GYKI-12743 a new postsynaptic vascular alpha-adrenoceptor antagonist.
Using the pithed rat preparation it has been proven that GYKI-12743 exerted its alpha-adrenergic blocking action only at the postsynaptic vascular level in the cardiovascular system. This new molecule failed to antagonize the presynaptic alpha 2-adrenoceptors of the cardiac sympathetic nerve endings. Thereby it was possible to demonstrate the first vasoselective postsynaptic adrenoceptor antagonist which potentially might be interesting in the cardiovascular therapy.
Institute for Drug Research, Budapest, Hungary.
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Rabloczky
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Jaszlits
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Horváth
D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology*; D000818:Animals; D001381:Azepines / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects*; D003000:Clonidine / Q000494:pharmacology; D003655:Decerebrate State; D004146:Dioxanes / Q000494:pharmacology*; D004558:Electric Stimulation; D006339:Heart Rate / Q000187:drug effects*; D019329:Idazoxan; D010646:Phentolamine / Q000494:pharmacology; D010656:Phenylephrine / Q000494:pharmacology; D011724:Pyridazines / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D015016:Yohimbine / Q000494:pharmacology
D000317:Adrenergic alpha-Antagonists; D001381:Azepines; D004146:Dioxanes; D011724:Pyridazines; C064892:GYKI 12743; D010656:Phenylephrine; D015016:Yohimbine; C015603:azepexole; D003000:Clonidine; D019329:Idazoxan; D010646:Phentolamine