501426-57-9Relevant academic research and scientific papers
Discovery of 2-[5-(4-chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H- pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an active metabolite. A novel, potent and selective cannabinoid-1 receptor inverse agonist with high antiobes
Wu, Chien-Huang,Hung, Ming-Shiu,Song, Jen-Shin,Yeh, Teng-Kuang,Chou, Ming-Chen,Chu, Cheng-Ming,Jan, Jiing-Jyh,Hsieh, Min-Tsang,Tseng, Shi-Liang,Chang, Chun-Ping,Hsieh, Wan-Ping,Lin, Yinchiu,Yeh, Yen-Nan,Chung, Wan-Ling,Kuo, Chun-Wei,Lin, Chin-Yu,Shy, Horng-Shing,Chao, Yu-Sheng,Shia, Kak-Shan
experimental part, p. 4496 - 4510 (2010/03/01)
By using the active metabolite 5 as an initial template, further structural modifications led to the identification of the titled compound 24 (BPR-890) as a highly potent CB1 inverse agonist possessing an excellent CB2/1 selectivity and remarkable in vivo
Heteroaryl-Pyrazole Derivatives as Cannabinoid CB1 Receptor Antagonists
-
Page/Page column 55, (2008/06/13)
A heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The present invention also provides a method for preparing the inventive heteroaryl-pyrasole compounds or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.
Biarylpyrazolyl oxadiazole as potent, selective, orally bioavailable cannabinoid-1 receptor antagonists for the treatment of obesity
Suk, Ho Lee,Hee, Jeong Seo,Lee, Sung-Han,Myung, Eun Jung,Park, Ji-Hyun,Park, Hyun-Ju,Yoo, Jakyung,Yun, Hoseop,Na, Jooran,Suk, Youn Kang,Song, Kwang-Seop,Kim, Min-Ah,Chang, Chong-Hwan,Kim, Jeongmin,Lee, Jinhwa
experimental part, p. 7216 - 7233 (2009/11/30)
Since the CB1 cannabinoid receptor antagonist 1 (SR141716, rimonabant) was previously reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. In the present study, biarylpyrazole analo
Synthesis, structure-activity relationship, and evaluation of SR141716 analogues: Development of central cannabinoid receptor ligands with lower lipophilicity
Katoch-Rouse, Reeti,Pavlova, Olga A.,Caulder, Tara,Hoffman, Alexander F.,Mukhin, Alexey G.,Horti, Andrew G.
, p. 642 - 645 (2007/10/03)
Exploration of the central CB1 cannabinoid receptors using positron emission tomography (PET) will allow for an understanding of the pharmacological and physiological role played by these receptors in the CNS. Current tracers are highly lipophi
