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Chemical modification and reactivity of sulfhydryls and disulfides of rat brain nicotinic-like acetylcholine receptors

Journal Article · · J. Biol. Chem.; (United States)
OSTI ID:6868924
;

Rat central nervous system binding sites for ..cap alpha..-bungarotoxin display considerable biochemical homology with characterized nicotinic acetylcholine receptors from the periphery. They possess a critical disulfide residue(s), which is susceptible to chemical modification and consequent specific alteration in the affinity of the binding site for cholinergic agonists. After reaction with Na/sub 2/S/sub 2/O/sub 5/, as with reaction with dithiothreitol and 5,5'-dithiobis(2-nitrobenzoic acid), the binding site is frozen in a high affinity state toward acetylcholine. After reduction with dithiothreitol and alkylation with a variety of compounds of different molecular configuration or electrical charge, or both, the binding site is frozen in a low affinity state toward acetylcholine. Thus, effects of disulfide/sulfhydryl modification on agonist binding affinity appear to be attributable to the nature of the covalent modification rather than charge or steric alteration at the receptor active site brought about by chemical modification.

Research Organization:
Univ. of California, Berkeley
DOE Contract Number:
W-7405-ENG-48
OSTI ID:
6868924
Journal Information:
J. Biol. Chem.; (United States), Journal Name: J. Biol. Chem.; (United States) Vol. 255:12; ISSN JBCHA
Country of Publication:
United States
Language:
English

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Related Subjects

550200* -- Biochemistry
551000 -- Physiological Systems
59 BASIC BIOLOGICAL SCIENCES
ACETYLCHOLINE
ALKALOIDS
AMINES
AMMONIUM COMPOUNDS
ANIMALS
AZINES
AZOLES
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL EFFECTS
BODY
BRAIN
CENTRAL NERVOUS SYSTEM
DISULFIDES
DRUGS
ESTERS
HETEROCYCLIC COMPOUNDS
KINETICS
MAMMALS
NERVOUS SYSTEM
NICOTINE
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANIC SULFUR COMPOUNDS
ORGANS
PARASYMPATHOMIMETICS
PYRIDINES
PYRROLES
PYRROLIDINES
QUATERNARY COMPOUNDS
RADICALS
RATS
REACTION KINETICS
RECEPTORS
RODENTS
SULFHYDRYL RADICALS
VERTEBRATES