Recent advances in the discovery of alpha1-adrenoceptor agonists

Curr Top Med Chem. 2007;7(2):135-45. doi: 10.2174/156802607779318217.

Abstract

The alpha(1) adrenoceptors are three of nine well-characterized receptors that are activated by epinephrine and norepinephrine. Agonists acting at the alpha(1) adrenoceptors produce numerous physiological effects, and are used therapeutically for several indications. Many known alpha(1) adrenoceptor agonists are alpha(1A) selective, but the discovery of highly selective alpha(1B) and alpha(1D) adrenoceptor agonists has proven to be an extremely difficult goal to achieve. This review will focus on recent advances in the discovery, development and clinical utility of subtype-specific alpha(1) agonists as well as contributions to our understanding of agonist-receptor interactions.

Publication types

  • Review

MeSH terms

  • Adrenergic alpha-1 Receptor Agonists*
  • Adrenergic alpha-Agonists / chemistry
  • Adrenergic alpha-Agonists / metabolism
  • Adrenergic alpha-Agonists / pharmacology*
  • Animals
  • Humans
  • Receptors, Adrenergic, alpha-1 / chemistry
  • Receptors, Adrenergic, alpha-1 / metabolism
  • Structure-Activity Relationship
  • Substrate Specificity

Substances

  • Adrenergic alpha-1 Receptor Agonists
  • Adrenergic alpha-Agonists
  • Receptors, Adrenergic, alpha-1