[Synthesis of tritium-labelled prostaglandin E1 and its binding to human platelets].
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 1.7-1.8 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 (approximately 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.
Shevchenko
V P
VP
Nagaev
I Iu
IIu
Vrzheshch
P V
PV
Ershov
D E
DE
Zaĭtsev
S V
SV
D000244:Adenosine Diphosphate / Q000494:pharmacology; D000527:Alprostadil / Q000138:chemical synthesis* / Q000378:metabolism; D001792:Blood Platelets / Q000378:metabolism*; D055598:Chemical Phenomena; D002621:Chemistry; D006801:Humans; D066298:In Vitro Techniques; D007553:Isotope Labeling; D007700:Kinetics; D008024:Ligands; D010974:Platelet Aggregation / Q000187:drug effects; D011869:Radioligand Assay; D014316:Tritium
D008024:Ligands; D014316:Tritium; D000244:Adenosine Diphosphate; D000527:Alprostadil
Sintez mechennogo tritiem prostaglandina e1 i ego sviazyvanie s trombotsitami cheloveka.