Title of article
Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2
Author/Authors
Trond Ulven، نويسنده , , Michael J. Gallen، نويسنده , , Mads C. Nielsen، نويسنده , , Nicole Merten، نويسنده , , Carola Schmidt، نويسنده , , Klaus Mohr، نويسنده , , Christian Tr?nkle، نويسنده , , Evi Kostenis، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
5924
To page
5927
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 [3H]TRQ11238 represents the first selective CRTH2 antagonist radioligand and exhibited a specific radioactivity of 52 Ci/mmol and a pKd of 9.0.
Keywords
DP2 , prostaglandin D2 , 7TM receptor , GPCR , Radioligand , CRTh2 , Antagonist
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798723
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