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Adrenergics and Adrenergic-Blocking Agents

  1. Robert K. Griffith

Published Online: 15 JAN 2003

DOI: 10.1002/0471266949.bmc093

Burger's Medicinal Chemistry and Drug Discovery

Burger's Medicinal Chemistry and Drug Discovery

How to Cite

Griffith, R. K. 2003. Adrenergics and Adrenergic-Blocking Agents. Burger's Medicinal Chemistry and Drug Discovery. 1–37.

Author Information

  1. West Virginia University, School of Pharmacy, Morgantown, West Virginia, USA

Publication History

  1. Published Online: 15 JAN 2003


This chapter reviews the drugs currently available in the United States that exert their therapeutic effects through actions on α- and β-adrenoceptors and biosynthesis, release, and processing of the neurotransmitter norepinephrine. Included in the review are drugs acting as selective and nonselective agonists and antagonists at both α- and β-adrenoceptors, as well as drugs that interfere with norepinephrine biosynthesis and release. Therapeutic categories include antihypertensives, bronchodilators, antiglaucoma agents, vasopressors, and nasal decongestants. Structure-activity relationships are reviewed as are the structure and function of various adrenoceptors. Briefly covered is the metabolism of representative drugs in each structural class as well as recent developments in approaches to new drugs in the areas of selective α1A-antagonists for treatment of prostatic hypertrophy and selective β3-agonists for treatment of obesity and diabetes.


  • α-blockers;
  • β-blockers;
  • antihypertensives;
  • antiglaucoma;
  • bronchodilators;
  • vasopressors;
  • nasal decongestants;
  • BPH;
  • drug metabolism;
  • adrenoceptors