Selectivity of antimuscarinic compounds for muscarinic receptors of human brain and heart

Eric W. Larson, Michael A. Pfenning, Elliott Richelson

Research output: Contribution to journalArticle

24 Scopus citations

Abstract

Seven antimuscarinic compounds, used mostly for the treatment of extrapyramidal problems, were tested in vitro in radioligand binding assays for evidence of selectivity for two different pharmacological subtypes of the human muscarinic receptor, M1, a predominant form in brain, and M2, a predominant form in heart. Although biperiden, scopolamine, procyclidine, and benztropine showed significant selectivity in the in vitro assays, it is likely that in clinical practice biperiden would be the drug of choice to avoid any antimuscarinic effects on the heart.

Original languageEnglish (US)
Pages (from-to)162-165
Number of pages4
JournalPsychopharmacology
Volume103
Issue number2
DOIs
StatePublished - Feb 1991

Keywords

  • M and M receptors
  • Parkinsonism drugs
  • Pirenzepine

ASJC Scopus subject areas

  • Pharmacology

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