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σ受体配体和苯环己哌啶类似物的生化及行为效应

Biochemical and behavioral effects of sigma and PCP ligands.

作者信息

Contreras P C, Contreras M L, O'Donohue T L, Lair C C

机构信息

Experimental Therapeutics Branch, National Institute of Neurological and Communicative Disorders and Stroke, Bethesda, Maryland 20892.

出版信息

Synapse. 1988;2(3):240-3. doi: 10.1002/syn.890020311.

DOI:10.1002/syn.890020311
PMID:2850629
Abstract

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.

摘要

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。

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1
Biochemical and behavioral effects of sigma and PCP ligands.σ受体配体和苯环己哌啶类似物的生化及行为效应
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The novel anticonvulsant MK-801: a potent and specific ligand of the brain phencyclidine/sigma-receptor.新型抗惊厥药MK-801:一种强效且特异性的脑苯环利定/σ受体配体。
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Comparative electroencephalographic and behavioral effects of phencyclidine, (+)-SKF-10,047 and MK-801 in rats.苯环利定、(+)-SKF-10,047和MK-801对大鼠脑电图及行为的比较影响
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Differential regulation of sigma and PCP receptors after chronic administration of haloperidol and phencyclidine in mice.小鼠长期给予氟哌啶醇和苯环己哌啶后σ受体和PCP受体的差异调节
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Synapse. 1989;4(1):1-10. doi: 10.1002/syn.890040102.

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Enhancement of immobility in a forced swimming test by subacute or repeated treatment with phencyclidine: a new model of schizophrenia.苯环己哌啶亚急性或重复给药增强强迫游泳试验中的不动时间:一种新的精神分裂症模型
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