Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
19
pubmed:dateCreated
1982-1-20
pubmed:abstractText
The effects of local anesthetics and perhydrohistrionicotoxin on the kinetic mechanism of carbamoylcholine binding to the membrane-bound acetylcholine receptor have been studied by stopped-flow methods. Receptor-enriched membrane fragments from Torpedo californica were reduced and then alkylated by 5-(iodoacetamido)salicylic acid, and the agonist binding kinetics were monitored by the fluorescence changes of this bound probe. The alkylation procedures did not alter the ability of the receptor to mediate agonist-induced cation flux. Preincubation of such modified receptor preparations with saturating concentrations of lidocaine, prilocaine, or dimethisoquin did not significantly affect the equilibrium dissociation constant for carbamoylcholine binding. The multiphasic kinetic signal which accompanies the binding of the agonist was, however, much simplified in the presence of local anesthetics, and the observed kinetics could be described by a mechanism in which a single conformational change follows the formation of the initial complex. Perhydrohistrionicotoxin did not act in the same way as the local anesthetics examined since saturating concentrations did not significantly perturb the agonist binding kinetics.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
0006-2960
pubmed:author
pubmed:issnType
Print
pubmed:day
15
pubmed:volume
20
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
5617-24
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1981
pubmed:articleTitle
Effects of local anesthetics and histrionicotoxin on the binding of carbamoylcholine to membrane-bound acetylcholine receptor.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't