Quantitative analysis on isolated organs of the autonomic blocking properties of indoramin hydrochloride (Wy 21901).
1. Indoramin is a competitive alpha-adrenoceptor blocking agent on the guinea-pig isolated vas deferens and aortic strip; the pA(2) value on the aorta is 7.4.2. Indoramin is devoid of beta-adrenoceptor blocking activity on the guinea-pig isolated trachea (10(-4)M) and the Langendorff preparation of the rabbit heart (10(-6)M). It also has no adrenergic neurone blocking action on the Finkleman preparation of the rabbit small intestine (10(-5)M).3. On the Langendorff preparation of the rabbit isolated heart, indoramin (above 10(-6)M) has cardio-inhibitory properties similar to those of propranolol.4. On the guinea-pig isolated ileum (10(-5)M) and trachea (10(-6)M), indoramin is devoid of anticholinergic activity, but has a potent antihistamine action which satisfies the criteria for competitive antagonism; the pA(2) value for this antagonism on the ileum is 8.2.5. Indoramin antagonizes 5-hydroxytryptamine on the rat isolated fundus and ileum; the pA(2) value for the antagonism on the ileum is 6.0.
D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology; D000577:Amides / Q000494:pharmacology; D000818:Animals; D001011:Aorta / Q000187:drug effects; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D006634:Histamine H1 Antagonists / Q000494:pharmacology; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D007211:Indoles / Q000494:pharmacology*; D007421:Intestine, Small / Q000187:drug effects; D008297:Male; D010276:Parasympatholytics / Q000494:pharmacology; D010880:Piperidines / Q000494:pharmacology; D011817:Rabbits; D051381:Rats; D012702:Serotonin Antagonists; D013270:Stomach / Q000187:drug effects; D013565:Sympatholytics / Q000494:pharmacology*; D014132:Trachea / Q000187:drug effects; D014649:Vas Deferens / Q000187:drug effects
D000317:Adrenergic alpha-Antagonists; D000577:Amides; D006634:Histamine H1 Antagonists; D007211:Indoles; D010276:Parasympatholytics; D010880:Piperidines; D012702:Serotonin Antagonists; D013565:Sympatholytics