Pharmacological studies on the selectivity of HV-723, a new alpha-1 adrenoceptor antagonist.
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The pharmacological profile of a new alpha-1 adrenoceptor antagonist, α-ethyl-3, 4, 5-trimethoxy-α-(3-((2-(2-methoxyphenoxy)ethyl)amino)propyl) benzene-acetonitrile fumarate (HV-723), was studied in vitro. In dog mesenteric arteries, HV-723, prazosin and yohimbine competitively inhibited noradrenaline-induced contraction: the pA<SUB>2</SUB> value of HV-723 (9.37) was apparently larger than that of prazosin (8.22) and yohimbine (7.18). However, HV-723 showed no or only a slight inhibition on the contractile responses to 5-HT, KCl and prostaglandin F<SUB>2α</SUB>. HV-723 also showed potent alpha-1 adrenoceptor antagonist activity in the dog mesenteric and saphenous veins. However, HV-723 showed little antagonist activity on the pre and postsynaptic alpha-2 adrenoceptors, beta-1 and beta-2 adrenoceptors and muscarinic receptors. HV-723 also inhibited the sympathetic contraction induced by electrical transmural stimulation in the dog mesenteric arteries, and the inhibition of HV-723 was about 10 times more potent than that of prazosin. However, <SUP>3</SUP>H-noradrenaline release evoked by electrical stimulation was not influenced by HV-723. These results clearly show that HV-723 is a potent and selective alpha-1 adrenoceptor antagonist.
- 公益社団法人 日本薬理学会の論文
公益社団法人 日本薬理学会 | 論文
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