The effects of bufuralol, a beta-adrenoceptor antagonist with predominant beta 2-adrenoceptor agonistic activity, in the cat and the dog.
The effects of bufuralol and its carbinol metabolite have been compared with those of propranolol in the anaesthetised and conscious cat and dog. Bufuralol and its carbinol metabolite are nonselective beta-adrenoceptor antagonists; the former has equivalent potency to propranolol, whereas the latter is six times more potent. In anaesthetised animals both bufuralol and its metabolite exhibited partial agonistic activity, resulting in tachycardia and vasodilation. In conscious cats there was no change in heart rate or slight bradycardia, whereas in dogs both compounds again produced tachycardia. In anaesthetised and conscious cats and conscious dogs, both bufuralol and the metabolite increased abdominal aortic blood flow. There was a reduction in blood pressure in the conscious dog. It is concluded that the partial agonistic activity of bufuralol and its carbinol metabolite is exerted mainly at the beta 2-adrenoceptor, producing vasodilation and reducing peripheral resistance, resulting in a reduction in blood pressure with a long duration of action.
D000318:Adrenergic beta-Agonists / Q000494:pharmacology*; D000319:Adrenergic beta-Antagonists / Q000494:pharmacology*; D000768:Anesthesia, General; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D002415:Cats; D003243:Consciousness; D004285:Dogs; D004983:Ethanolamines / Q000494:pharmacology*; D005260:Female; D006339:Heart Rate / Q000187:drug effects; D008297:Male; D011433:Propranolol / Q000494:pharmacology; D011943:Receptors, Adrenergic, beta / Q000187:drug effects; D012039:Regional Blood Flow / Q000187:drug effects; D013997:Time Factors; D014655:Vascular Resistance / Q000187:drug effects; D014664:Vasodilation / Q000187:drug effects
D000318:Adrenergic beta-Agonists; D000319:Adrenergic beta-Antagonists; D004983:Ethanolamines; D011943:Receptors, Adrenergic, beta; C039685:Ro 03-7410; C010831:bufuralol; D011433:Propranolol