(+)-3-PPP antagonizes the discriminative stimulus effects of (+)-N-allylnormetazocine.
The functional significance of the reported affinity of (+)-3-PPP and (+)-N-allylnormetazocine (NANM) for the same binding site in rat brain membranes was assessed by studying (+)-3-PPP as a agonist and antagonist of (+)-NANM in rats trained to discriminate 5.0 mg/kg (+)-NANM from saline. Over a wide dose range, (+)-3-PPP was able to block the discriminative stimulus effects of (+)-NANM, with complete antagonism at 1.0 mg/kg i.p. Since (+)-NANM is a prototype sigma-opioid agonist, (+)-3-PPP is a good candidate for being a competitive sigma antagonist.
D000818:Animals; D001665:Binding Sites; D003216:Conditioning, Operant; D004192:Discrimination, Psychological; D005795:Generalization, Stimulus; D010620:Phenazocine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D010880:Piperidines / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D011957:Receptors, Opioid / Q000187:drug effects; D017465:Receptors, Opioid, delta
D010880:Piperidines; D011957:Receptors, Opioid; D017465:Receptors, Opioid, delta; C012134:SK&F 10047; C026539:preclamol; D010620:Phenazocine