Eugenodilol: a third-generation beta-adrenoceptor blocker, derived from eugenol, with alpha-adrenoceptor blocking and beta2-adrenoceptor agonist-associated vasorelaxant activities

Journal of Cardiovascular Pharmacology
Y C HuangI J Chen

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 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-bi...Continue Reading

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Citations

Sep 1, 2006·Indian Journal of Clinical Biochemistry : IJCB·Rashmi ChoudharyC Subramanyam
Dec 14, 2011·Psychopharmacology·Chin-Wei HuangSheng-Nan Wu
Mar 21, 2003·Vascular Pharmacology·Carlos Estevam Nolf DamianiDalton Valentim Vassallo
Jan 4, 2005·Pharmacology·K NandakumarS H Bhardwaj
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May 22, 2002·Journal of Cardiovascular Pharmacology·Jwu-Lai YehIng-Jun Chen
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Related Concepts

Eugenodilol
Adrenergic beta-Agonists
Adrenergic beta-Antagonists
Anesthesia Procedures
Metazoa
Descending Aorta
Bradycardia
Dose-Response Relationship, Drug
Drug Interactions
Eugenol

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