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Titolo:
Eugenodilol: A third-generation beta-adrenoceptor blocker, derived from eugenol, with alpha-adrenoceptor blocking and beta(2)-adrenoceptor agonist-associated vasorelaxant activities
Autore:
Huang, YC; Wu, BN; Lin, YT; Chen, SJ; Chiu, CC; 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 Foo Yin Inst Technol, Kaohsiung, Taiwan Foo Yin Inst Technol Kaohsiung Taiwan n Inst Technol, Kaohsiung, Taiwan
Titolo Testata:
JOURNAL OF CARDIOVASCULAR PHARMACOLOGY
fascicolo: 1, volume: 34, anno: 1999,
pagine: 10 - 20
SICI:
0160-2446(199907)34:1<10:EATBBD>2.0.ZU;2-Z
Fonte:
ISI
Lingua:
ENG
Soggetto:
SMOOTH-MUSCLE; HEART-FAILURE; PARTIAL BETA(2)-AGONIST; RABBIT AORTA; BETA-2-ADRENOCEPTOR; RAT; BETA(1)-ADRENOCEPTOR; ANTAGONIST; CARVEDILOL; PINDOLOL;
Keywords:
adrenoceptors; eugenodilol; vasorelaxant;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
39
Recensione:
Indirizzi per estratti:
Indirizzo: Chen, IJ Kaohsiung Med Coll, Dept Pharmacol, 100 Shih-Chuan 1st Rd, Kaohsiung 807, Taiwan Kaohsiung Med Coll 100 Shih-Chuan 1st Rd Kaohsiung Taiwan 807 an
Citazione:
Y.C. Huang et al., "Eugenodilol: A third-generation beta-adrenoceptor blocker, derived from eugenol, with alpha-adrenoceptor blocking and beta(2)-adrenoceptor agonist-associated vasorelaxant activities", J CARDIO PH, 34(1), 1999, pp. 10-20

Abstract

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 andphenylephrine, 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 pA(2) 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 pA(2) 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 werecompetitively antagonized by ICI 118,551 (10(-8)-10(-6) M), a relatively selective beta(2)-adrenoceptor antagonist. Zn the radioligand-binding assay,the K-i values of [H-3]CGP-12177 binding to rat ventricle and lung membranes were 9.72 and 48.29 nM, respectively, and the value of [H-3]prazosin binding to rat brain membrane was 38.72 nM. These results further confirmed the alpha/beta-odronoceptors-blocking activities of eugenodilol reported in the functional studies. We conclude that eugenodilol is a novel third-generation P-adrenoceptor blocker with ancillary blocking activity at alpha-adrenoceptors and weak sympathomimetic activity at beta(2)-adrenoceptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/09/20 alle ore 11:48:54