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

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

doi:10.1007/BF02244197

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

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

Neuroscience

Research output: Contribution to journal › Article › peer-review

25 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 language	English (US)
Pages (from-to)	162-165
Number of pages	4
Journal	Psychopharmacology
Volume	103
Issue number	2
DOIs	https://doi.org/10.1007/BF02244197
State	Published - Feb 1991

Keywords

M and M receptors
Parkinsonism drugs
Pirenzepine

ASJC Scopus subject areas

Pharmacology

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10.1007/BF02244197

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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.",

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

Abstract

Keywords

ASJC Scopus subject areas

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