Linked Life Data

2145838

Source:http://linkedlifedata.com/resource/pubmed/id/2145838

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
7
pubmed:dateCreated
1990-11-8
pubmed:abstractText
9,11-Dimethylmethano -11,12-methano-16-(3-azido-4-iodophenoxy)-13,14- dihydro-13-aza-15 alpha beta-omega-tetranor TXA2 (I-PTA-PON3) was synthesized and evaluated as a potential photoaffinity probe of the human platelet thromboxane A2/prostaglandin H2 (TXA2/PGH2) receptor. I-PTA-PON3 inhibited the aggregation of washed human platelets induced by the TXA2 mimetic U46619 [(15S)-hydroxy-11 alpha, 9 alpha-(epoxymethano)prosta-5Z,13E-dienoic acid]. Schild analysis of the data revealed a Kd of 9.5 nM and a slope not significantly different from -1. Equilibrium binding studies using [125I]PTA-OH, a TXA2/PGH2 receptor antagonist, showed that I-PTA-PON3 plus photolysis resulted in a 52% reduction in the number of binding sites (1252 +/- 202/platelet) compared to the nonphotolyzed group (2557 +/- 293/platelet) (N = 5, P less than 0.05) with no significant change in the Kd. Repetition of the incubation with I-PTA-PON3 and photolysis a second time resulted in a further 77% (578 +/- 163 binding sites/platelet) reduction in the number of binding sites. Incubation of washed human platelets with I-PTA-PON3 (163 nM) followed by photolysis and removal of the non-covalently bound I-PTA-PON3 resulted in no change in the EC50 value for the TXA2 mimetic, U46619, when compared to controls that were either exposed to I-PTA-PON3 and not photolyzed or exposed only to photolysis. The second photolysis of I-PTA-PON3 resulted in a significant 42% increase in the EC50 value of U46619-induced aggregation compared to the non-photolyzed group (N = 4, P less than 0.05). These results suggest that I-PTA-PON3 is a useful probe for the study of TXA2/PGH2 receptors and that spare TXA2/PGH2 receptors may exist in the platelet.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0006-2952
pubmed:author
pubmed:issnType
Print
pubmed:day
1
pubmed:volume
40
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1457-61
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1990
pubmed:articleTitle
Photoaffinity receptor antagonist for human platelet thromboxane A2/prostaglandin H2 receptors.
pubmed:affiliation
Department of Cell and Molecular Pharmacology, Medical University of South Carolina, Charleston 29425.
pubmed:publicationType
Journal Article, Comparative Study, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't