[On the pharmacology of the beta-receptor blocker penbutolol (author's transl)].
1-tert.-Butylamino-3-(2-cyclopentylphenoxy)-propan-2-ol (penbutolol, Hoe 893d) is a beta-adrenergic blocking agent about 4 times more active than propranolol in vivo and in vitro. In comparison to propranolol it is characterized by a longer lasting activity. The antihypertensive effect of penbutolol in spontaneously hypertonic rats is more than 5 times stronger than that of propranolol. Penbutolol reduces basal plasma renin activity in the same dose range as does propranolol but is about 3 times stronger with respect to isoproterenol-induced increase of PRA. Penbutolol is 5 times more potent than propranolol inhibiting isoproterenol-stimulated phosphorylase activity in the isolated heart. In reserpine pretreated rats, penbutolol has a moderate intrinsic sympathomimetic activity (ISA). Penbutolol shows less unspecific actions -- such as negative inotropy or calcium antagonism -- than propranolol. Characteristic parameters of lung function (compliance and resistance) are less affected by penbutolol than propranolol in spite of the fact that penbutolol has a stronger beta-adrenergic blocking effect.
D000818:Animals; D002118:Calcium / Q000037:antagonists & inhibitors; D002415:Cats; D004285:Dogs; D006168:Guinea Pigs; D006439:Hemodynamics / Q000187:drug effects; D006973:Hypertension / Q000503:physiopathology; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D010394:Penbutolol / Q000494:pharmacology* / Q000633:toxicity; D006005:Phosphorylases / Q000037:antagonists & inhibitors; D011412:Propanolamines / Q000494:pharmacology*; D051381:Rats; D012083:Renin / Q000097:blood; D012119:Respiration / Q000187:drug effects; D013045:Species Specificity; D013997:Time Factors
D011412:Propanolamines; D010394:Penbutolol; D006005:Phosphorylases; D012083:Renin; D002118:Calcium
Zur Pharmakologie des beta-rezeptorenblockers penbutolol.