The sigma [corrected] ligand rimcazole antagonises (+)SKF 10,047, but not (+)3-PPP, in the mouse isolated vas deferens.
We have characterized the actions of several sigma receptor ligands on the electrically evoked, neurogenic contractions of the mouse isolated vas deferens. (-)SKF 10,047 was significantly more potent than (+)SKF 10,047 in potentiating twitch contractions and was equipotent with (+)3-PPP. Rimcazole (1 and 3 microM) antagonised the potentiation induced by 100 microM (+)SKF 10,047 and, to a lesser extent, that induced by 30 microM (-)SKF 10,047 but increased that elicited by (+)3-PPP (30 microM). This apparent contradiction may arise from sigma agonists acting in this tissue at both sigma and non-sigma sites.
Kennedy
C
C
Department of Pharmacology, University of Cambridge, U.K.
Jarvis
G E
GE
Henderson
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G
D000818:Animals; D014150:Antipsychotic Agents / Q000494:pharmacology*; D002227:Carbazoles / Q000494:pharmacology*; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D008811:Mice, Inbred DBA; D009130:Muscle, Smooth / Q000187:drug effects*; D010620:Phenazocine / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors / Q000494:pharmacology; D010880:Piperidines / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D013237:Stereoisomerism; D014649:Vas Deferens / Q000187:drug effects
D014150:Antipsychotic Agents; D002227:Carbazoles; D010880:Piperidines; C012134:SK&F 10047; C026539:preclamol; C034931:rimcazole; D010620:Phenazocine