The alpha- and beta-adrenoceptor blocking potencies of labetalol and its individual stereoisomers in anaesthetized dogs and in isolated tissues

British Journal of Pharmacology
R T BrittainG P Levy


1 The antagonist potencies of labetalol and each of its four stereoisomers have been compared at alpha 1-, beta 1- and beta 2-adrenoceptors in anaesthetized dogs and in isolated tissues. 2 The RR stereoisomer is a potent, non-selective antagonist at beta-adrenoceptors but has only weak alpha 1-adrenoceptor blocking activity. 3 The SR stereoisomer was the most potent antagonist at alpha 1-adrenoceptors, and it also had similar potency as an antagonist at beta-adrenoceptors. 4 The alpha- and beta-adrenoceptor blocking profile of the RS stereoisomer is intermediate between that of the RR and SR, but the SS stereoisomer is a relatively weak antagonist at both alpha- and beta-adrenoceptors. 5 It is concluded that, although most of the alpha 1-adrenoceptor blocking activity of labetalol is attributable to the SR stereoisomer and nearly all of its beta-adrenoceptor blocking activity resides in the RR stereoisomer, each of the stereoisomers contributes to the overall pharmacological profile of labetalol.


Nov 3, 1975·Naunyn-Schmiedeberg's Archives of Pharmacology·K StarkeH D Taube
Apr 1, 1977·British Journal of Pharmacology·A G Blakeley, R J Summers
Aug 1, 1978·British Journal of Pharmacology·P P Humphrey
Oct 1, 1976·British Journal of Pharmacology·E ApperleyG P Levy
May 1, 1973·The American Journal of Physiology·R F Coburn, T Tomita
Nov 1, 1973·European Journal of Pharmacology·M F LokhandwalaB S Jandhyala
Feb 10, 1967·Annals of the New York Academy of Sciences·R F Furchgott
Oct 1, 1980·Japanese Journal of Pharmacology·Y NakagawaS Imai
Mar 1, 1981·Journal of Cardiovascular Pharmacology·R C DageJ K Woodward
Sep 5, 1980·European Journal of Pharmacology·J W ConstantineR A Weeks
Aug 1, 1981·Naunyn-Schmiedeberg's Archives of Pharmacology·J R DochertyK Starke
Mar 1, 1959·British Journal of Pharmacology and Chemotherapy·O ARUNLAKSHANA, H O SCHILD
Sep 1, 1949·British Journal of Pharmacology and Chemotherapy·H O SCHILD


Dec 1, 1989·Journal of Clinical Pharmacology·J D Wallin, W H Frishman
Jan 1, 1991·Cardiovascular Drugs and Therapy·W J LouisL H Tung
Jan 1, 1990·European Journal of Clinical Pharmacology·W KrauseN Sauerbrey
Mar 1, 1983·Naunyn-Schmiedeberg's Archives of Pharmacology·R R RuffoloE L Yaden
Jan 1, 1984·European Journal of Clinical Pharmacology·E J Ariëns
Dec 1, 1990·Cardiovascular Drugs and Therapy·M O den BoerP D Verdouw
Oct 1, 1984·Irish Journal of Medical Science·E G BreenJ A Keogh
Jan 1, 1995·European Journal of Drug Metabolism and Pharmacokinetics·G Pifferi, E Perucca
Dec 4, 2013·Clinical Pharmacokinetics·James H FischerKeith A Rodvold
Dec 4, 2003·Pharmacology & Therapeutics·Noboru Toda
Jun 1, 1988·Clinical and Experimental Pharmacology & Physiology·G AnfossiG Emanuelli
Aug 1, 1990·British Journal of Pharmacology·G KrumplG Raberger
Jan 1, 1989·Clinical and Experimental Hypertension. Part A, Theory and Practice·W J LouisL G Howes
Jun 6, 2006·Journal of Cardiothoracic and Vascular Anesthesia·Simon LewisJas Soar
Nov 25, 2003·Pharmacology & Toxicology·Bertil Waldeck
Jul 1, 1984·Medicinal Research Reviews·M Simonyi
Apr 1, 1988·Medicinal Research Reviews·E J Ariëns
Dec 12, 2007·Chirality·Carsten D SiebertThomas Nagel
Jan 1, 1983·Acta Medica Scandinavica·M Lilja
Sep 22, 2012·British Journal of Clinical Pharmacology·Clive Page, Patrick Humphrey
Feb 1, 1995·The Annals of Pharmacotherapy·T S Tracy
Jan 1, 1985·European Journal of Clinical Pharmacology·R L Smith
Jul 28, 2020·BMC Veterinary Research·Francesco ZublenaFederico Corletto
Aug 6, 1999·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·C BelloliG Re

Related Concepts

Adrenergic alpha-Antagonists
Adrenergic beta-Antagonists
Anesthesia Procedures
Descending Aorta
Canis familiaris
Cavia porcellus

Related Feeds

Adrenergic Receptors: Trafficking

Adrenergic receptor trafficking is an active physiological process where adrenergic receptors are relocated from one region of the cell to another or from one type of cell to another. Discover the latest research on adrenergic receptor trafficking here.