SYNTHESIS OF TRITIUM-LABELED PROSTAGLANDIN E-1 AND ITS USE AS A RADIOLIGAND IN STUDYING PGE1 BINDING TO HUMAN-PLATELETS
- 1 August 1988
- journal article
- research article
- Vol. 14 (8) , 1075-1085
Abstract
A method has been developed that makes it possible to obtain [5.6-3H2]PGE1 with a yield of 35% and a molar radioactivity of 1,7.sbd.1,8 TBq/mmol. The binding of [5,6-3H2]PGE1 to native platelets proved to be specific, saturating and reversible. It is characterized by low values (.apprx. 10-9 M) of dissociation constants for high-affinity sites, correlates with the inhibition of ADP-induced aggregation of platelets and can be considered as receptor binding. Specific binding of 10 .+-. 2 molecules of PGE1 with one platelet was found to cause 50% inhibition of the ADP-induced aggregation.This publication has 3 references indexed in Scilit:
- The use of stable prostaglandins to investigate prostacyclin (PGI2)-binding sites and PGI2-sensitive adenylate cyclase in human platelet membranesProstaglandins, 1984
- Identification of platelet receptors for prostaglandin I2 and D2.Journal of Biological Chemistry, 1979
- PROSTAGLANDINS + RELATED FACTORS .27. SYNTHESIS OF TRITIUM-LABELED PROSTAGLANDIN E1 + STUDIES ON ITS DISTRIBUTION + EXCRETION IN RAT1964