Pharmacological effects of an aldehyde type alpha/beta-adrenoceptor blocking agent with vasodilating properties

General Pharmacology
C C ChiuJ L Yeh

Abstract

KMUP 880723 (0.5, 1.0, and 3.0 mg/kg, iv) produced dose-dependent hypotensive and bradycardia responses in pentobarbital-anesthetized Wistar rats. KMUP 880723 (1.0 mg/kg, iv) also markedly inhibited both the tachycardia effects induced by (-)isoproterenol and arterial pressor responses induced by phenylephrine. In the isolated Wistar rat right atria, left atria, and guinea pig tracheal strips, KMUP 880723 competitively antagonized the (-)isoproterenol-induced positive chronotropic effects, inotropic effects, and tracheal relaxation effects in a concentration-dependent manner. The parallel shift to the right of the concentration-response curve of (-)isoproterenol suggested that KMUP 880723 was a beta(1)/beta(2)-adrenoceptor competitive antagonist. The apparent pA(2) values were 6.89+/-0.10 in the right atria, 7.02+/-0.09 in the left atria, and 6.59+/-0.11 in the trachea, indicating that KMUP 880723 was a nonselective beta-adrenoceptor blocker. In thoracic aorta experiments, KMUP 880723 also produced a competitive antagonism of norepinephrine-induced contraction with a pA(2) value of 7.14+/-0.06. In isolated rat thoracic aorta, KMUP 880723 more potently relaxed the contractions induced by norepinephrine (3 x 10(-6) M) than those ...Continue Reading

References

Feb 1, 1991·American Heart Journal·W H Frishman
Mar 1, 1994·Journal of the American College of Cardiology·R N DoughtyN Sharpe
Jul 1, 1996·Journal of Cardiovascular Pharmacology·Y T LinI J Chen
Mar 31, 1999·American Journal of Therapeutics·H K Shapiro

Citations

Jan 4, 2005·Pharmacology·K NandakumarS H Bhardwaj
Dec 29, 2007·The Journal of Pharmacology and Experimental Therapeutics·Tamara J van SteegElizabeth C M de Lange
May 22, 2002·Journal of Cardiovascular Pharmacology·Jwu-Lai YehIng-Jun Chen

Related Concepts

N-(4-(2-hydroxy-3-(2-methoxy-1-oxyethylaminobenzene)propoxy))benzaldehyde
Adrenergic alpha-Antagonists
Adrenergic beta-Antagonists
Metazoa
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Tenormin
Benzaldehydes
Diastolic Blood Pressure
Cardiovascular Agents
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