Chieh, Yeh, Teng-Kuang, Song, Jen-Shin, Lin, Yinchiu, Wu, Chien-Huang, Kuo, Po-Chu, Amancha, Prashanth K., Wong, Ying-Chieh, Hsiao, Wen-Chi, Chao, Yu-Sheng, Shia, Kak-Shan
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Anti-Obesity Agents - chemistry
Anti-Obesity Agents - pharmacology
blood-brain barrier
Blood-Brain Barrier - metabolism
brain-to-plasma ratio
cannabinoid-1 receptor
central nervous system
diet-induced obesity
Disease Models, Animal
Drug Evaluation, Preclinical
Drug Inverse Agonism
Humans
Hypothermia - drug therapy
Male
Pyrazoles - chemical synthesis
Pyrazoles - chemistry
Pyrazoles - pharmacokinetics
Rats
Rats, Sprague-Dawley
Receptor, Cannabinoid, CB1 - antagonists & inhibitors
Receptor, Cannabinoid, CB1 - metabolism
Receptor, Cannabinoid, CB2 - antagonists & inhibitors
Receptor, Cannabinoid, CB2 - metabolism
Structure-Activity Relationship
Thiophenes - chemical synthesis
Thiophenes - chemistry
Thiophenes - pharmacokinetics
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Zusammenfassung:Fast food nation! The title compound (pictured) was identified as a potential peripheral CB1‐acting antagonist based on its negative central effects in CB1R agonist‐induced hypothermia and analgesia models, and low brain exposure as indicated by the blood‐to‐plasma ratio. This compound represents a potential lead in the treatment of metabolic disorders.
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.201000246