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源自大麻素的药物。4. 硫和碳环类似物中烷基取代的影响。

Drugs derived from cannabinoids. 4. Effect of alkyl substitution in sulfur and carbocyclic analogs.

作者信息

Razdan R K, Handrick G R, Dalzell H C, Howes J F, Winn M, Plotnikoff N P, Dodge P W, Dren A T

出版信息

J Med Chem. 1976 Apr;19(4):552-4. doi: 10.1021/jm00226a023.

DOI:10.1021/jm00226a023
PMID:944269
Abstract

Various CNS-active cannabinoids in which the alicyclic ring was thiopheno, cyclopenteno, or cyclohexeno with the alkyl substituent in various positions (structural types 1-6) were synthesized by procedures described previously. These compounds were compared in selected pharmacological tests in mice, rats, dogs, and cats. The results suggested that methyl substitution in the close proximity of the phenolic hydroxyl group strongly influenced the activity of some cannabinoids, particularly of those which had a planar five-membered alicyclic ring rather than a six-membered ring.

摘要

通过先前描述的方法合成了各种中枢神经系统活性大麻素,其中脂环族环为噻吩并、环戊烯并或环己烯并,烷基取代基位于不同位置(结构类型1 - 6)。在小鼠、大鼠、狗和猫身上进行的选定药理学测试中对这些化合物进行了比较。结果表明,酚羟基附近的甲基取代对某些大麻素的活性有强烈影响,特别是那些具有平面五元脂环族环而非六元环的大麻素。

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