Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2.
Synthesis and preliminary in vitro biological evaluation of a selective high-affinity CRTH2 antagonist is described. The stability of an N-benzyl group facilitated synthesis of the corresponding radioligand by tritiation of a brominated precursor. The compound [(3)H]TRQ11238 represents the first selective CRTH2 antagonist radioligand and exhibited a specific radioactivity of 52 Ci/mmol and a pK(d) of 9.0.
Ulven
Trond
T
Department of Physics and Chemistry, University of Southern Denmark, Campusvej 55, DK-5230 Odense M, Denmark.
Gallen
Michael J
MJ
Nielsen
Mads C
MC
Merten
Nicole
N
Schmidt
Carola
C
Mohr
Klaus
K
Tränkle
Christian
C
Kostenis
Evi
E
D004353:Drug Evaluation, Preclinical; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology*; D011869:Radioligand Assay; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors*; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors*; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology*
D007211:Indoles; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; D013449:Sulfonamides; C526169:TRQ11238; C036293:prostaglandin D2 receptor