Dopamine receptor stimulating and alpha adrenoceptor blocking actions of trans (CS-265) and cis (CS-263) isomers of nonhydroxylated N-propyl octahydrobenzo[F]quinoline.
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| Abstract |
Experiments were designed to determine the dopaminergic and alpha adrenergic receptors involvement of cis (CS-263) and trans (CS-265) isomers of nonhydroxylated N-propyl octahydrobenzo[f]quinoline. Both compounds caused competitive blockade of presynaptic alpha-2 adrenoceptors of guinea-pig ileum and rat vas deferens. Postsynaptic alpha-1 adrenoceptors of rabbit aorta was inhibited. In the guinea-pig ileum, these compounds were found to be as active as yohimbine. In the rabbit aorta, they were weaker antagonists of phenylephrine than prazosin. CS-compounds reversed epinephrine-induced pressor responses and inhibited reflex hypertensive responses to stimulation of the central stump of sciatic nerve in anesthetized cats. Only CS-265 inhibited reflex tachycardia of sciatic nerve stimulation. In isolated cat right atria, CS-265 inhibited stimulation-induced tachycardic response through stimulation of presynaptic dopamine receptors in contrast to CS-263 that produced potentiation of stimulation-induced tachycardia. The results suggest that CS-265 is an unusual compound having dopamine receptor stimulating activity and alpha adrenoceptor blocking properties. These divergent properties provide direct evidence that presynaptic alpha-2 adrenoceptors and dopamine-receptors are different entities on the sympathetic nerve terminal.
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| Authors | M Ilhan, J P Long, J G Cannon |
| Journal | The Journal of pharmacology and experimental therapeutics (J Pharmacol Exp Ther) Vol. 231 Issue 2 Pg. 361-6 (Nov 1984) ISSN: 0022-3565 [Print] United States |
| PMID | 6149308 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, P.H.S.) |
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