Contreras P C, Contreras M L, O'Donohue T L, Lair C C
Experimental Therapeutics Branch, National Institute of Neurological and Communicative Disorders and Stroke, Bethesda, Maryland 20892.
Synapse. 1988;2(3):240-3. doi: 10.1002/syn.890020311.
The purpose of this study was to examine the binding and behavioral effects mediated by PCP and sigma receptors in the rat. From the radioreceptor assays, it was possible to characterize two binding sites that interact with PCP and sigma ligands. The two sites, a PCP and sigma receptor, could be differentiated based on drug selectivity and potency. In the behavioral assays, MK-801, which bound preferentially to the PCP receptor, and 1,3-di-0-tolylguanidine, which bound preferentially to the sigma receptor, induced sniffing, rearing, circling, backpedaling, and weaving behavior. These results indicate that there are distinct PCP and sigma receptors that are both involved in mediating stereotyped behavior and ataxia in the rat.
本研究的目的是检测大鼠中由苯环己哌啶(PCP)和σ受体介导的结合及行为效应。从放射受体分析中,有可能鉴定出与PCP和σ配体相互作用的两个结合位点。这两个位点,即PCP和σ受体,可以根据药物选择性和效力加以区分。在行为分析中,优先与PCP受体结合的MK-801和优先与σ受体结合的1,3-二邻甲苯基胍,均可诱发嗅探、竖毛、转圈、倒退及摇摆行为。这些结果表明,存在不同的PCP和σ受体,它们均参与介导大鼠的刻板行为和共济失调。