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O-1269 : ウィキペディア英語版
O-1269

O-1269 is a drug that is a diarylpyrazole derivative, related to potent cannabinoid antagonist drugs such as rimonabant and surinabant. However O-1269 and several related drugs were unexpectedly found to act as full or partial agonists at the cannabinoid receptors rather than antagonists, and so produce the usual effects expected of cannabinoid agonists in animal tests, such as sedation and analgesic effects. The N-heptyl homologue O-1270 and the N-propyl homologue O-1399 also act as cannabinoid agonists with similar potency ''in vivo'', despite weaker binding affinity at cannabinoid receptors compared to the pentyl homologue O-1269.〔Billy R. Martin, Raj K. Razdan, Anu Mahadevan. Pyrazole cannabinoid agonist and antagonists. US Patent 6509367, filed Sep 22, 2001, issued Jan 21, 2003.〕〔Shim JY, Welsh WJ, Cartier E, Edwards JL, Howlett AC. Molecular interaction of the antagonist N-(piperidin-1-yl)-5-(4-chlorophenyl)-1- (2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide with the CB1 cannabinoid receptor. ''Journal of Medicinal Chemistry''. 2002 Mar 28;45(7):1447-59. PMID 11906286〕〔Francisco ME, Seltzman HH, Gilliam AF, Mitchell RA, Rider SL, Pertwee RG, Stevenson LA, Thomas BF. Synthesis and structure-activity relationships of amide and hydrazide analogues of the cannabinoid CB(1) receptor antagonist N-(piperidinyl)- 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716). ''Journal of Medicinal Chemistry''. 2002 Jun 20;45(13):2708-19. PMID 12061874〕 Agonist-like and atypical cannabinoid activity has also been observed with a number of related compounds.
==References==



抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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