title: Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2.
abstract: 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.
authors.affiliation: Department of Physics and Chemistry, University of Southern Denmark, Campusvej 55, DK-5230 Odense M, Denmark.
authors.forename: Trond
authors.initials: T
authors.lastname: Ulven
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Gallen
authors.forename: Mads C
authors.initials: MC
authors.lastname: Nielsen
authors.forename: Nicole
authors.initials: N
authors.lastname: Merten
authors.forename: Carola
authors.initials: C
authors.lastname: Schmidt
authors.forename: Klaus
authors.initials: K
authors.lastname: Mohr
authors.forename: Christian
authors.initials: C
authors.lastname: Tränkle
authors.forename: Evi
authors.initials: E
authors.lastname: Kostenis
mesh_terms: 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*
chemical_list: D007211:Indoles; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; D013449:Sulfonamides; C526169:TRQ11238; C036293:prostaglandin D2 receptor