N-立方基甲基取代吗啡类化合物作为新型麻醉拮抗剂。

N-cubylmethyl substituted morphinoids as novel narcotic antagonists.

作者信息

Cheng C Y, Hsin L W, Lin Y P, Tao P L, Jong T T

机构信息

School of Pharmacy, College of Medicine, National Taiwan University, Taipei, R.O.C.

出版信息

Bioorg Med Chem. 1996 Jan;4(1):73-80. doi: 10.1016/0968-0896(95)00165-4.

DOI:10.1016/0968-0896(95)00165-4

PMID:8689242

Abstract

N-Cubylmethylnormorphine (1) and N-cubylmethylnoroxymorphone (2) have been synthesized and found to be more potent ligands at the mu and kappa opioid receptors than morphine and oxymorphone respectively. In the guinea-pig ileum preparation, compounds 1 and 2 were characterized as opioid mu antagonists (Ke = 68 and 16 nM, respectively). Compound 2 also showed effective kappa-antagonism (Ke = 22 nM). The narcotic antagonism activity of 1 has been confirmed by in vivo assays.

摘要

N-立方甲基去甲吗啡（1）和N-立方甲基去甲羟吗啡酮（2）已被合成，并且发现它们分别在μ和κ阿片受体上比吗啡和羟吗啡酮是更有效的配体。在豚鼠回肠制备实验中，化合物1和2被表征为阿片μ拮抗剂（Ke分别为68和16 nM）。化合物2也显示出有效的κ拮抗作用（Ke = 22 nM）。1的麻醉拮抗活性已通过体内试验得到证实。