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Title: Distribution of muscarinic receptor subtypes in rat brain as determined in binding studies with AF-DX 116 and pirenzepine

Abstract

In vitro competition binding experiments with the selective muscarinic antagonists AF-DX 116 and pirenzepine (PZ) vs /sup 3/H-N-methylscopolamine as radioligand revealed a characteristic distribution of muscarinic receptor subtypes in different regions of rat brain. Based on nonlinear least squares analysis, the binding data were compatible with the presence of three different subtypes: the M/sub 1/ receptor (high affinity for PZ), the cardiac M/sub 2/ receptor (high affinity for AF-DX 116) and the glandular M/sub 2/ receptor (low affinity for PZ and AF-DX 116). The highest proportion of M/sub 1/ receptors was found in the hippocampus, while the cerebellum and the hypothalamus were the regions with the largest fraction of the cardiac M/sub 2/ and glandular M/sub 2/ receptors, respectively. In certain brain areas, depending on the relative proportions of the subtypes, flat binding curves were seen for AF-DX 116 and PZ. Based on these data, an approximate distribution pattern of the subtypes in the various brain regions is presented. 19 references, 1 figure, 2 tables.

Authors:
; ;
Publication Date:
Research Org.:
Instituto De Angeli, Milan, Italy
OSTI Identifier:
6846924
Resource Type:
Journal Article
Journal Name:
Life Sci.; (United States)
Additional Journal Information:
Journal Volume: 40:9
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; ANTIPYRETICS; BIOCHEMICAL REACTION KINETICS; CHOLINE; RECEPTORS; TISSUE DISTRIBUTION; AFFINITY; BRAIN; EXPERIMENTAL DATA; LIGANDS; RATS; TRACER TECHNIQUES; TRITIUM COMPOUNDS; ALCOHOLS; AMINES; AMMONIUM COMPOUNDS; ANIMALS; BODY; CENTRAL NERVOUS SYSTEM; CENTRAL NERVOUS SYSTEM DEPRESSANTS; DATA; DISTRIBUTION; DRUGS; HYDROXY COMPOUNDS; INFORMATION; ISOTOPE APPLICATIONS; KINETICS; LABELLED COMPOUNDS; LIPOTROPIC FACTORS; MAMMALS; MEMBRANE PROTEINS; NERVOUS SYSTEM; NUMERICAL DATA; ORGANIC COMPOUNDS; ORGANS; PROTEINS; QUATERNARY COMPOUNDS; REACTION KINETICS; RODENTS; VERTEBRATES; 550201* - Biochemistry- Tracer Techniques

Citation Formats

Giraldo, E, Hammer, R, and Ladinsky, H. Distribution of muscarinic receptor subtypes in rat brain as determined in binding studies with AF-DX 116 and pirenzepine. United States: N. p., 1987. Web. doi:10.1016/0024-3205(87)90031-2.
Giraldo, E, Hammer, R, & Ladinsky, H. Distribution of muscarinic receptor subtypes in rat brain as determined in binding studies with AF-DX 116 and pirenzepine. United States. https://doi.org/10.1016/0024-3205(87)90031-2
Giraldo, E, Hammer, R, and Ladinsky, H. 1987. "Distribution of muscarinic receptor subtypes in rat brain as determined in binding studies with AF-DX 116 and pirenzepine". United States. https://doi.org/10.1016/0024-3205(87)90031-2.
@article{osti_6846924,
title = {Distribution of muscarinic receptor subtypes in rat brain as determined in binding studies with AF-DX 116 and pirenzepine},
author = {Giraldo, E and Hammer, R and Ladinsky, H},
abstractNote = {In vitro competition binding experiments with the selective muscarinic antagonists AF-DX 116 and pirenzepine (PZ) vs /sup 3/H-N-methylscopolamine as radioligand revealed a characteristic distribution of muscarinic receptor subtypes in different regions of rat brain. Based on nonlinear least squares analysis, the binding data were compatible with the presence of three different subtypes: the M/sub 1/ receptor (high affinity for PZ), the cardiac M/sub 2/ receptor (high affinity for AF-DX 116) and the glandular M/sub 2/ receptor (low affinity for PZ and AF-DX 116). The highest proportion of M/sub 1/ receptors was found in the hippocampus, while the cerebellum and the hypothalamus were the regions with the largest fraction of the cardiac M/sub 2/ and glandular M/sub 2/ receptors, respectively. In certain brain areas, depending on the relative proportions of the subtypes, flat binding curves were seen for AF-DX 116 and PZ. Based on these data, an approximate distribution pattern of the subtypes in the various brain regions is presented. 19 references, 1 figure, 2 tables.},
doi = {10.1016/0024-3205(87)90031-2},
url = {https://www.osti.gov/biblio/6846924}, journal = {Life Sci.; (United States)},
number = ,
volume = 40:9,
place = {United States},
year = {Mon Mar 02 00:00:00 EST 1987},
month = {Mon Mar 02 00:00:00 EST 1987}
}