Salva P S, Hite G J, Heyman R A, Gianutsos G
J Med Chem. 1986 Oct;29(10):2111-3. doi: 10.1021/jm00160a054.
The synthesis of a series of 9-phenyl-3,7-diazabicyclanes and 9-(m-hydroxyphenyl)-3,7-diazabicyclanes is described. Members of both series were tested for antinociception in rat tail withdrawal and mouse acetic acid writhing assays. Their affinities for opiate receptors in rat brain homogenate were also determined. The 9-phenyl compounds, 1a-c, were inactive. However, the 9-(m-hydroxyphenyl) analogues, 2a-c, were found to possess significant activity in the writhing assay, comparable to that of morphine. All activity was reversed by naloxone.
本文描述了一系列9-苯基-3,7-二氮杂双环烷和9-(间羟基苯基)-3,7-二氮杂双环烷的合成。对这两个系列的成员进行了大鼠甩尾和小鼠醋酸扭体试验的抗伤害感受测试。还测定了它们对大鼠脑匀浆中阿片受体的亲和力。9-苯基化合物1a-c无活性。然而，发现9-(间羟基苯基)类似物2a-c在扭体试验中具有显著活性，与吗啡相当。所有活性均被纳洛酮逆转。
