Determination of MK-852, a new fibrinogen receptor antagonist, in plasma and urine by radioimmunoassay.
MK-852 is a novel fibrinogen receptor antagonist. A sensitive and specific radioimmunoassay has been developed for the determination of this drug candidate in plasma and urine. The immunogen was prepared by coupling to albumin via a dinitrophenylene bridge and the radioligand by reaction of the drug with the 125I-labelled Bolton-Hunter reagent. The method was specific and no immunoreactive material other than parent drug was detectable in plasma from dosed volunteers. The direct assay using 0.05 ml of plasma is sensitive to 0.2 ng ml-1 without matrix interference and has sufficient sensitivity, precision, accuracy, and selectivity for the analysis of clinical samples. The lower quantifiable limit in (diluted) urine is 50 ng ml-1.
Yuan
A S
AS
Merck Research Laboratories, West Point, PA 19486.
Hand
E L
EL
Hichens
M
M
Olah
T V
TV
Barrish
A
A
Fernandez-Metzler
C
C
Gilbert
J D
JD
D000595:Amino Acid Sequence; D000818:Animals; D001798:Blood Proteins; D003429:Cross Reactions; D005260:Female; D006493:Heparin / Q000494:pharmacology; D006801:Humans; D008969:Molecular Sequence Data; D009842:Oligopeptides / Q000652:urine*; D010456:Peptides, Cyclic / Q000652:urine*; D010980:Platelet Membrane Glycoproteins / Q000037:antagonists & inhibitors*; D011817:Rabbits; D011863:Radioimmunoassay; D015203:Reproducibility of Results; D012680:Sensitivity and Specificity; D012710:Serum Albumin, Bovine; D053778:Thiazolidines
D001798:Blood Proteins; D009842:Oligopeptides; D010456:Peptides, Cyclic; D010980:Platelet Membrane Glycoproteins; D053778:Thiazolidines; C083231:MK 0852; D012710:Serum Albumin, Bovine; D006493:Heparin