L-BUNOLOL AND PROPRANOLOL - ORAL AND INTRAVENOUS BETA-ADRENOCEPTOR BLOCKING ACTIVITY IN RATS COMPARED TO DOGS AND HUMANS

被引：1

作者：

KAPLAN, HR ^{[1
]}

COMMARATO, MA ^{[1
]}

LATTIME, EC ^{[1
]}

机构：

[1] WARNER LAMBERT RES INST,DEPT PHARMACOL,MORRIS PLAINS,NJ 07950

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 1978年 / 67卷 / 01期

关键词：

Antiadrenergic agents—l‐bunolol β‐adrenoceptor blocking activity compared in dogs; rats; and humans; oral and intravenous dosage; l‐Bunolol—β‐adrenoceptor blocking activity compared in dogs; Propranolol—β‐adrenoceptor blocking activity compared in dogs and rats; β‐Adrenoceptor blocking activity—l‐bunolol and propranolol compared in dogs;

D O I：

10.1002/jps.2600670139

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Abstract To determine the pharmacological significance of reported differences between species in l‐bunolol metabolism, oral and intravenous β‐adrenoceptor bloiking activity against an isoproterenol‐induced tachycardia was compared in dogs, rats, and humans. Propranolol was similarly studied in rats and dogs. Species differences in intravenous potency were minimal for both compounds in contrast to oral dose studies. Oral to intravenous ratios of doses causing a comparable degree of β‐adrenoceptor blockade after l‐bunolol were: rat, 212; dog, 4; and human, 5. For propranolol, the oral to intravenous dose ratios were 210 and 32 for the rat and dog, respectively. These pharmacological findings show major differences in the rat compared to dogs and humans and may be explained in part by differences in the urinary excretion patterns of l‐bunolol in the various species. Copyright © 1978 Wiley‐Liss, Inc., A Wiley Company

引用

页码：132 / 133

页数：2

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