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B Basil

Publications and source records attributed to B Basil.

9 recordsLinked to original sources
PubMed1982

Pharmacological properties of diacetolol (M & B 16,942), a major metabolite of acebutolol.

Diacetolol (M & B 16,942), the major metabolite of the beta-adrenoceptor blocking agent, has been compared pharmacologically with acebutolol. In vitro, the beta-adrenoceptor blocking potency of diacetolol was less than that of acebutolol but its cardioselectivity (atrial relative to tracheal tissue) was greater. In the anaesthetized cat both agents had closely similar beta-adrenoceptor blocking potency and cardioselectivity. Diacetolol had weak intrinsic sympathomimetic activity (ISA), and no significant membrane-stabilizing activity (MSA). It did not restore sinus rhythm to anaesthetized dogs with ouabain-induced arrhythmias but was similar to acebutolol in preventing arrhythmia induced by adrenaline/methylchloroform in anaesthetized cats. It is concluded that, in experimental animals, diacetolol has beta-adrenoceptor blocking properties and ISA similar to the parent compound but differs in its lack of MSA.

Acebutolol↗
PubMed1976

A new series of cardioselective adrenergic beta-receptor blocking compounds. 1-(2-Acyl-4-acylaminophenoxy)-3-isopropylaminopropan-2-ols.

A series of 1-(2-acyl-4-acylaminophenoxy)-3-isopropylaminopropan-2-ols has been synthesized and examined for beta-receptor blocking and antiarrhythmic activity. Several of these compounds are more than 20 times as active in blocking cardiac beta-receptors than vascular beta-receptors when given intravenously to anesthetized cats. The activities have been correlated quantitatively with partition and steric substitution constants. The observed relationships are consistent with a tentative proposal that the vascular receptor is situated in a more lipophilic environment than the cardiac receptor so that there is a differential transport effect between the two types of receptor.

Adrenergic beta-Antagonists↗
PubMed1975

[Pharmacology of acebutolol in animals].

In the course of routine screening of beta-adrenoceptor blocking compounds, it was found that a number of compounds did not block the vascular and cardiac effects of isoprenaline in proportion. Moreover, it was also found that the anti-arrhythmic action was not wholly related to the beta-adrenoceptor blocking potency. In particular, the anti-ouabain arrhythmia properties were not dependent upon beta-blocking potency. It was, therefore, possible to select a compound which had both cardioselective beta-adrenoceptor blocking and anti-ouabain arrhythmic activities. The chosen compound was acebutolol. Acebutolol is a cardioselective beta-adrenoceptor blocking agent which has marked anti-arrhythmic against arrhythmia induced by methylchloroform and adrenalin in the cat, and also arrhythmia induced by ouabain in dogs and rabbits. It has less pronounced membrane stabilising properties than propranolol and has no demonstrable sympathomimetic action in normal anaesthetised cats or dogs. Bronchial beta-adrenoceptor blockade has been investigated in anaesthetised cats in which bronchoconstriction is evoked by PGF2 alpha. Isoprenaline prevents the effect of PGF2 alpha and this is restored by pre-treatment with propranolol. Acebutolol is 100 times less active than propranolol in these experiments.

Acebutolol↗
PubMed1974

A comparison of the experimental anti-arrhythmic properties of acebutolol (M and B 17,803), propranolol and practolol.

1 The beta-adrenoceptor blocking agent, acebutolol (M & B 17,803), has been compared with propranolol, practolol, lignocaine and quinidine for its ability to revert or prevent various types of experimental arrhythmias.2 By intravenous infusion, acebutolol had one half the potency of propranolol in reverting an established ouabain-induced ventricular arrhythmia in the anaesthetized dog. Practolol was ineffective in the conditions used.3 High oral doses of acebutolol or propranolol significantly increased the arrhythmic dose of ouabain in the conscious rabbit. Similar doses of practolol produced a significant decrease (i.e. potentiation) in the dose of ouabain required to produce arrhythmia. Lignocaine and quinidine showed no or little activity in this test.4 Propranolol, acebutolol and practolol were all effective in decreasing the frequency of ectopic beats induced by adrenaline and methylchloroform in the anaesthetized cat. Lignocaine and quinidine were only weakly effective.5 Acebutolol and propranolol were equally effective either intravenously or orally in reducing the incidence of ventricular fibrillation produced by chloroform in mice.6 It is suggested that the wide spectrum of experimental anti-arrhythmic activity of acebutolol coupled with its cardioselectivity may make it an interesting compound in the treatment of cardiac arrhythmias in man.

Administration, Oral↗
PubMed1973

Beta-adrenoceptor blocking properties and cardioselectivity of M & B 17,803A.

1. The beta-adrenoceptor blocking properties of (+/-)-1-(2-acetyl-4-n-butyramidophenoxy)-2-hydroxy-3-isopropylaminopropane hydrochloride (M&B 17,803A) have been compared with those of practolol and propranolol in the guinea-pig, cat and dog.2. Following either intravenous or oral administration in the cat or dog, M&B 17,803A and practolol had similar potency in antagonizing isoprenaline-induced tachycardia and both showed cardioselectivity, but both were less potent than propranolol.3. M&B 17,803A and practolol had approximately one hundredth the intravenous potency of propranolol in increasing the severity of anaphylactic bronchospasm in the conscious sensitized guinea-pig.4. M&B 17,803A possessed less marked intrinsic sympathomimetic activity than practolol but, like propranolol, it had significant local anaesthetic properties and increased the refractory period of rabbit isolated atria.

Acetanilides↗