title: Development of [(3)H]2-Carboxy-4,6-dichloro-1H-indole-3-propionic Acid ([(3)H]PSB-12150): A Useful Tool for Studying GPR17.
abstract: The recently described synthetic GPR17 agonist 2-carboxy-4,6-dichloro-1H-indole-3-propionic acid (1) was prepared in tritium-labeled form by catalytic hydrogenation of the corresponding propenoic acid derivative 8 with tritium gas. The radioligand [(3)H]PSB-12150 (9) was obtained with a specific activity of 17 Ci/mmol (629 GBq/mmol). It showed specific and saturable binding to a single binding site in membrane preparations from Chinese hamster ovary cells recombinantly expressing the human GPR17. A competition assay procedure was established, which allows the determination of ligand binding affinities.
authors.affiliation: PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn , Bonn, Germany.
authors.forename: Meryem
authors.initials: M
authors.lastname: Köse
authors.affiliation: PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn , Bonn, Germany.
authors.forename: Kirsten
authors.initials: K
authors.lastname: Ritter
authors.affiliation: PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn , Bonn, Germany.
authors.forename: Katharina
authors.initials: K
authors.lastname: Thiemke
authors.affiliation: UCB Pharma S.A. , CNS Research, Chemin du Foriest, B-1420 Braine-l'Alleud, Belgium.
authors.forename: Michel
authors.initials: M
authors.lastname: Gillard
authors.affiliation: PharmaCenter Bonn, Institute of Pharmaceutical Biology, Section of Molecular-, Cellular-, and Pharmacobiology, University of Bonn , Bonn, Germany.
authors.forename: Evi
authors.initials: E
authors.lastname: Kostenis
authors.affiliation: PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn , Bonn, Germany.
authors.forename: Christa E
authors.initials: CE
authors.lastname: Müller
keywords: MDL29,951; montelukast; multiple sclerosis; nucleotide; orphan GPCR; pranlukast; radioligand