Pharmacology of GYKI-41 099 (Chlorpropanol, Tobanum®) a new potent beta-adrenergic antagonist

M. Fekete, I. Elekes, M. Kurti, J. Borvendeg

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

The compound GYKI-41 099, as a beta-adrenergic antagonist, is 3-8 times more potent than propranolol in vitro and in vivo. Its antiarrhythmic effectiveness surpasses that of propranolol and pindolol inhibiting the ouabain arrhythmia in dogs and cats. GYKI-41 099 has a negligible cardiodepressant activity; it is not cardioselective. The compound shows a rapid and long lasting effect. There was a prolonged elimination of the radioactivity after the injection of 14C-41 099 to rats and dogs. The half life of the unlabelled substance in humans was more than 10 hours.

Original languageEnglish
Pages (from-to)190-202
Number of pages13
JournalArchives Internationales de Pharmacodynamie et de Therapie
Volume248
Issue number2
Publication statusPublished - 1980

Fingerprint

Adrenergic beta-Antagonists
Adrenergic beta-3 Receptor Antagonists
Propranolol
Pharmacology
Dogs
Pindolol
Ouabain
Radioactivity
Half-Life
Cardiac Arrhythmias
Cats
Injections
tobanum
In Vitro Techniques

ASJC Scopus subject areas

  • Pharmacology

Cite this

Pharmacology of GYKI-41 099 (Chlorpropanol, Tobanum®) a new potent beta-adrenergic antagonist. / Fekete, M.; Elekes, I.; Kurti, M.; Borvendeg, J.

In: Archives Internationales de Pharmacodynamie et de Therapie, Vol. 248, No. 2, 1980, p. 190-202.

Research output: Contribution to journalArticle

@article{9bbfbe5ff41a45d88d39a9268b96f3aa,
title = "Pharmacology of GYKI-41 099 (Chlorpropanol, Tobanum{\circledR}) a new potent beta-adrenergic antagonist",
abstract = "The compound GYKI-41 099, as a beta-adrenergic antagonist, is 3-8 times more potent than propranolol in vitro and in vivo. Its antiarrhythmic effectiveness surpasses that of propranolol and pindolol inhibiting the ouabain arrhythmia in dogs and cats. GYKI-41 099 has a negligible cardiodepressant activity; it is not cardioselective. The compound shows a rapid and long lasting effect. There was a prolonged elimination of the radioactivity after the injection of 14C-41 099 to rats and dogs. The half life of the unlabelled substance in humans was more than 10 hours.",
author = "M. Fekete and I. Elekes and M. Kurti and J. Borvendeg",
year = "1980",
language = "English",
volume = "248",
pages = "190--202",
journal = "Archives Internationales de Pharmacodynamie et de Therapie",
issn = "0003-9780",
publisher = "Wiley-Blackwell",
number = "2",

}

TY - JOUR

T1 - Pharmacology of GYKI-41 099 (Chlorpropanol, Tobanum®) a new potent beta-adrenergic antagonist

AU - Fekete, M.

AU - Elekes, I.

AU - Kurti, M.

AU - Borvendeg, J.

PY - 1980

Y1 - 1980

N2 - The compound GYKI-41 099, as a beta-adrenergic antagonist, is 3-8 times more potent than propranolol in vitro and in vivo. Its antiarrhythmic effectiveness surpasses that of propranolol and pindolol inhibiting the ouabain arrhythmia in dogs and cats. GYKI-41 099 has a negligible cardiodepressant activity; it is not cardioselective. The compound shows a rapid and long lasting effect. There was a prolonged elimination of the radioactivity after the injection of 14C-41 099 to rats and dogs. The half life of the unlabelled substance in humans was more than 10 hours.

AB - The compound GYKI-41 099, as a beta-adrenergic antagonist, is 3-8 times more potent than propranolol in vitro and in vivo. Its antiarrhythmic effectiveness surpasses that of propranolol and pindolol inhibiting the ouabain arrhythmia in dogs and cats. GYKI-41 099 has a negligible cardiodepressant activity; it is not cardioselective. The compound shows a rapid and long lasting effect. There was a prolonged elimination of the radioactivity after the injection of 14C-41 099 to rats and dogs. The half life of the unlabelled substance in humans was more than 10 hours.

UR - http://www.scopus.com/inward/record.url?scp=0019256454&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0019256454&partnerID=8YFLogxK

M3 - Article

C2 - 6111982

AN - SCOPUS:0019256454

VL - 248

SP - 190

EP - 202

JO - Archives Internationales de Pharmacodynamie et de Therapie

JF - Archives Internationales de Pharmacodynamie et de Therapie

SN - 0003-9780

IS - 2

ER -