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翻訳と辞書　辞書検索 [ 開発暫定版 ] スポンサード リンク NESS-0327 ： ウィキペディア英語版 NESS-0327 NESS-0327 is a drug used in scientific research which acts as an extremely potent and selective antagonist of the cannabinoid receptor CB1. It is much more potent an antagonist, and more selective for the CB1 receptor over CB2, than the more commonly used ligand rimonabant, with a Ki at CB1 of 350fM (i.e. 0.00035nM) and a selectivity of over 60,000x for CB1 over CB2.〔Ruiu S, Pinna GA, Marchese G, Mussinu JM, Saba P, Tambaro S, Casti P, Vargiu R, Pani L. Synthesis and characterization of NESS 0327: a novel putative antagonist of the CB1 cannabinoid receptor. ''Journal of Pharmacology and Experimental Therapeutics''. 2003 Jul;306(1):363-70. PMID 12663689〕 Independently, two other groups have described only modest nanomolar CB1 affinity for this compound (125nM〔A.R. Stoit, J.H.M. Lange, A.P. den Hartog, E. Ronken, K. Tipker, H.H. van Stuivenberg, J.A.R. Dijksman, H.C. Wals, C.G. Kruse, Chem. Pharm. Bull. 50 (2002) 1109-1113〕 and 18.4nM〔Y. Zhang, J.P. Burgess, M. Brackeen, A. Gilliam, S.W. Mascarella, K. Page, H.H. Seltzman, B.F. Thomas, J. Med. Chem. 51 (2008) 3526-3539〕). Also unlike rimonabant, NESS-0327 does not appear to act as an inverse agonist at higher doses, instead being a purely neutral antagonist which blocks the CB1 receptor but does not produce any physiological effect of its own.〔Tambaro S, Mongeau R, Dessi C, Pani L, Ruiu S. Modulation of ATP-mediated contractions of the rat vas deferens through presynaptic cannabinoid receptors. ''European Journal of Pharmacology''. 2005 Nov 21;525(1-3):150-3. PMID 16271359〕 ==See also== * Discovery and development of Cannabinoid Receptor 1 Antagonists * NESS-040C5 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「NESS-0327」の詳細全文を読む スポンサード リンク 翻訳と辞書 : 翻訳のためのインターネットリソース Copyright(C) kotoba.ne.jp 1997-2016. All Rights Reserved.