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.
Rabloczky
G
G
Institute for Drug Research, Budapest, Hungary.
Jaszlits
L
L
Horváth
E
E
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