Recent Advances in Selective alpha1-adrenoreceptor Antagonists as Antihypertensive Agents

Bioorg Med Chem. 2008 May 1;16(9):4759-800. doi: 10.1016/j.bmc.2008.02.091. Epub 2008 Mar 4.


Hypertension is one of the most serious health problems of the modern world with a continuous rise in the number of patients. Selective alpha(1)-adrenoreceptor antagonists though have many advantages and uses in the management of arterial hypertension, their lack of specificity at the level of alpha(1)-adr subtypes leads to multiple side effects. Existence of multiple alpha(1)-adr subtypes holds great promise for the discovery and development of more specific and selective drug molecules, targeting only one alpha(1)-adr subtype at a time and thus relative freedom from side effects. Herein, the research done on the discovery and evaluation of a variety of chemically diverse structures as selective antagonists of alpha(1)-adr and alpha(1)-adr subtypes in recent years has been reviewed.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Adrenergic alpha-1 Receptor Antagonists*
  • Adrenergic alpha-Antagonists / chemistry
  • Adrenergic alpha-Antagonists / pharmacology
  • Adrenergic alpha-Antagonists / therapeutic use*
  • Animals
  • Antihypertensive Agents / chemistry
  • Antihypertensive Agents / pharmacology
  • Antihypertensive Agents / therapeutic use*
  • Humans
  • Hypertension / drug therapy*
  • Molecular Structure
  • Receptors, Adrenergic, alpha-1 / classification
  • Risk Factors
  • Stereoisomerism
  • Structure-Activity Relationship


  • Adrenergic alpha-1 Receptor Antagonists
  • Adrenergic alpha-Antagonists
  • Antihypertensive Agents
  • Receptors, Adrenergic, alpha-1