Linked Life Data

6895603

Source:http://linkedlifedata.com/resource/pubmed/id/6895603

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
25
pubmed:dateCreated
1982-3-13
pubmed:abstractText
A radioactive photoaffinity derivative of the potent local anesthetic trimethisoquin, 5-azido[3H]trimethisoquin, was used to label the acetylcholine receptor from Torpedo marmorata electric organ. The product labeled the 66 000-dalton (delta) subunit of the receptor with the selectivity expected for an affinity label of the site for noncompetitive blockers. That is, the labeling was enhanced by cholinergic agonists and inhibited by other noncompetitive blockers. The 40 000-dalton (alpha)( subunit of the receptor was labeled in a manner consistent with the attachment of 5-azido[3H]trimethisoquin to an acetylcholine binding site as the incorporation of radioactivity into the alpha chain was inhibited by cholinergic agonists and antagonists, such as carbamylcholine, d-tubocurarine, and alpha-bungarotoxin. The reversible binding of [3H]phencyclidine, a potent noncompetitive blocker, to acetylcholine receptor rich membranes resembled qualitatively and quantitatively the 5-azido[3H]trimethisoquin labeling of the delta subunit and was inhibited by the prior covalent labeling of the membranes with nonradioactive 5-azidotrimethisoquin. Thus, 5-azido[3H]-trimethisoquin labels at least a portion of the binding site for noncompetitive blockers at the level of the delta subunit. The functional significance of this site and the use of 5-azidotrimethisoquin in the study of acetylcholine receptor structure and function are discussed.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Dec
pubmed:issn
0006-2960
pubmed:author
pubmed:issnType
Print
pubmed:day
8
pubmed:volume
20
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
7166-74
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1981
pubmed:articleTitle
Selective labeling of the delta subunit of the acetylcholine receptor by a covalent local anesthetic.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't