Linked Life Data

1816763

Source:http://linkedlifedata.com/resource/pubmed/id/1816763

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:dateCreated
1992-6-29
pubmed:abstractText
The effects of CD349 [2-nitratopropyl-3-nitratopropyl-2,6-dimethyl-4-(3- nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate], a dihydropyridine derivative Ca2+ antagonist, were studied on low and high voltage-activated Ca2+ currents in single pyramidal neurons isolated from the rat hippocampal CA1 region. CD349 inhibited the peak amplitude of the low voltage-activated Ca2+ current in a concentration-dependent manner with a threshold concentration of about 10(-7) M. The concentration for half-maximum inhibition was 1.5 x 10(-6) M. At 10(-5) M or more, a complete suppression of the low voltage-activated Ca2+ current was observed. There was no apparent effect on the current-voltage relationship and the current kinetics (rising and decaying phases of the current). The inhibitory potency of CD349 was similar to that of nicardipine. CD349, at a concentration of 10(-6) M (near the half-maximum inhibition concentration), delayed the reactivation and enhanced voltage- and time-dependently the inactivation of the low voltage-activated Ca2+ channel, suggesting that CD349 preferentially binds to the inactivated Ca2+ channel. CD349 also decreased the peak amplitude of the high voltage-activated Ca2+ current at half-maximum inhibition concentrations of 5.7 x 10(-6) M. The current kinetics of the high voltage-activated Ca2+ current were slightly accelerated without shifting the current-voltage relationship in the presence of 10(-5) M of CD349. The potency of CD349 in inhibiting both types of Ca2+ current was also similar to that of nicardipine. It is suggested that the blocking effect of CD349 on neuronal Ca2+ influx, in combination with a cerebral vasodilatory action, may contribute to a favorable effect on ischemic brain damage.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0301-4533
pubmed:author
pubmed:issnType
Print
pubmed:volume
313
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
47-62
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:articleTitle
Effect of CD349, a new dihydropyridine derivative Ca2+ antagonist, on the voltage-dependent Ca2+ currents in isolated mammalian brain neurons.
pubmed:affiliation
Department of Neurophysiology, Tohoku University School of Medicine, Sendai, Japan.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't