Linked Life Data

10440531

Source:http://linkedlifedata.com/resource/pubmed/id/10440531

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1999-10-28
pubmed:abstractText
Isoeugenolol (1.0, 3.0, 5.0 mg/kg, i.v.) produced a dose-dependent bradycardia and a decrease in blood pressure in anesthetized Wistar rats. Isoeugenolol inhibited the tachycardia effects induced by (-)isoproterenol, but had no blocking effect on the arterial pressor responses induced by (-)phenylephrine. In isolated guinea pig tissues, isoeugenolol antagonized (-)isoproterenol-induced positive inotropic and chronotropic effects on the atria and tracheal relaxations in a concentration-dependent manner. The apparent pA2 values for isoeugenolol on right atria, left atria and trachea were 7.63+/-0.03, 7.89+/-0.12 and 6.12+/-0.05, respectively, indicating that isoeugenolol was a highly selective beta1-adrenoceptor blocker. On the other hand, isoeugenolol produced a mild direct cardiac depression at high concentration and was without intrinsic sympathomimetic activity (ISA). In isolated rat thoracic aorta, isoeugenolol relaxed more potently the contractions induced by (-)phenylephrine (10 microM) and 5-HT (10 microM) than those by high K+ (75 mM). In isolated guinea pig trachea, isoeugenolol attenuated the carbachol (1 microM)-con-tracted trachea more significantly than those contracted with high K+. Furthermore, the binding characteristics of isoeugenolol and various beta-adrenoceptor antagonists were evaluated in [3H]CGP-12177 binding to rat ventricle, lung and interscapular brown adipose tissue (IBAT) membranes. The -log IC50 values of isoeugenolol for predominate beta1-, beta2- and beta3-adrenergic receptor sites were 5.82+/-0.09, 4.74+/-0.05 and 4.73+/-0.12, respectively. In conclusion, isoeugenolol was found to be a highly selective beta1-adrenoceptor antagonist with tracheal and vascular smooth muscle relaxant activities, but was devoid of alpha-adrenoceptor-blocking action.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0021-5198
pubmed:author
pubmed:issnType
Print
pubmed:volume
80
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
127-36
pubmed:dateRevised
2010-11-18
pubmed:meshHeading
pubmed-meshheading:10440531-Adrenergic beta-1 Receptor Antagonists, pubmed-meshheading:10440531-Adrenergic beta-2 Receptor Antagonists, pubmed-meshheading:10440531-Adrenergic beta-Antagonists, pubmed-meshheading:10440531-Animals, pubmed-meshheading:10440531-Blood Pressure, pubmed-meshheading:10440531-Carbachol, pubmed-meshheading:10440531-Dose-Response Relationship, Drug, pubmed-meshheading:10440531-Eugenol, pubmed-meshheading:10440531-Guinea Pigs, pubmed-meshheading:10440531-Heart Rate, pubmed-meshheading:10440531-Male, pubmed-meshheading:10440531-Muscle, Smooth, Vascular, pubmed-meshheading:10440531-Muscle Contraction, pubmed-meshheading:10440531-Muscle Relaxation, pubmed-meshheading:10440531-Potassium Chloride, pubmed-meshheading:10440531-Radioligand Assay, pubmed-meshheading:10440531-Rats, pubmed-meshheading:10440531-Rats, Wistar, pubmed-meshheading:10440531-Trachea
pubmed:year
1999
pubmed:articleTitle
Isoeugenolol: a selective beta1-adrenergic antagonist with tracheal and vascular smooth muscle relaxant properties.
pubmed:affiliation
Department of Cardiovascular Surgery, Kaohsiung Medical College, Taiwan.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't