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Abstract

Effect of trimetoquinol analogs for antagonism of endoperoxide/thromboxane A2-mediated responses in human platelets and rat aorta.

A Mukhopadhyay, S S Navran, H M Amin, S A Abdel-Aziz, J Chang, D J Sober, D D Miller and D R Feller
Journal of Pharmacology and Experimental Therapeutics January 1985, 232 (1) 1-9;
A Mukhopadhyay
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S S Navran
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H M Amin
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S A Abdel-Aziz
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J Chang
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D J Sober
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D D Miller
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D R Feller
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Abstract

The pharmacological properties of a limited series of tetrahydro-isoquinoline [trimetoquinol (TMQ)] analogs for inhibition of endoperoxide (U46619)-mediated responses in human platelets and rat aorta were examined. All analogs blocked U46619-induced aggregatory and secretory responses in platelets, and contraction of rat aorta in a concentration-dependent manner. R-(+)-TMQ was a competitive-type inhibitor of U46619-induced contractions of rat aorta. The relative inhibitory potency for TMQ analogs against U46619-induced effects was TMQ greater than N-methyl TMQ greater than or equal to erythro-alpha-methyl TMQ greater than threo-alpha-methyl TMQ greater than or equal to alpha-dimethyl TMQ. R-(+)-TMQ and the azoprostanoid analog (U51605) were potent antagonists of U46619 action in rat aorta with pA2 values of 5.97 and 5.70, respectively. Other experiments indicated that U51605 was a partial agonist and R-(+)-TMQ was an inhibitor of U51605-induced contractions of rat aorta (pKB = 5.94). R-(+)-TMQ also blocked prostaglandin E2-mediated responses in rat aorta (pA2 = 5.46) but was ineffective as an antagonist of prostaglandin F2 alpha and LTD4 responses in dog iris sphincter and guinea-pig trachea or lung parenchyma, respectively. The data indicate that 1) the TMQ analogs were antagonists of endoperoxide/thromboxane A2-mediated responses in rat aorta and human platelets involving a similar mechanism of action and 2) stereochemical requirements of these TMQ analogs for activation of beta adrenoceptors and antagonism of endoperoxide/thromboxane A2-mediated responses are different. It is concluded that selectivity for these two pharmacological properties of TMQ can be achieved by appropriate stereochemical modification of the tetrahydroisoquinoline nucleus.

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Journal of Pharmacology and Experimental Therapeutics
Vol. 232, Issue 1
1 Jan 1985
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Abstract

Effect of trimetoquinol analogs for antagonism of endoperoxide/thromboxane A2-mediated responses in human platelets and rat aorta.

A Mukhopadhyay, S S Navran, H M Amin, S A Abdel-Aziz, J Chang, D J Sober, D D Miller and D R Feller
Journal of Pharmacology and Experimental Therapeutics January 1, 1985, 232 (1) 1-9;

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Abstract

Effect of trimetoquinol analogs for antagonism of endoperoxide/thromboxane A2-mediated responses in human platelets and rat aorta.

A Mukhopadhyay, S S Navran, H M Amin, S A Abdel-Aziz, J Chang, D J Sober, D D Miller and D R Feller
Journal of Pharmacology and Experimental Therapeutics January 1, 1985, 232 (1) 1-9;
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