[Alpha1-adrenoceptor subtypes and alpha1-adrenoceptor antagonists]

Yakugaku Zasshi. 2006 Mar:126 Spec no.:187-98. doi: 10.1248/yakushi.126.187.
[Article in Japanese]

Abstract

Alpha(1)-adrenoceptors are widely distributed in the human body and play important physiologic roles. Three alpha(1)-adrenoceptor subtypes (alpha(1A), alpha(1B) and alpha(1D)) have been cloned and show different pharmacologic profiles. In addition, a putative alpha(1)-adrenoceptor (alpha(1L) subtype) has also been proposed. Recently, three drugs (tamsulosin, naftopidil, and silodosin) have been developed in Japan for the treatment of urinary obstruction in patients with benign prostatic hyperplasia. In this review, we describe recent alpha(1)-adrenoceptor subclassifications and the pharmacologic characteristics (subtype selectivity and clinical relevance) of alpha(1)-adrenoceptor antagonists.

Publication types

  • Review

MeSH terms

  • Adrenergic alpha-1 Receptor Antagonists
  • Adrenergic alpha-Antagonists* / adverse effects
  • Adrenergic alpha-Antagonists* / pharmacology
  • Adrenergic alpha-Antagonists* / therapeutic use
  • Amino Acid Sequence
  • Animals
  • Cloning, Molecular
  • Drug Design
  • Drug Tolerance
  • Humans
  • Male
  • Molecular Sequence Data
  • Naphthalenes
  • Piperazines
  • Prostatic Hyperplasia / complications
  • Prostatic Hyperplasia / drug therapy
  • Receptors, Adrenergic, alpha-1 / chemistry
  • Receptors, Adrenergic, alpha-1 / classification*
  • Receptors, Adrenergic, alpha-1 / physiology
  • Sulfonamides
  • Tamsulosin
  • Urethral Obstruction / drug therapy
  • Urethral Obstruction / etiology

Substances

  • Adrenergic alpha-1 Receptor Antagonists
  • Adrenergic alpha-Antagonists
  • Naphthalenes
  • Piperazines
  • Receptors, Adrenergic, alpha-1
  • Sulfonamides
  • Tamsulosin
  • naftopidil