Phencyclidine An Update by Doris H. (Ed.) Clouet PDF

By Doris H. (Ed.) Clouet

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1984). These data indicate that the nicotinic AChR-PCP receptor differs from the rat brain PCP receptor. Furthermore, our findings are 46 consistent with the view that the rat brain PCP receptor is the voltage-regulated, noninactivating K channel in the nerve terminals, and that this channel consists of at least two subunits of MR=80 kD and 95 kD. HOW DOES PCP PRODUCE ITS BEHAVIORAL EFFECTS? The striking correlation between behavioral potency and block of 86Rb efflux component SV, for PCP analogues and the stereoisomer pairs of "sigma opiates," provides strong circumstantial evidence that the K channel block may underlie the behavioral effects of these drugs.

Assuming that block of the K channels corresponding to SV does cause the behavioral deficit, it is important to consider the possibility that block of only a small fraction of these K channels may be sufficient to induce behavioral change. THE EFFECTS OF PCP ANALOGUES ON COMPONENT Sv If the behavioral activity of PCP is related to its block of presynaptic K channels (Albuquerque et al. 1981; Albuquerque et al. 1983; Blaustein and Ickowicz 1983), PCP-like analogues should block these same K channels with a rank order of potency that parallels their relative in vivo psychotomimetic activity.

Isolation of peptide hormones by reverse-phase high pressure liquid chromatography. , ed. Peptides, Structure and Biological Function. , 1979. pp. 121-125. L. Stereoisomers of Nallylnormetazocine: phencyclidine-like behavioral effects in squirrel monkeys and rats. Science 215:178, 1982. ; and Cuatrecasas, P. Multiple opiate receptors: Different regional distribution in the brain and differential binding of opiates and opioid peptides. Mol Pharmacol 16:91-104, 1979. , and Cuatrecasas, P. Novel opiate binding sites selective for benzomorphan drugs.

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Phencyclidine An Update by Doris H. (Ed.) Clouet


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