一系列外型和内型-6-羟基-2-氨基苯并降冰片烯的合成及抗伤害感受特性

Synthesis and antinociceptive properties of a series of exo- and endo-6-hydroxy-2-aminobenzonorbornenes.

作者信息

Crooks P A, Burn P, Sewell R D, Upton N

出版信息

J Pharm Sci. 1986 Oct;75(10):1010-3. doi: 10.1002/jps.2600751022.

DOI:10.1002/jps.2600751022

Abstract

A series of 6-hydroxy endo- and exo-derivatives of 2-aminobenzonorbornene has been synthesized and evaluated for antinociceptive activity in the mouse. The results indicated a stereospecific effect in the antinociceptive responses exhibited by the two isomeric groups of compounds. The exo-amines 10a-10c were inactive in both the tail immersion and tail clip tests. The corresponding endo-isomers exhibited antinociceptive properties; 4a was the most active compound tested but was toxic at the dose administered.

摘要

已合成了一系列2-氨基苯并降冰片烯的6-羟基内型和外型衍生物，并在小鼠中评估了其抗伤害感受活性。结果表明，这两类异构体化合物在抗伤害感受反应中表现出立体特异性效应。外型胺10a - 10c在尾部浸入和尾部夹捏试验中均无活性。相应的内型异构体表现出抗伤害感受特性；4a是测试的最具活性的化合物，但在所给药剂量下有毒。

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