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In vivo experiments for the evaluation of alpha 1-adrenoceptor antagonistic effects of SGB-1534 on canine urethra.

作者信息

Imagawa J, Akima M, Sakai K

机构信息

Department of Pharmacology, Chugai Pharmaceutical Co., Ltd., Shizuoka, Japan.

出版信息

Eur J Pharmacol. 1989 Aug 11;167(1):167-72. doi: 10.1016/0014-2999(89)90759-0.

DOI:10.1016/0014-2999(89)90759-0
PMID:2570705
Abstract

The alpha 1-adrenoceptor blocking effects of SGB-1534 on the urethral smooth muscle were compared in in vivo lower urinary tract preparations of anesthetized dogs, with the effects of other alpha 1-adrenoceptor antagonists, prazosin and bunazosin. Hypogastric nerve stimulation and selective administration of phenylephrine to the urethra and bladder through the cannulated right external iliac artery (i.a.) elicited reproducible frequency- and dose-dependent increases in intra-urethral pressure. Intra-bladder pressure was increased by the nerve stimulation but not by i.a. phenylephrine. SGB-1534, prazosin or bunazosin (0.1-10 micrograms/kg i.v.) dose dependently suppressed the urethral contraction evoked by the nerve stimulation and i.a. phenylephrine but did not influence the bladder contraction elicited by nerve stimulation. The alpha 1-adrenoceptor blocking potency of SGB-1534 was approximately 2.3 and 8.1 times greater than that of prazosin and bunazosin, respectively. The results indicate that alpha 1-adrenoceptors may mediate mainly the urethral contraction induced by hypogastric nerve stimulation and i.a. phenylephrine, and that SGB-1534 was more potent alpha 1-adrenoceptor blocking activity than prazosin and bunazosin in the canine urethra.

摘要

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