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Titolo:
Isoeugenolol: A selective beta(1)-adrenergic antagonist with tracheal and vascular smooth muscle relaxant properties
Autore:
Lin, YT; Wu, BN; Horng, CF; Huang, YC; Hong, SJ; Lo, YC; Cheng, CJ; Chen, IJ;
Indirizzi:
Kaohsiung Med Coll, Dept Pharmacol, Kaohsiung 807, Taiwan Kaohsiung Med Coll Kaohsiung Taiwan 807 Pharmacol, Kaohsiung 807, Taiwan Kaohsiung Med Coll, Dept Cardiovasc Surg, Kaohsiung 807, Taiwan Kaohsiung Med Coll Kaohsiung Taiwan 807 vasc Surg, Kaohsiung 807, Taiwan
Titolo Testata:
JAPANESE JOURNAL OF PHARMACOLOGY
fascicolo: 2, volume: 80, anno: 1999,
pagine: 127 - 136
SICI:
0021-5198(199906)80:2<127:IASBAW>2.0.ZU;2-5
Fonte:
ISI
Lingua:
ENG
Soggetto:
BETA-ADRENOCEPTOR BLOCKER; RAT AORTA; BETA-3-ADRENERGIC RECEPTOR; PARTIAL BETA(2)-AGONIST; CALCIUM MOBILIZATION; ADRENERGIC-RECEPTOR; MOLECULAR-CLONING; VASORELAXANT; BINDING; HYPERTENSION;
Keywords:
isoeugenol; beta(1)-adrenoceptor antagonist; smooth muscle relaxation; interscapular brown adipose tissue; radioligand binding study;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
40
Recensione:
Indirizzi per estratti:
Indirizzo: Chen, IJ KaohsiungaiwanColl, Dept Pharmacol, 100 Shih Chuan 1st Rd, Kaohsiung 807, T Kaohsiung Med Coll 100 Shih Chuan 1st Rd Kaohsiung Taiwan 807 T
Citazione:
Y.T. Lin et al., "Isoeugenolol: A selective beta(1)-adrenergic antagonist with tracheal and vascular smooth muscle relaxant properties", JPN J PHARM, 80(2), 1999, pp. 127-136

Abstract

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 presser 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 pA(2) 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 beta(1)-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 mu M) and 5-HT (10 mu M) than those by high K+ (75 mM). In isolated guinea pig trachea, isoeugenolol attenuated the carbachol (1 mu M)-contracted trachea more significantly than those contracted with high Kf. Furthermore, the binding characteristics of isoeugenolol and various B-adrenoceptor antagonists were evaluated in [H-3]CGP-12177 binding to rat ventricle, lung and interscapular brown adipose tissue (IBAT) membranes. The -log IC50 values of isoeugenolol for predominate beta(1)-, beta(2)-and beta(3)-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 beta(1)-adrenoceptor antagonist with tracheal and vascular smooth muscle relaxant activities, but was devoid of alpha-adrenoceptor-blocking action.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/09/20 alle ore 16:18:52