Stereochemical facets of clinical β-blockers: An overview

Chirality. 2020 May;32(5):722-735. doi: 10.1002/chir.23200. Epub 2020 Feb 27.

Abstract

The modern β-adrenergic agonists (β-blockers) possess one or more than one chiral center in their structure. Two enantiomers exhibit distinct pharmacodynamic and pharmacokinetic behaviors. Current progress in drug designing has resulted in the ability to understand the role of chirality in modern therapeutics. Furthermore, with a greater understanding of the molecular structure of precise drug targets, development of new drugs is directed towards the pure enantiomers instead of its racemates. The present review deals with a discussion on the stereochemical facets of chiral clinical β-blockers. This review provides details of stereo-selectivity in the pharmacological behavior of some of β-blockers and their metabolites. An effort has been made on highlighting the distinction between the therapeutic behavior of the racemic mixtures and pure enantiomers.

Keywords: chirality; pharmacodynamics; pharmacokinetics; stereochemical facets; β-blockers.

Publication types

  • Review

MeSH terms

  • Adrenergic beta-Antagonists / chemistry*
  • Adrenergic beta-Antagonists / metabolism
  • Adrenergic beta-Antagonists / pharmacology
  • Humans
  • Stereoisomerism

Substances

  • Adrenergic beta-Antagonists