Behavioral and biochemical stereoselectivity of sigma opiate/PCP receptors.
The relative potencies of the stereoisomers of ketamine, N-allylnormetazocine and cyclazocine were determined at mu opiate and sigma opiate/phencyclidine (PCP) receptors in vitro in rat brain homogenates, as well as in a discriminative stimulus behavioral paradigm in rats trained to discriminate PCP from saline. In all cases the in vivo and in vitro data were in agreement. The (+)-isomers of N-allylnormetazocine and cyclazocine are highly specific sigma opiate/PCP ligands.
D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects*; D001921:Brain / Q000378:metabolism; D003496:Cyclazocine / Q000494:pharmacology*; D004091:Hydromorphone / Q000494:pharmacology*; D066298:In Vitro Techniques; D007649:Ketamine / Q000494:pharmacology*; D008297:Male; D010620:Phenazocine / Q000031:analogs & derivatives* / Q000494:pharmacology; D010622:Phencyclidine / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D011957:Receptors, Opioid / Q000187:drug effects / Q000502:physiology*; D013237:Stereoisomerism
D011957:Receptors, Opioid; D007649:Ketamine; C012134:SK&F 10047; D010620:Phenazocine; D010622:Phencyclidine; D003496:Cyclazocine; D004091:Hydromorphone