论文部分内容阅读
本文介绍奥派文和蒂巴因C_6和C_(14)间桥联-乙烯键的衍生物I_(a-k),具有强吗啡激动剂作用,当R_1、R_2为小基团氢或甲基时(I_(a-d)),作用随脂溶性增大而增强。当R_1为甲基,R_2增长为乙基、正丙基(C_(19)为R构型)其作用显著增强,其中依托啡(I_i)效力为吗啡的1200倍;但当R_2为甲基,R_1增长时(C_(19)为S构型)作用无明显变化(表I)。此外,当氮上甲基以拮抗性基团烯丙基或环丙甲基取代时,如C_(19)取代基及构型均与依托啡相同,则仍为强激动剂,但如R_1、R_2与I_d相同(皆为甲基)则为拮抗剂,其中N-环丙甲基衍生物拮抗作用为丙烯吗啡50倍(表Ⅱ)。
In this paper, I_ (ak), a derivative of bridging-vinyl bond between C_6 and C_ (14), is a powerful morphine agonist. When R_1 and R_2 are small groups of hydrogen or methyl group I_ (ad)), the role of fat-soluble increase with increased. When R_1 is methyl, R_2 is increased to ethyl and n-propyl (C_ (19) is R), the effect of etomid (I_i) is 1200 times of that of morphine. But when R_2 is methyl, R_1 increased (C_ (19) for the S configuration) no significant change in the role (Table I). In addition, when the methyl group on the nitrogen is replaced by an allyl or cyclopropylmethyl group as an antagonist, the C 19 substituent and the conformation are the same as that of etorphine and are still strong agonists. However, R_2 and I_d are the same (all methyl) as antagonists, with N-cyclopropylmethyl antagonists antagonizing 50 times propylene morphine (Table II).