rdf:type |
|
lifeskim:mentions |
umls-concept:C0005821,
umls-concept:C0030685,
umls-concept:C0086418,
umls-concept:C0166382,
umls-concept:C0391871,
umls-concept:C0450442,
umls-concept:C0596235,
umls-concept:C0680255,
umls-concept:C1280500,
umls-concept:C1283071,
umls-concept:C1550548,
umls-concept:C1555714,
umls-concept:C1705654,
umls-concept:C1963578
|
pubmed:issue |
2
|
pubmed:dateCreated |
1992-4-21
|
pubmed:abstractText |
We have studied the effects of the antithrombitic agent PCA 4230 on the entry of Mn2+, used here as a Ca2+ surrogate for Ca2+ channels, and on the release of Ca2+ from the intracellular stores in stimulated human platelets loaded with fura-2. PCA 4230 prevented receptor-operated calcium entry activated by thrombin, ADP and collagen with no modification of the Ca2+ release from the intracellular stores. PCA 4230 also inhibited cytochrome P-450-mediated O-dealkylase activity with the same concentration-dependence as the thrombin-induced Mn2+ entry. These results suggest that the inhibitory effects of PCA 4230 on Ca2+ influx may be due to its interaction with cytochrome P-450, which has been proposed recently to be involved in the activation of receptor-operated Ca2+ channels. In addition, PCA 4230 inhibited both PAF-induced Ca2+ entry and Ca2+ release, behaving as a PAF-antagonist. All these effects contribute to explain the antithrombitic action of PCA 4230.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Mar
|
pubmed:issn |
0006-3002
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
2
|
pubmed:volume |
1104
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
257-60
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:1312357-Blood Platelets,
pubmed-meshheading:1312357-Calcium,
pubmed-meshheading:1312357-Calcium Channels,
pubmed-meshheading:1312357-Cytochrome P-450 Enzyme System,
pubmed-meshheading:1312357-Dihydropyridines,
pubmed-meshheading:1312357-Fura-2,
pubmed-meshheading:1312357-Humans,
pubmed-meshheading:1312357-Indoles,
pubmed-meshheading:1312357-Manganese,
pubmed-meshheading:1312357-Platelet Activating Factor,
pubmed-meshheading:1312357-Thrombin
|
pubmed:year |
1992
|
pubmed:articleTitle |
Effects of the antithrombitic agent PCA 4230 on agonist-induced Ca2+ entry and Ca2+ release in human platelets.
|
pubmed:affiliation |
Departamento de Bioquímica y Biología Molecular y Fisiología, Facultad de Medicina, Universidad de Valladolid, Spain.
|
pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
|