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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Veröffentlicht in:	Psychopharmacologia 1991-01, Vol.103 (2), p.162-165
Hauptverfasser:	LARSON, E. W, PFENNING, M. A, RICHELSON, E
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Brain - drug effects Brain - metabolism Cholinergic system Heart - drug effects Humans In Vitro Techniques Kinetics Medical sciences Myocardium - metabolism Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Parasympatholytics - pharmacology Pharmacology. Drug treatments Quinuclidinyl Benzilate - pharmacology Radioligand Assay Receptors, Muscarinic - drug effects
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Beschreibung
Zusammenfassung:	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 1432-2072
DOI:	10.1007/BF02244197