Alpha-adrenoceptor-blocking properties of some trypanocidal diamidines.
A series of trypanocidal diamidines and diimidazolines known to cause severe hypotension were tested for their alpha-adrenoceptor blocking properties in vitro. At the postsynaptic alpha 1-receptor of the guinea-pig aorta in vitro all compounds at doses of 0.5 to 50 mumol/l showed weak antagonistic effects against noradrenaline. Similar results were obtained at the presynaptic alpha 2-receptor of the rat vas deferens.
D000317:Adrenergic alpha-Antagonists; D000818:Animals; D001667:Binding, Competitive; D005260:Female; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D009638:Norepinephrine / Q000037:antagonists & inhibitors; D051381:Rats; D011919:Rats, Inbred Strains; D014344:Trypanocidal Agents / Q000494:pharmacology*
D000317:Adrenergic alpha-Antagonists; D014344:Trypanocidal Agents; D009638:Norepinephrine