Phencyclidine/SKF-10,047 binding sites: evaluation of function.
Results of correlation analyses comparing rank-order affinities with rank-order potencies of (+)SKF-10,047, phencyclidine (PCP), and several PCP analogs support the involvement of [3H]-1-[1-(2-thienyl)cyclohexyl]piperidine binding sites (TCP sites) in mediating both the discriminative stimulus properties of PCP and production of 180 degrees perseveration in a 4-arm radial maze. For the same group of drugs, no significant relationship was found to exist between affinities at haloperidol-sensitive (+)[3H]SKF-10,047 binding sites (H-S-SKF sites) and potencies. Also, H-S-SKF sites were found to lack pharmacological selectivity and to be localized in the microsomal fraction of cells. It is concluded that TCP sites may represent receptors which mediate effects not only of PCP, but also of (+)SKF-10,047. In addition, the possibility that H-S-SKF sites may represent a type of membrane-bound enzyme is discussed.
McCann
D J
DJ
Department of Pharmacology and Therapeutics, School of Medicine and Biomedical Sciences, State University of New York, Buffalo 14214.
Rabin
R A
RA
Rens-Domiano
S
S
Winter
J C
JC
D000818:Animals; D004347:Drug Interactions; D006220:Haloperidol / Q000494:pharmacology; D007858:Learning / Q000187:drug effects; D008297:Male; D008861:Microsomes / Q000187:drug effects; D051381:Rats; D011916:Rats, Inbred F344; D017981:Receptors, Neurotransmitter / Q000502:physiology*; D011957:Receptors, Opioid / Q000502:physiology*; D017478:Receptors, Phencyclidine; D017480:Receptors, sigma; D013574:Synaptosomes / Q000187:drug effects; D014403:Tubocurarine / Q000494:pharmacology
D017981:Receptors, Neurotransmitter; D011957:Receptors, Opioid; D017478:Receptors, Phencyclidine; D017480:Receptors, sigma; D006220:Haloperidol; D014403:Tubocurarine