Biomaterial Database

Relaxant effects of BRL 38227 and pinacidil on the rat gastric fundus. 1992

R A Lefebvre, and J Horacek

Heymans Institute of Pharmacology, University of Gent Medical School, Belgium.

Concentration-effect curves for BRL 38227 (lemakalim) and pinacidil were obtained in longitudinal muscle strips of the rat gastric fundus contracted by prostaglandin F2 alpha. Both agents induced a concentration-dependent relaxation, with BRL 38227 (EC50 = 3 x 10(-6) M) being more potent than pinacidil (EC50 = 8 x 10(-6) M). Glibenclamide (10(-7), 10(-6) and 10(-5) M) antagonized the relaxant effect of BRL 38227 and pinacidil but neither antagonism was of the simple competitive type. Phentolamine (10(-7), 10(-6) and 10(-5) M) competitively antagonized the effect of pinacidil and non-competitively that of BRL 38227. Glibenclamide had no influence on the relaxant effect induced by vasoactive intestinal polypeptide or by electrical field stimulation in the presence of atropine and guanethidine. The results suggest that glibenclamide-sensitive K+ channels are present in the rat gastric fundus and that they do not mediate the inhibitory response to non-adrenergic, non-cholinergic neurostimulation.

UI	MeSH Term	Description	Entries
D008297	Male		Males
D009126	Muscle Relaxation	That phase of a muscle twitch during which a muscle returns to a resting position.	Muscle Relaxations,Relaxation, Muscle,Relaxations, Muscle
D010646	Phentolamine	A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.	Fentolamin,Phentolamine Mesilate,Phentolamine Mesylate,Phentolamine Methanesulfonate,Phentolamine Mono-hydrochloride,Regitine,Regityn,Rogitine,Z-Max,Mesilate, Phentolamine,Mesylate, Phentolamine,Methanesulfonate, Phentolamine,Mono-hydrochloride, Phentolamine,Phentolamine Mono hydrochloride
D011758	Pyrroles	Azoles of one NITROGEN and two double bonds that have aromatic chemical properties.	Pyrrole
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
D005260	Female		Females
D005748	Gastric Fundus	The superior portion of the body of the stomach above the level of the cardiac notch.	Fundus, Gastric
D005905	Glyburide	An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide	Glibenclamide,Daonil,Diabeta,Euglucon 5,Euglucon N,Glybenclamide,HB-419,HB-420,Maninil,Micronase,Neogluconin,HB 419,HB 420,HB419,HB420
D006146	Guanidines	A family of iminourea derivatives. The parent compound has been isolated from mushrooms, corn germ, rice hulls, mussels, earthworms, and turnip juice. Derivatives may have antiviral and antifungal properties.
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia