PMID: 6116195Feb 1, 1981

Duration and selectivity in beta-adrenoceptor blocking action of a beta-adrenoceptor blocking drug, D-32 in conscious dogs

Naunyn-Schmiedeberg's Archives of Pharmacology
N HimoriT Ishimori

Abstract

In conscious dogs, the selectivity and duration of beta-blocking activity, and serum concentration of a beta-blocking agent, D-32 [dl-1-tert-butylamino-3-(2,3-dimethylphenoxy)-2-propanol hydrochloride] was compared to that of propranolol, pindolol, atenolol and IPS-339 [dl-1-tert-butylamino-3-(-9-fluorenylideneaminoxy)-2-propanol hydrochloride]. Ratios of doses causing a 50% inhibition of tachycardia to that on hypotension induced by isoprenaline were as follows: D-32 (0.69), propranolol (0.67), atenolol (0.03) and IPS-339 (6.3). Thus, present experiments indicate that, unlike atenolol and IPS-339, D-32, propranolol and pindolol are non-selective beta-adrenoceptor blocking agents. Atenolol and IPS-339, however, selectively blocked cardiac beta1, receptors and vascular beta2-receptors respectively, as would be expected. In an optimal dose range these two drugs can be used satisfactorily as a pharmacological tool for inhibiting responses mediated via the respective beta-receptors. After oral administration, the pharmacological half-life (time required for 50% recovery of beta-blocking action) was 15.8 +/- 4.5 h for propranolol (3 mg/kg), 21.8 +/- 6.4 h for D-32 (0.5 mg/kg), 30.5 +/- 3.1 h for atenolol (6 mg/kg) and 30-35 h for pi...Continue Reading

References

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Related Concepts

Xibenolol, (+-)-isomer
IPS 339, monohydrochloride, (+-)-isomer
Adrenergic beta-Antagonists
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Rexigen
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