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α1肾上腺素能受体阻断在男性下尿路及其他身体系统中的作用

Alpha1 adrenergic receptor blockade in the male lower urinary tract and other body systems.

作者信息

Andersson K E

机构信息

Department of Clinical Pharmacology, University Hospital of Lund, Sweden.

出版信息

Scand J Urol Nephrol Suppl. 1995;168:13-9.

PMID:7541547
Abstract

Recent developments in pharmacology and molecular cloning techniques have led to an increased interest in the therapeutic potential of drugs which act via alpha adrenoceptors. Of particular interest are the alpha 1 adrenoceptors. Pharmacologically, two subtypes of the alpha 1 adrenoceptor have been characterised, namely alpha 1A and alpha 1B. Three subtypes with high affinity for selective alpha 1 adrenoceptor antagonists have also been cloned, that is the alpha 1b, alpha 1c and alpha 1a/d subtypes. Selective alpha 1 adrenoceptor antagonists have become an accepted treatment alternative in the management of both benign prostatic hyperplasia and hypertension, based on their ability to inhibit alpha 1 adrenoceptors of the lower urinary tract and cardiovascular system. Central actions may also be apparent. While cloned receptors of the prostatic stroma seem to be of the alpha 1c subtype, none of the adrenoceptor antagonists available today is subtype selective. This paper will discuss the characterization and localization of the different alpha 1 adrenoceptors and the therapeutic implications of inhibition.

摘要

药理学和分子克隆技术的最新进展引发了人们对通过α肾上腺素能受体起作用的药物治疗潜力的更多关注。其中,α1肾上腺素能受体尤其受到关注。在药理学上,已鉴定出α1肾上腺素能受体的两种亚型,即α1A和α1B。还克隆出了对选择性α1肾上腺素能受体拮抗剂具有高亲和力的三种亚型,即α1b、α1c和α1a/d亚型。基于其抑制下尿路和心血管系统α1肾上腺素能受体的能力,选择性α1肾上腺素能受体拮抗剂已成为治疗良性前列腺增生和高血压的一种公认的替代疗法。其对中枢的作用也可能很明显。虽然前列腺基质的克隆受体似乎属于α1c亚型,但目前可用的肾上腺素能受体拮抗剂均无亚型选择性。本文将讨论不同α1肾上腺素能受体的特性和定位以及抑制作用的治疗意义。

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