Biomaterial Database

Involvement of sigma-receptors in the increase in contraction of mouse vas deferens induced by exogenous ATP. 1996

K Matsuno, and T Kobayashi, and S Mita

Central Research Laboratories, Santen Pharmaceutical Co., Ltd., Osaka, Japan.

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.

UI	MeSH Term	Description	Entries
D008024	Ligands	A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)	Ligand
D008297	Male		Males
D009119	Muscle Contraction	A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	Inotropism,Muscular Contraction,Contraction, Muscle,Contraction, Muscular,Contractions, Muscle,Contractions, Muscular,Inotropisms,Muscle Contractions,Muscular Contractions
D009130	Muscle, Smooth	Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)	Muscle, Involuntary,Smooth Muscle,Involuntary Muscle,Involuntary Muscles,Muscles, Involuntary,Muscles, Smooth,Smooth Muscles
D010423	Pentazocine	The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97)	Fortral,Lexir,Pentazocine Hydrochloride,Pentazocine Lactate,Talwin,Hydrochloride, Pentazocine,Lactate, Pentazocine
D010620	Phenazocine	An opioid analgesic with actions and uses similar to MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1095)	Phenbenzorphan,Phenethylazocine,Narphen,Phenazocine Hydrobromide,Hydrobromide, Phenazocine
D010880	Piperidines	A family of hexahydropyridines.
D012044	Regression Analysis	Procedures for finding the mathematical function which best describes the relationship between a dependent variable and one or more independent variables. In linear regression (see LINEAR MODELS) the relationship is constrained to be a straight line and LEAST-SQUARES ANALYSIS is used to determine the best fit. In logistic regression (see LOGISTIC MODELS) the dependent variable is qualitative rather than continuously variable and LIKELIHOOD FUNCTIONS are used to find the best relationship. In multiple regression, the dependent variable is considered to depend on more than a single independent variable.	Regression Diagnostics,Statistical Regression,Analysis, Regression,Analyses, Regression,Diagnostics, Regression,Regression Analyses,Regression, Statistical,Regressions, Statistical,Statistical Regressions
D002227	Carbazoles	Benzo-indoles similar to CARBOLINES which are pyrido-indoles. In plants, carbazoles are derived from indole and form some of the INDOLE ALKALOIDS.
D004305	Dose-Response Relationship, Drug	The relationship between the dose of an administered drug and the response of the organism to the drug.	Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response