An Index of Relative Central α-Adrenergic Receptor Antagonism by Antipsychotic Medications

Michael J. Minzenberg, Jong H. Yoon

Research output: Contribution to journalArticlepeer-review

14 Scopus citations


Antipsychotic medications exert variable and clinically significant levels of antagonism at central α-adrenergic receptors. To evaluate the impact of this activity on both clinical and experimental measures, an index estimating the relative activity of these medications is needed. We comprehensively searched the empirical literature testing in vitro binding to mammalian brain α-adrenergic receptors of all antipsychotic medications available for clinical use in the United States as of August 2010 and created a quantitative summary index of the potency of binding to α receptors relative to haloperidol (HALα1 and HALα2 equivalents). The potency of binding at α1- and α2-adrenergic receptors varies widely among these medications, with a 532-fold range for α1 antagonism and a 400-fold range for α2 antagonism among atypical antipsychotics. There is considerable overlap between atypical and typical antipsychotic medication groups on each of these measures. This index of HALα equivalents should facilitate the determination of the effects of α-adrenergic antagonism by these medications on clinical efficacy, side effects, and biological and cognitive measures of illness and treatment.

Original languageEnglish (US)
Pages (from-to)31-39
Number of pages9
JournalExperimental and Clinical Psychopharmacology
Issue number1
StatePublished - Feb 2011


  • α-adrenergic
  • Antipsychotic
  • Atypical
  • Neuroleptic

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)
  • Psychiatry and Mental health


Dive into the research topics of 'An Index of Relative Central α-Adrenergic Receptor Antagonism by Antipsychotic Medications'. Together they form a unique fingerprint.

Cite this