Selectivity of muscarinic antagonists in radioligand and in vivo experiments for the putative M1, M2 and M3 receptors.

Article Details

Citation

Doods HN, Mathy MJ, Davidesko D, van Charldorp KJ, de Jonge A, van Zwieten PA

Selectivity of muscarinic antagonists in radioligand and in vivo experiments for the putative M1, M2 and M3 receptors.

J Pharmacol Exp Ther. 1987 Jul;242(1):257-62.

PubMed ID
3612532 [ View in PubMed
]
Abstract

In the present study we investigated the nature of the muscarinic receptors present in the hippocampus, sympathetic ganglia, atria and salivary glands of the rat. The heterogeneity of the muscarinic receptors was examined both in vivo and in radioligand binding experiments. To study whether the receptors present in the investigated tissues are indeed distinct subtypes we determined the potencies of antagonists in both systems. It is proposed that there are three different binding sites present in hippocampal, atrial and submandibular membranes and we suggest to classify them as M1, M2 and M3, respectively. Both in vivo and in vitro pirenzepine appears to possess high affinity for M1 receptors, whereas 4-diphenylacetoxy-N-methylpiperidine methobromide and dicyclomine show high affinity for both M1 and M3 receptors. AF-DX 116 (11-2[[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5, 11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepine-6-one) displayed high affinity for M2 receptors.

DrugBank Data that Cites this Article

Drugs
Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
DicyclomineMuscarinic acetylcholine receptor M1ProteinHumans
Yes
Antagonist
Details
DicyclomineMuscarinic acetylcholine receptor M2ProteinHumans
Unknown
Antagonist
Details
DicyclomineMuscarinic acetylcholine receptor M3ProteinHumans
Unknown
Antagonist
Details