Linked Life Data

1649411

Source:http://linkedlifedata.com/resource/pubmed/id/1649411

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
1991-8-16
pubmed:abstractText
The inhibitory effect of a new dihydropyridine derivative, (+/-)-2-[benzyl(phenyl)amino]ethyl-1,4-dihydro-2,6-dimethyl-5- (5,5-dimethyl-2-oxo-1,3,2-dioxaphosphorinan-2-yl)-4-(3-nitrophenyl )-3- pyridinecarboxylate hydrochloride (NZ-105), on whole cell Ca2+ current (ICa) in cultured vascular smooth muscle cells was investigated with the patch clamp technique. NZ-105 blocked ICa in a concentration-dependent manner when the command pulse ranged from +10 mV to -50 mV. The inhibitory effect of NZ-105 appeared at concentrations higher than 10 pmol/l and it blocked ICa completely at a concentration of 1 nmol/l. The concentration which produced the half-maximal inhibitory effect was estimated to be around 20 pmol/l. NZ-105 (500 pmol/l) completely blocked ICa elicited by depolarization to +10 mV at a holding potential of -40 mV, whereas it blocked ICa by only 67% at a holding potential of -90 mV. NZ-105 (100 pmol/l) shifted the steady-state inactivation curve by 40 mV to more negative potentials without affecting its slope factor. The blocking time constant of 500 pmol/l NZ-105 was 57.6 +/- 9.9 s at a holding potential of -70 mV. These results indicate that NZ-105 has characteristics typical of dihydropyridines and binds to Ca2+ channels of vascular smooth muscle cells with a high affinity. They also suggested that the slow onset of its action is due to the slow binding of the drug to Ca2+ channels.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
0028-1298
pubmed:author
pubmed:issnType
Print
pubmed:volume
343
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
405-10
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1991
pubmed:articleTitle
Mechanisms underlying the slow onset of action of a new dihydropyridine, NZ-105, on a cultured smooth muscle cell line.
pubmed:affiliation
Department of Physiology, Jikei University, School of Medicine, Tokyo, Japan.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't