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一些4-苯胺基哌啶和4-苯基哌啶与μ、δ和κ结合位点的相互作用。

Interactions of some 4-anilinopiperidines and 4-phenylpiperidines with the mu, delta- and kappa-binding sites.

作者信息

Jin W Q, Paterson S J, Kosterlitz H W, Casy A F

出版信息

Life Sci. 1983;33 Suppl 1:251-3. doi: 10.1016/0024-3205(83)90490-3.

Abstract

The binding and pharmacological profiles of some 4-anilinopiperidine and 4-phenylpiperidine analogues were determined. The potency of the compounds to displace the binding of selective tritiated ligands was measured in homogenates of guinea-pig brain at 25 degrees C. All the compounds tested had high affinity for the mu-binding site, low affinity for the delta-site and were almost inactive at the kappa-site. The compounds were also tested for agonist activity in the guinea-pig ileum and the vasa deferentia of the mouse and rat. The pharmacological and binding profiles were compared.

摘要

测定了一些4-苯胺基哌啶和4-苯基哌啶类似物的结合和药理特性。在25℃下,于豚鼠脑匀浆中测定这些化合物取代选择性氚标记配体结合的效力。所有测试的化合物对μ-结合位点具有高亲和力,对δ-位点具有低亲和力,而对κ-位点几乎无活性。还在豚鼠回肠以及小鼠和大鼠的输精管中测试了这些化合物的激动剂活性。对药理和结合特性进行了比较。

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