Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2
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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 Udgivelsesdato: 2007-Nov-1
| Original language | English |
|---|---|
| Journal | Bioorganic & Medicinal Chemistry Letters |
| Volume | 17 |
| Issue number | 21 |
| Pages (from-to) | 5924-5927 |
| Number of pages | 4 |
| ISSN | 0960-894X |
| DOIs | |
| Publication status | Published - 1 Nov 2007 |
- Drug Evaluation, Preclinical, Indoles, Radioligand Assay, Receptors, Immunologic, Receptors, Prostaglandin, Sulfonamides
Research areas
ID: 189158552