Biochemical and behavioral effects of sigma and PCP ligands.
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.
Contreras
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Experimental Therapeutics Branch, National Institute of Neurological and Communicative Disorders and Stroke, Bethesda, Maryland 20892.
Contreras
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O'Donohue
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Lair
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D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism*; D003986:Dibenzocycloheptenes / Q000494:pharmacology; D016291:Dizocilpine Maleate; D006146:Guanidines / Q000494:pharmacology; D007700:Kinetics; D008024:Ligands; D008297:Male; D008566:Membranes / Q000378:metabolism; D009294:Narcotics / Q000494:pharmacology*; D010622:Phencyclidine / Q000378:metabolism* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D017981:Receptors, Neurotransmitter / Q000187:drug effects / Q000378:metabolism*; D011957:Receptors, Opioid / Q000187:drug effects / Q000378:metabolism*; D017478:Receptors, Phencyclidine; D017480:Receptors, sigma; D013239:Stereotyped Behavior / Q000187:drug effects*
D000927:Anticonvulsants; D003986:Dibenzocycloheptenes; D006146:Guanidines; D008024:Ligands; D009294:Narcotics; D017981:Receptors, Neurotransmitter; D011957:Receptors, Opioid; D017478:Receptors, Phencyclidine; D017480:Receptors, sigma; D016291:Dizocilpine Maleate; D010622:Phencyclidine; C050232:1,3-ditolylguanidine