Proton magnetic resonance studies of cholinergic ligand binding to the acetylcholine receptor in its membrane environment.

Proton magnetic resonance has been used to monitor binding of choline, a known partial agonist, to acetylcholine receptor-enriched membrane preparations from Torpedo californica electroplax. The interaction between choline and receptor led to a broadening of the resonance of the choline methyl group...

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Manylion Llyfryddiaeth
Prif Awduron: Miller, J, Witzemann, V, Quast, U, Raftery, M A
Fformat: Erthygl
Iaith:en
Cyhoeddwyd: 1979
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Research Article
Mynediad Ar-lein:https://ncbi.nlm.nih.gov/pmc/articles/PMC383875/
https://ncbi.nlm.nih.gov/pubmed/291025
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id pubmed-383875
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spelling pubmed-3838752004-07-30 Proton magnetic resonance studies of cholinergic ligand binding to the acetylcholine receptor in its membrane environment. Miller, J Witzemann, V Quast, U Raftery, M A Proc Natl Acad Sci U S A Research Article Proton magnetic resonance has been used to monitor binding of choline, a known partial agonist, to acetylcholine receptor-enriched membrane preparations from Torpedo californica electroplax. The interaction between choline and receptor led to a broadening of the resonance of the choline methyl groups and this effect was reversed by alpha-bungarotoxin, a quasi-irreversible antagonist of the acetylcholine receptor. From the concentration dependence of line broadening the equilibrium dissociation constant for choline was obtained (Kd = 190 +/- 65 microM). The temperature dependence of the parameters observed in the choline titrations gave an enthalpy of binding delta H less than 1.5 kcal/mol and allowed estimates for the dissociation rate constant of the receptor-choline complex (kdiss greater than 1.6 x 10(3) S(1) and the respective activation energy, Ea (Kdiss) approximately 5.5 kcal/mol. The association of other ligands with the membrane-bound receptor could also be studied by observing effects of varying concentrations of such ligands on the choline methyl group linewidth at a constant choline concentration. 1979-08 /pmc/articles/PMC383875/ /pubmed/291025 Text en
institution US National Library of Medicine
collection PubMed Central
language en
format Article
topic Research Article
spellingShingle Research Article
Miller, J
Witzemann, V
Quast, U
Raftery, M A
Proton magnetic resonance studies of cholinergic ligand binding to the acetylcholine receptor in its membrane environment.
description Proton magnetic resonance has been used to monitor binding of choline, a known partial agonist, to acetylcholine receptor-enriched membrane preparations from Torpedo californica electroplax. The interaction between choline and receptor led to a broadening of the resonance of the choline methyl groups and this effect was reversed by alpha-bungarotoxin, a quasi-irreversible antagonist of the acetylcholine receptor. From the concentration dependence of line broadening the equilibrium dissociation constant for choline was obtained (Kd = 190 +/- 65 microM). The temperature dependence of the parameters observed in the choline titrations gave an enthalpy of binding delta H less than 1.5 kcal/mol and allowed estimates for the dissociation rate constant of the receptor-choline complex (kdiss greater than 1.6 x 10(3) S(1) and the respective activation energy, Ea (Kdiss) approximately 5.5 kcal/mol. The association of other ligands with the membrane-bound receptor could also be studied by observing effects of varying concentrations of such ligands on the choline methyl group linewidth at a constant choline concentration.
author Miller, J
Witzemann, V
Quast, U
Raftery, M A
author_facet Miller, J
Witzemann, V
Quast, U
Raftery, M A
author_sort Miller, J
title Proton magnetic resonance studies of cholinergic ligand binding to the acetylcholine receptor in its membrane environment.
title_short Proton magnetic resonance studies of cholinergic ligand binding to the acetylcholine receptor in its membrane environment.
title_full Proton magnetic resonance studies of cholinergic ligand binding to the acetylcholine receptor in its membrane environment.
title_fullStr Proton magnetic resonance studies of cholinergic ligand binding to the acetylcholine receptor in its membrane environment.
title_full_unstemmed Proton magnetic resonance studies of cholinergic ligand binding to the acetylcholine receptor in its membrane environment.
title_sort proton magnetic resonance studies of cholinergic ligand binding to the acetylcholine receptor in its membrane environment.
publishDate 1979
url https://ncbi.nlm.nih.gov/pmc/articles/PMC383875/
https://ncbi.nlm.nih.gov/pubmed/291025
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