Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2 |
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Authors: | Ulven Trond Gallen Michael J Nielsen Mads C Merten Nicole Schmidt Carola Mohr Klaus Tränkle Christian Kostenis Evi |
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Affiliation: | Department of Physics and Chemistry, University of Southern Denmark, Campusvej 55, DK-5230 Odense M, Denmark. |
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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. |
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