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Title: Binding of /sup 3/H-acetylcholine to cholinergic receptors in bovine cerebral arteries

Abstract

Cholinergic receptor sites in bovine cerebral arteries were analyzed using radioligand binding techniques with the cholinergic agonist, /sup 3/H-acetylcholine (ACh), as the ligand. Specific binding of /sup 3/H-ACh to membrane preparations of bovine cerebral arteries was saturable, of two binding sites, with dissociation constant (K/sub D/) values of 0.32 and 23.7 nM, and maximum binding capacity (Bmax) values of 67 and 252 fmol/mg protein, respectively. Specific binding of /sup 3/H-ACh was displaced effectively by muscarinic cholinergic agents and less effectively by nicotinic cholinergic agents. IC/sub 50/ values of cholinergic drugs for /sup 3/H-ACh binding were as follows: atropine, 38.5 nM; ACh, 59.8 nM; oxotremorine, 293 nM; scopolamine 474 nM; carbamylcholine, 990 nM. IC/sub 50/ values of nicotinic cholinergic agents such as nicotine, cytisine and ..cap alpha..-bungarotoxin exceeded 50 ..mu..M. Choline acetyltransferase activity was 1.09 nmol/mg protein/hour in the cerebral arteries. These findings suggest that the cholinergic nerves innervate the bovine cerebral arteries and that there are at least two classes of ACh binding sites of different affinities on muscarinic reporters in these arteries. 18 references, 2 figures, 2 tables.

Authors:
; ; ;
Publication Date:
Research Org.:
Kyoto Univ., Japan
OSTI Identifier:
6138596
Resource Type:
Journal Article
Journal Name:
Life Sci.; (United States)
Additional Journal Information:
Journal Volume: 37:20
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; ACETYLCHOLINE; BIOCHEMICAL REACTION KINETICS; CHOLINE; RECEPTORS; TRANSFERASES; ENZYME ACTIVITY; AFFINITY; ARTERIES; ATROPINE; BRAIN; CATTLE; CELL MEMBRANES; CHEMICAL BONDS; EXPERIMENTAL DATA; LIGANDS; NERVES; NICOTINE; TRACER TECHNIQUES; TRITIUM COMPOUNDS; ALCOHOLS; ALKALOIDS; AMINES; AMMONIUM COMPOUNDS; ANIMALS; AUTONOMIC NERVOUS SYSTEM AGENTS; AZINES; AZOLES; BLOOD VESSELS; BODY; CARDIOVASCULAR SYSTEM; CELL CONSTITUENTS; CENTRAL NERVOUS SYSTEM; DATA; DOMESTIC ANIMALS; DRUGS; ENZYMES; ESTERS; HETEROCYCLIC COMPOUNDS; HYDROXY COMPOUNDS; INFORMATION; ISOTOPE APPLICATIONS; KINETICS; LABELLED COMPOUNDS; LIPOTROPIC FACTORS; MAMMALS; MEMBRANE PROTEINS; MEMBRANES; NERVOUS SYSTEM; NEUROREGULATORS; NUMERICAL DATA; ORGANIC COMPOUNDS; ORGANIC NITROGEN COMPOUNDS; ORGANS; PARASYMPATHOLYTICS; PARASYMPATHOMIMETICS; PROTEINS; PYRIDINES; PYRROLES; PYRROLIDINES; QUATERNARY COMPOUNDS; REACTION KINETICS; RUMINANTS; VERTEBRATES; 550201* - Biochemistry- Tracer Techniques

Citation Formats

Shimohama, S, Tsukahara, T, Taniguchi, T, and Fujiwara, M. Binding of /sup 3/H-acetylcholine to cholinergic receptors in bovine cerebral arteries. United States: N. p., 1985. Web. doi:10.1016/0024-3205(85)90006-2.
Shimohama, S, Tsukahara, T, Taniguchi, T, & Fujiwara, M. Binding of /sup 3/H-acetylcholine to cholinergic receptors in bovine cerebral arteries. United States. https://doi.org/10.1016/0024-3205(85)90006-2
Shimohama, S, Tsukahara, T, Taniguchi, T, and Fujiwara, M. 1985. "Binding of /sup 3/H-acetylcholine to cholinergic receptors in bovine cerebral arteries". United States. https://doi.org/10.1016/0024-3205(85)90006-2.
@article{osti_6138596,
title = {Binding of /sup 3/H-acetylcholine to cholinergic receptors in bovine cerebral arteries},
author = {Shimohama, S and Tsukahara, T and Taniguchi, T and Fujiwara, M},
abstractNote = {Cholinergic receptor sites in bovine cerebral arteries were analyzed using radioligand binding techniques with the cholinergic agonist, /sup 3/H-acetylcholine (ACh), as the ligand. Specific binding of /sup 3/H-ACh to membrane preparations of bovine cerebral arteries was saturable, of two binding sites, with dissociation constant (K/sub D/) values of 0.32 and 23.7 nM, and maximum binding capacity (Bmax) values of 67 and 252 fmol/mg protein, respectively. Specific binding of /sup 3/H-ACh was displaced effectively by muscarinic cholinergic agents and less effectively by nicotinic cholinergic agents. IC/sub 50/ values of cholinergic drugs for /sup 3/H-ACh binding were as follows: atropine, 38.5 nM; ACh, 59.8 nM; oxotremorine, 293 nM; scopolamine 474 nM; carbamylcholine, 990 nM. IC/sub 50/ values of nicotinic cholinergic agents such as nicotine, cytisine and ..cap alpha..-bungarotoxin exceeded 50 ..mu..M. Choline acetyltransferase activity was 1.09 nmol/mg protein/hour in the cerebral arteries. These findings suggest that the cholinergic nerves innervate the bovine cerebral arteries and that there are at least two classes of ACh binding sites of different affinities on muscarinic reporters in these arteries. 18 references, 2 figures, 2 tables.},
doi = {10.1016/0024-3205(85)90006-2},
url = {https://www.osti.gov/biblio/6138596}, journal = {Life Sci.; (United States)},
number = ,
volume = 37:20,
place = {United States},
year = {Mon Nov 18 00:00:00 EST 1985},
month = {Mon Nov 18 00:00:00 EST 1985}
}