Literature DB >> 5809739

Anti-arrhythmic, local anaesthetic, and adrenergic blocking activity of some beta-receptor antagonists.

K Hermansen.   

Abstract

1. The antagonistic effect of the beta-receptor blocking compounds propranolol, Ph QA 33 and INPEA on ouabain-induced cardiac fibrillations in guinea-pigs was compared with their local anaesthetic and beta-receptor blocking properties.2. All three compounds were found capable of increasing the tolerance to ouabain and of reversing ouabain-induced fibrillations, the ED50 being 0.3 mg/kg intravenously, 0.5 mg/kg intravenously, and 1.5 mg/kg intravenously, respectively for propranolol, Ph QA 33 and INPEA.3. Propranolol and Ph QA 33 were found to be moderate to strong local anaesthetics while INPEA had a considerably weaker though significant effect.4. The order of potency as beta-receptor blocking compounds was propranolol >/= Ph QA 33 >> INPEA, the latter compound being less than 1% as active as propranolol.5. Despite the surprising finding that INPEA was effective against non-catecholamine-induced arrhythmias, the results support the general assumption that the anti-arrhythmic effect of beta-receptor blocking compounds is related to their local anaesthetic action rather than to their beta-blocking ability.

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Year:  1969        PMID: 5809739      PMCID: PMC1703362          DOI: 10.1111/j.1476-5381.1969.tb08289.x

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN: 0007-1188            Impact factor:   8.739


  14 in total

1.  [Problem of standardization tests for local anesthetics].

Authors:  F HERR
Journal:  Arzneimittelforschung       Date:  1958-03

2.  A simple new quantitative method for testing local anaesthetics.

Authors:  C BIANCHI
Journal:  Br J Pharmacol Chemother       Date:  1956-06

3.  Blockade of epinephrine- and ouabain-induced cardiac arrhythmias in the dog heart-lung preparation.

Authors:  P Somani; B K Lum
Journal:  J Pharmacol Exp Ther       Date:  1966-05       Impact factor: 4.030

4.  The antiarrhythmic properties of ICI 46037, a quaternary analog of propranolol.

Authors:  B R Lucchesi; T Iwami
Journal:  J Pharmacol Exp Ther       Date:  1968-07       Impact factor: 4.030

5.  Control of ventricular fibrillation during induced hypothermia in cats after blocking the adrenergic neurons with bretylium.

Authors:  K C Nielsen; C Owman
Journal:  Life Sci       Date:  1968-02-01       Impact factor: 5.037

Review 6.  Mode of action of beta receptor antagonists on cardiac muscle.

Authors:  E M Williams
Journal:  Am J Cardiol       Date:  1966-09       Impact factor: 2.778

7.  Antiarrhythmic effects of beta adrenergic blocking agents.

Authors:  B R Lucchesi; L S Whitsitt; J L Stickney
Journal:  Ann N Y Acad Sci       Date:  1967-02-10       Impact factor: 5.691

8.  Pharmacological properties of 1-(4'-nitrophenyl)-2-isopropylamino-ethanol (INPEA), a new beta-adrenergic receptor antagonist. II. Studies of local anesthetic activity.

Authors:  W Murmann; M Saccani-Guelfi; A Gamba
Journal:  Boll Chim Farm       Date:  1966-04

9.  Optical isomers of propranolol.

Authors:  R Howe; R G Shanks
Journal:  Nature       Date:  1966-06-25       Impact factor: 49.962

10.  Some pharmacological properties of a new beta-adrenergic blocking agent, 1-(isopropylamino)-3-(o-phenoxyphenoxy)-2-propanol, HCl (Ph QA 33).

Authors:  K Hermansen
Journal:  Acta Pharmacol Toxicol (Copenh)       Date:  1968
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  2 in total

1.  Measurement of hydrophobicity, surface activity, local anaesthesia, and myocardial conduction velocity as quantitative parameters of the non-specific membrane affinity of nine -adrenergic blocking agents.

Authors:  D Hellenbrecht; B Lemmer; G Wiethold; H Grobecker
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1973       Impact factor: 3.000

2.  The effects of (+)- and (-)-propranolol on 3H-transmitter efflux in guinea-pig atria and the presynaptic beta-adrenoceptor hypothesis.

Authors:  S Kalsner
Journal:  Br J Pharmacol       Date:  1980-11       Impact factor: 8.739

  2 in total

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