Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
12
pubmed:dateCreated
1982-4-12
pubmed:abstractText
The tritiated calcium antagonist 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridine carboxylic acid, 3-ethyl-5-methyl ester (nitrendipine, Bay e 5009), a potent analogue of nifedipine, binds in a reversible and saturable manner to partially purified guinea-pig heart membranes. The analyses of the equilibrium binding data with Scatchard plots is in accord with either negative cooperativity of binding or with the assumption of two classes of binding sites, where one site has an equilibrium dissociation constant (Kd value) of 0.1 nmol/l and a density of 300 fmol/mg of protein. The binding sites are stereoselective and discriminate between (+)-nitrendipine and (-)-nitrendipine. We conclude that a high-affinity binding site at which 1,4-dihydropyridines bind, has now been identified with radioligand binding techniques. This site may well represent the locus where the potent 1,4-dihydropyridines exert their pharmacological action.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0004-4172
pubmed:author
pubmed:issnType
Print
pubmed:volume
31
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2064-7
pubmed:dateRevised
2003-11-14
pubmed:meshHeading
pubmed:year
1981
pubmed:articleTitle
[3H]-Nitrendipine, a potent calcium antagonist, binds with high affinity to cardiac membranes.
pubmed:publicationType
Journal Article