PMID: 702319Sep 1, 1978Paper

Studies on bitolterol, di-p-toluate ester of N-tert.-butylarterenol: a new long-acting bronchodilator with reduced cardiovascular effects

The Journal of Pharmacology and Experimental Therapeutics
H Minatoya

Abstract

The bronchodilator activity of bitolterol, the di-p-toluate ester of N-tert.-butylarterenol (N-t-B) was evaluated by comparing it with the activity of the parent compound (N-t-B), isoproterenol and in some experiments with salbutamol in the anesthetized, open-chest dog maintained under artificial respiration. Bronchodilation was expressed as percent inhibition of the control bronchoconstriction induced by intravenous carbachol or histamine. At equiactive intravenous bronchodilator doses, the duration of action of bitolterol was 10 times that of N-t-B or isoproterenol. In the cardiovascular studies in anesthetized dogs, chronotropic, inotropic and blood pressure effects of bitolterol were markedly reduced relative to its bronchodilator effect. The bronchodilator/heart rate ratio for bitolterol was 22 times that of isoproterenol and 6 times that of N-t-B or salbutamol suggesting greater selectivity for beta2 adrenoreceptors for bitolterol. A good intraduodenal bronchodilator activity with a prolonged duration of action was obtained with bitolterol when compared with N-t-B and isoproterenol. The intraduodenal/intravenous bronchodilator dose ratio for bitolterol was 2 compared with 240 and 960 for N-t-B and isoproterenol, respectiv...Continue Reading

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