5,8-二取代-2-氨甲基-3,4-二氢萘的镇痛及镇静活性
Analgesic and tranquilizing activity of 5,8-disubstituted 2-aminomethyl-3,4-dihydronaphthalenes.
作者信息
Welch W M, Plattner J J, Stratten W P, Harbert C A
出版信息
J Med Chem. 1978 Mar;21(3):257-63. doi: 10.1021/jm00201a004.
PMID:628000
Abstract
Interesting analgesic activity approaching that of meperidine and codeine was observed in standard animal models for 8-chloro-3,4-dihydro-5-methoxy-2-pyrrolidinomethylnaphthalene (compound 7). This compound was orally effective and its analgesic activity was not reversed by the opiate antagonist, naloxone. A limited number of other 2-aminomethyl analogues displayed activity in neuroleptic screens.
摘要
在标准动物模型中，观察到8-氯-3,4-二氢-5-甲氧基-2-吡咯烷甲基萘（化合物7）具有接近哌替啶和可待因的有趣镇痛活性。该化合物口服有效，其镇痛活性不会被阿片拮抗剂纳洛酮逆转。其他有限数量的2-氨基甲基类似物在抗精神病药物筛选中显示出活性。
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