Hexahydro-1H-1-pyrindines from acid rearrangement of 9-alkylidene-5-(m-methoxyphenyl)-2-methylmorphans. Structural type of narcotic antagonists

H Awaya, EL May, MD Aceto, LS Harris…

文献索引：Awaya; May; Aceto; Harris; Silverton; Rice; Mattson; Jacobson Journal of Medicinal Chemistry, 1987 , vol. 30, # 5 p. 947 - 950

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被引用次数: 4

摘要

2, 4a, 5, 6, 7, 7a-hexahydro-4-(3-hydroxyphenyl)-l-methyl-1H-pyrindine] follows from analogy and NMR data. Compounds 3 and 4 are opioid antagonists of about the potency of nalorphine in the tail-flick vs. morphine assay and precipitate a complete abstinence syndrome in morphine-dependent monkeys. Both are nearly devoid of antinociceptive activity and they have about 0.025 times the affinity of nalorphine for the p opioid receptor. ...