title: Involvement of sigma-receptors in the increase in contraction of mouse vas deferens induced by exogenous ATP.
abstract: The effects of sigma-receptor ligands on the twitch contraction elicited by the exogenous application of adenosine 5'-triphosphate (ATP) in the unstimulated mouse vas deferens were studied. (-)-Pentazocine, 1,3-di(2-tolyl)guanidine(DTG) and two pairs of optical isomers of 3-(3-hydroxyphenyl)-N-(1-propyl)piperidine(3-PPP) and N-allylnormetazocine (SKF-10,047) potentiated the exogenous application of ATP-induced twitch-type contraction in a concentration-dependent manner, while (+)-pentazocine did not affect it. The order of potentiating ability was: (+)-3-PPP > (-)pentazocine > (-)-SKF-10,047> DTG > (-)-3-PPP > (+)-SKF-10,047. On the other hand, haloperidol and rimcazole, putataive sigma-receptor antagonists, suppressed this twitch contraction. In addition, these antagonists significantly blocked the (+)-3-PPP- and (-)-pentazocine-induced potentiation at concentrations which did not affect contractions per se. These findings indicate that the exogenous application of ATP-induced twitch contraction in the mouse vas deferens is regulated by sigma-receptors. In addition, the present ranking order suggests that the sigma-receptor potentiating the ATP-induced twitch contraction at post-junctional sites may differ from the sigma 1- and/or sigma 2-receptor subtypes.
authors.affiliation: Central Research Laboratories, Santen Pharmaceutical Co., Ltd., Osaka, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Matsuno
authors.forename: T
authors.initials: T
authors.lastname: Kobayashi
authors.forename: S
authors.initials: S
authors.lastname: Mita
mesh_terms: D000255:Adenosine Triphosphate / Q000494:pharmacology*; D000701:Analgesics, Opioid / Q000494:pharmacology; D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology; D014150:Antipsychotic Agents / Q000494:pharmacology; D002227:Carbazoles / Q000494:pharmacology; D018491:Dopamine Agonists / Q000494:pharmacology; D018492:Dopamine Antagonists / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004357:Drug Synergism; D006146:Guanidines / Q000494:pharmacology; D006220:Haloperidol / Q000494:pharmacology; D008024:Ligands; D008297:Male; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects* / Q000502:physiology; D010423:Pentazocine / Q000494:pharmacology; D010620:Phenazocine / Q000031:analogs & derivatives / Q000494:pharmacology; D010880:Piperidines / Q000494:pharmacology; D017480:Receptors, sigma / Q000037:antagonists & inhibitors / Q000502:physiology*; D012044:Regression Analysis; D013329:Structure-Activity Relationship; D014649:Vas Deferens / Q000187:drug effects* / Q000378:metabolism / Q000502:physiology
chemical_list: D000701:Analgesics, Opioid; D000927:Anticonvulsants; D014150:Antipsychotic Agents; D002227:Carbazoles; D018491:Dopamine Agonists; D018492:Dopamine Antagonists; D006146:Guanidines; D008024:Ligands; D010880:Piperidines; D017480:Receptors, sigma; C012134:SK&F 10047; D000255:Adenosine Triphosphate; C026539:preclamol; C034931:rimcazole; D010620:Phenazocine; D006220:Haloperidol; C050232:1,3-ditolylguanidine; D010423:Pentazocine