TETRAHYDRO-9-AMINOACRIDINE (THA) INTERACTS WITH THE PHENCYCLIDINE (PCP) RECEPTOR-SITE

被引：42

作者：

ALBIN, RL ^{[1
]}

YOUNG, AB ^{[1
]}

PENNEY, JB ^{[1
]}

机构：

[1] UNIV MICHIGAN, DEPT NEUROL, NEUROSCI LAB BLDG, 1103 E HURON, ANN ARBOR, MI 48104 USA

来源：

NEUROSCIENCE LETTERS | 1988年 / 88卷 / 03期

关键词：

D O I：

10.1016/0304-3940(88)90228-5

中图分类号：

Q189 [神经科学];

学科分类号：

071006 [神经生物学];

摘要：

The effect of tetrahydro-9-aminoacridine (THA) and related compounds on ligand binding to the dissociative anesthetic (phencyclidine, PCP) receptor site was assessed using a rat brain homogenate assay. THA displaced the dissociative anesthetic ligand [3H]N-(1-[2-thienyl]cyclohexyl)3-4-piperidine ([3H]TCP) binding with an IC50 of 26 .mu.M. Other acridine derivatives displayed similar potency as displacers of [3H]TCP. Cholinesterase inhibitors and aminopyridines had IC50s equal to or greater than 100 .mu.M. Saturation studies of [3H]TCP in the presence and absence of 30 .mu.M THA revealed competitive inhibition with a K1 of 15 .mu.M. The clinical pharmacology of THA suggests that it antagonizes the effects of dissociative anesthetics whereas in vitro, it behaves as a weak PCP agonist. THA may exert some of its clinical effects through interaction with the PCP receptor, and may have mixed agonist-antagonist properties.

引用

页码：303 / 307

页数：5

共 17 条

[1]

TETRAHYDROAMINOACRIDINE ANTAGONISM TO NARCOTIC ADDICTION [J].