Studies on the Mechanism of the Acute Antihypertensive and Vasodilator Actions of Several β‐Adrenoceptor Antagonists

  title={Studies on the Mechanism of the Acute Antihypertensive and Vasodilator Actions of Several $\beta$‐Adrenoceptor Antagonists},
  author={Edmund J. Sybertz and Thomas Baum and Kathryn Pula and Steve Nelson and E Eynon and C S Sabin},
  journal={Journal of Cardiovascular Pharmacology},
  • E. Sybertz, T. Baum, C. Sabin
  • Published 1 September 1982
  • Medicine, Chemistry, Biology
  • Journal of Cardiovascular Pharmacology
Summary Several new β-adrenoceptor antagonists (sulfinalol, MK 761, and prizidilol) have been reported to possess direct vasodilator activity in addition to blocking β-receptors. The mechanism of the hypotensive and vasodilator actions of these agents was examined and compared to that of pindolol and hydralazine. Intraarterial injection of each agent increased blood flow in the sympathetically denervated hindlimb of anesthetized dogs. Doses increasing flow by 50 ml/min (ED50) were 0.48, 0.24… 
Autonomic and antihypertensive activity of oral amosulalol (YM-09538), a combined alpha- and beta-adrenoceptor blocking agent in conscious rats.
It is concluded that alpha-adrenoceptor blockade by amosulalol might account for its antihypertensive activity and that its beta-ad Renin activity reduces plasma renin activity (PRA) and heart rate in SHR with established hypertension and may inhibit reflexogenic increases in heart rate and PRA due to the reduction in blood pressure.
Comparative β-adrenoceptor blocking effect and pharmacokinetics of bucindolol and propranolol in man
Comparison of the time courses of plasma bucindolol and the cardiac β-adrenoceptor blockade strongly suggests that in man buc Cindolol undergoes an extensive first-pass effect, leading to the formation of one or more active metabolites.
Materials and Methods a and 9-Adrenoceptor blocking activity in pithed rats: Male normotensive Wistar rats
Amosulalol is a newly developed antihypertensive agent with a combined a and ,3-adrenoceptor blocking activity, which was selected from a series of sulfamoylphenethylamines and exerts a selective postsynaptic a1 adrenoceptor and a nonselective Adrenoceptor blockade.
  • J. Marwood, G. Stokes
  • Chemistry, Medicine
    Clinical and experimental pharmacology & physiology
  • 1986
A portion of the hypotensive effect of bucindolol was independent of effects on α‐ or β‐adrenoceptors, and this was attributed to direct vasodilatation.
Comparison of intravenous dilevalol with placebo in moderate hypertension
Compared with placebo, dilevalol given intravenously appears to be safe and effective antihypertensive treatment.
Beta-adrenoceptor partial agonists: a renaissance in cardiovascular therapy?
  • D. Waller
  • Biology, Medicine
    British journal of clinical pharmacology
  • 1990
0-adrenoceptors were first identified more than 40 years ago by Ahlquist (1948), and were subsequently shown to consist of two subtypes, known as 13 and 12, which have become established in the management of a wide variety of cardiovascular diseases.