5'-胍基纳曲吲哚，一种高度选择性且强效的κ-阿片受体拮抗剂。
5'-Guanidinonaltrindole, a highly selective and potent kappa-opioid receptor antagonist.
作者信息
Jones R M, Portoghese P S
机构信息
Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, 308 Harvard Street S.E., Minneapolis, MN 55455, USA.
出版信息
Eur J Pharmacol. 2000 May 12;396(1):49-52. doi: 10.1016/s0014-2999(00)00208-9.
5'-Guanidinonaltrindole (GNTI) possesses 5-fold greater opioid antagonist potency (K(e)=0.04 nM) and an order of magnitude greater selectivity (selectivity ratios >500) than the prototypical kappa-opioid receptor antagonist, norbinaltorphimine, in smooth muscle preparations. Binding and functional studies conducted on cloned human opioid receptors expressed in Chinese hamster ovarian (CHO) cells afforded pA(2) values that were comparable to the smooth muscle data. In view of the high selectivity and potency of GNTI, it is a potentially valuable pharmacological tool for opioid research.
5'-胍基纳曲吲哚（GNTI）在平滑肌制剂中具有比典型的κ-阿片受体拮抗剂诺宾那托啡胺高5倍的阿片拮抗剂效力（K(e)=0.04 nM）和一个数量级以上的选择性（选择性比率>500）。对在中国仓鼠卵巢（CHO）细胞中表达的克隆人阿片受体进行的结合和功能研究得出的pA(2)值与平滑肌数据相当。鉴于GNTI的高选择性和效力，它是阿片类药物研究中一种潜在有价值的药理学工具。
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