Linked Life Data

10413061

Source:http://linkedlifedata.com/resource/pubmed/id/10413061

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
1999-10-14
pubmed:abstractText
Eugenodilol, derived from natural eugenol, was first investigated with in vivo and in vitro models. In our in vivo study, eugenodilol (0.5, 1.0, and 1.5 mg/kg, i.v.) produced dose-dependent hypotensive and bradycardic responses in pentobarbital-anesthetized Wistar rats. Eugenodilol also inhibited the tachycardia and arterial pressor effects induced by (-)isoproterenol and phenylephrine, respectively. In our in vitro study, eugenodilol competitively antagonized (-)isoproterenol-induced positive inotropic and chronotropic effects and tracheal-relaxation responses on isolated guinea pig tissues in a concentration-dependent manner. The apparent pA2 values were 7.88+/-0.12 for right atria, 7.52+/-0.05 for left atria, and 7.33+/-0.15 for trachea, indicating that eugenodilol was a nonselective beta-adrenoceptor blocker. In thoracic aorta experiments, the apparent pA2 values of alpha-adrenoceptor blockade were 7.05+/-0.25 and 6.87+/-0.08 for eugenodilol and labetalol, respectively. In addition, eugenodilol produced cumulative relaxation responses on isolated guinea pig tracheal strips. The effects were competitively antagonized by ICI 118,551 (10(-8)-10(-6) M), a relatively selective beta2-adrenoceptor antagonist. In the radioligand-binding assay, the Ki values of [3H]CGP-12177 binding to rat ventricle and lung membranes were 9.72 and 48.29 nM, respectively, and the value of [3H]prazosin binding to rat brain membrane was 38.72 nM. These results further confirmed the alpha/beta-adrenoceptors-blocking activities of eugenodilol reported in the functional studies. We conclude that eugenodilol is a novel third-generation beta-adrenoceptor blocker with ancillary blocking activity at alpha-adrenoceptors and weak sympathomimetic activity at beta2-adrenoceptors.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
0160-2446
pubmed:author
pubmed:issnType
Print
pubmed:volume
34
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
10-20
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed-meshheading:10413061-Adrenergic beta-Agonists, pubmed-meshheading:10413061-Adrenergic beta-Antagonists, pubmed-meshheading:10413061-Anesthesia, pubmed-meshheading:10413061-Animals, pubmed-meshheading:10413061-Aorta, Thoracic, pubmed-meshheading:10413061-Bradycardia, pubmed-meshheading:10413061-Dose-Response Relationship, Drug, pubmed-meshheading:10413061-Drug Interactions, pubmed-meshheading:10413061-Eugenol, pubmed-meshheading:10413061-Female, pubmed-meshheading:10413061-Guinea Pigs, pubmed-meshheading:10413061-Hypotension, pubmed-meshheading:10413061-Isoproterenol, pubmed-meshheading:10413061-Labetalol, pubmed-meshheading:10413061-Male, pubmed-meshheading:10413061-Muscle Contraction, pubmed-meshheading:10413061-Phenylephrine, pubmed-meshheading:10413061-Radioligand Assay, pubmed-meshheading:10413061-Rats, pubmed-meshheading:10413061-Rats, Wistar, pubmed-meshheading:10413061-Time Factors, pubmed-meshheading:10413061-Trachea, pubmed-meshheading:10413061-Vasodilator Agents
pubmed:year
1999
pubmed:articleTitle
Eugenodilol: a third-generation beta-adrenoceptor blocker, derived from eugenol, with alpha-adrenoceptor blocking and beta2-adrenoceptor agonist-associated vasorelaxant activities.
pubmed:affiliation
Department of Pharmacology, Kaohsiung Medical College, Taiwan, Republic of China.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't