N-cubylmethyl substituted morphinoids as novel narcotic antagonists

CY Cheng, LW Hsin, YP Lin, PL Tao, TT Jong

文献索引：Cheng, Chen-Yu; Hsin, Ling-Wei; Lin, Yen-Pin; Tao, Pao-Luh; Jong, Ting-Ting Bioorganic and Medicinal Chemistry, 1996 , vol. 4, # 1 p. 73 - 80

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被引用次数: 29

摘要

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