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PMID: 272000 Published · ppublish English Journal Article

Histrionicotoxin enhances agonist-induced desensitization of acetylcholine receptor.

Proceedings of the National Academy of Sciences of the United States of America ·Vol. 74 ·No. 12 ·1977-12-00 ·Pages 5754-8

Burgermeister W, Catterall WA, Witkop B

Abstract

Dihydroisohistrionicotoxin inhibits acetylcholine receptor-dependent 22Na+ uptake of cultured chick muscle cells with a KI of 0.2 micrometer. The inhibition is noncompetitive with respect to agonists. The toxin enhances desensitization of the receptor by agonists which is accompanied by a 10-fold increase in receptor affinity for agonists. Dihydroisohistrionicotoxin increases the affinity of the desensitized form of the receptor for agonists but not antagonists. The results suggest that dihydroisohistrionicotoxin inhibits the acetylcholine receptor by causing an increase in the affinity of the desensitized form of the receptor for agonists and thereby stabilizing the desensitized state.

MeSH Terms
Amphibian Venoms/pharmacology Animals Binding, Competitive Biological Transport/drug effects Bungarotoxins/metabolism Chick Embryo Muscles/drug effects,metabolism Parasympatholytics/metabolism Parasympathomimetics/metabolism Receptors, Cholinergic/drug effects,metabolism Sodium/metabolism
Chemicals
Amphibian Venoms Bungarotoxins Parasympatholytics Parasympathomimetics Receptors, Cholinergic Sodium
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Burgermeister W
Catterall W A
Witkop B
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20 references, click to expand
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Article Info
Journal
Proceedings of the National Academy of Sciences of the United States of America
Abbr.
Proc Natl Acad Sci U S A
ISSN
0027-8424
DOI
10.1073/pnas.74.12.5754
Published
1977-12-00
Pages
5754-8
Language
English
Region
United States
NLM ID
7505876
PMCID
PMC431872
Subset
IM
External Links
PubMed source DOI: 10.1073/pnas.74.12.5754 PMC Full Text View journal details
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