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

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...

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Bibliographic Details
Published inPsychopharmacology Vol. 103; no. 2; p. 162
Main Authors Larson, E W, Pfenning, M A, Richelson, E
Format Journal Article
LanguageEnglish
Published Germany 01.01.1991
Subjects
Brain - drug effects
Brain - metabolism
Heart - drug effects
Humans
In Vitro Techniques
Kinetics
Myocardium - metabolism
Parasympatholytics - pharmacology
Quinuclidinyl Benzilate - pharmacology
Radioligand Assay
Receptors, Muscarinic - drug effects
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Summary: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.
ISSN:0033-3158
DOI:10.1007/BF02244197