Quantitative analysis of binding parameters of [ 3H] N-methylscopolamine in central nervous system of muscarinic acetylcholine receptor knockout mice

We have studied binding parameters ( K d, B max) of [ 3H] N-methylscopolamine ([ 3H]NMS) in various brain regions and spinal cord of wild-type (WT) and muscarinic acetylcholine receptor (mAChR) subtype (M 1–M 5) knockout (KO) mice. In the M 1–M 4 KO mice, the number of [ 3H]NMS binding sites ( B max...

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Veröffentlicht in:Brain research. Molecular brain research. 2005-01, Vol.133 (1), p.6-11
Hauptverfasser: Oki, Tomomi, Takagi, Yukiko, Inagaki, Sayuri, Taketo, Makoto M., Manabe, Toshiya, Matsui, Minoru, Yamada, Shizuo
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container_title Brain research. Molecular brain research.
container_volume 133
creator Oki, Tomomi
Takagi, Yukiko
Inagaki, Sayuri
Taketo, Makoto M.
Manabe, Toshiya
Matsui, Minoru
Yamada, Shizuo
description We have studied binding parameters ( K d, B max) of [ 3H] N-methylscopolamine ([ 3H]NMS) in various brain regions and spinal cord of wild-type (WT) and muscarinic acetylcholine receptor (mAChR) subtype (M 1–M 5) knockout (KO) mice. In the M 1–M 4 KO mice, the number of [ 3H]NMS binding sites ( B max) was decreased throughout the central nervous system (CNS) with significant regional differences. Our results collectively suggest that M 1 receptor was present in a relatively high density in the cerebral cortex and hippocampus, and the densities of M 1 and M 4 subtypes were highest in the corpus striatum. M 2 receptor appeared to be the major subtype in the thalamus, hypothalamus, midbrain, pons-medulla, cerebellum and spinal cord. These findings may contribute significantly not only to the further understanding of the physiological roles of mAChR subtypes in the central cholinergic functions, but also to the development of selective therapeutic agents targeting specific subtype.
doi_str_mv 10.1016/j.molbrainres.2004.09.012
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Molecular brain research.</title><addtitle>Brain Res Mol Brain Res</addtitle><description>We have studied binding parameters ( K d, B max) of [ 3H] N-methylscopolamine ([ 3H]NMS) in various brain regions and spinal cord of wild-type (WT) and muscarinic acetylcholine receptor (mAChR) subtype (M 1–M 5) knockout (KO) mice. In the M 1–M 4 KO mice, the number of [ 3H]NMS binding sites ( B max) was decreased throughout the central nervous system (CNS) with significant regional differences. Our results collectively suggest that M 1 receptor was present in a relatively high density in the cerebral cortex and hippocampus, and the densities of M 1 and M 4 subtypes were highest in the corpus striatum. M 2 receptor appeared to be the major subtype in the thalamus, hypothalamus, midbrain, pons-medulla, cerebellum and spinal cord. 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subjects Animals
Biological and medical sciences
Central Nervous System - metabolism
CNS distribution
Dose-Response Relationship, Drug
Fundamental and applied biological sciences. Psychology
Knockout mice
Mice
Mice, Knockout - metabolism
Muscarinic acetylcholine receptor subtype
N-Methylscopolamine - pharmacokinetics
Parasympatholytics - pharmacokinetics
Protein Binding
Radioligand Assay - methods
Receptors, Muscarinic - classification
Receptors, Muscarinic - genetics
Receptors, Muscarinic - metabolism
Tissue Distribution
Tritium
Vertebrates: nervous system and sense organs
title Quantitative analysis of binding parameters of [ 3H] N-methylscopolamine in central nervous system of muscarinic acetylcholine receptor knockout mice
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