Linked Life Data

7230009

Source:http://linkedlifedata.com/resource/pubmed/id/7230009

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
1981-7-23
pubmed:abstractText
In the presence of biologically active grayanotoxins, the frog skeletal muscle fiber generated a spontaneous action potential which was followed by a sustained depolarization. This depolarization was due to the specific increase in the membrane permeability to sodium, as it was abolished by withdrawal of sodium from the external medium or application of 1 x 10(-6) M tetrodotoxin. Potencies of biological activity of 34 grayanotoxin analogs were estimated from the measurement of critical concentrations for spontaneous generation of a prolonged action potential. It was found that the biological activity of grayanotoxins was largely dependent on both stereospecificity and hydrophobicity of the molecules. The essential groups in the grayanotoxin molecules for the biological activity were determined to be 3 beta-OH or 2 beta, 3 beta-epoxy group, 5 beta-OH, 6 beta-OH and 10 beta-methyl groups. There was an optimal hydrophobicity of the molecule for the maximal biological activity. Either increase or decrease in the number of OH groups from the optimal number of five reduced the biological activity. Four essential groups corresponding to those in the grayanotoxin molecules are also present in the molecules of veratridine, batrachotoxin and aconitine, all of which are known to keep the sodium channel open.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0022-3565
pubmed:author
pubmed:issnType
Print
pubmed:volume
217
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
812-9
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1981
pubmed:articleTitle
Structure-activity relationship for grayanotoxin derivatives in frog skeletal muscle.
pubmed:publicationType
Journal Article, In Vitro, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't