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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
1989-3-21
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pubmed:abstractText |
The pharmacological profile of a new alpha-1 adrenoceptor antagonist, alpha-ethyl-3,4,5-trimethoxy-alpha-(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 pA2 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 F2 alpha. 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, 3H-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.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Acetonitriles,
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic alpha-Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Norepinephrine,
http://linkedlifedata.com/resource/pubmed/chemical/Prazosin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, alpha,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Muscarinic,
http://linkedlifedata.com/resource/pubmed/chemical/Yohimbine
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0021-5198
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
47
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
229-35
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:2906098-Acetonitriles,
pubmed-meshheading:2906098-Adrenergic alpha-Antagonists,
pubmed-meshheading:2906098-Animals,
pubmed-meshheading:2906098-Dogs,
pubmed-meshheading:2906098-Electric Stimulation,
pubmed-meshheading:2906098-Female,
pubmed-meshheading:2906098-Male,
pubmed-meshheading:2906098-Mesenteric Arteries,
pubmed-meshheading:2906098-Norepinephrine,
pubmed-meshheading:2906098-Prazosin,
pubmed-meshheading:2906098-Rats,
pubmed-meshheading:2906098-Receptors, Adrenergic, alpha,
pubmed-meshheading:2906098-Receptors, Adrenergic, beta,
pubmed-meshheading:2906098-Receptors, Muscarinic,
pubmed-meshheading:2906098-Vas Deferens,
pubmed-meshheading:2906098-Yohimbine
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pubmed:year |
1988
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pubmed:articleTitle |
Pharmacological studies on the selectivity of HV-723, a new alpha-1 adrenoceptor antagonist.
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pubmed:affiliation |
Research Laboratories, Hokuriku Seiyaku Co., Ltd., Fukui, Japan.
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pubmed:publicationType |
Journal Article,
Comparative Study,
In Vitro
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