دورية
Identification of a Potent and Selective Synthetic Agonist at the CRTH2 Receptor
| العنوان: | Identification of a Potent and Selective Synthetic Agonist at the CRTH2 Receptor |
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| المؤلفون: | Gervais, François G., Morello, Jean-Pierre, Beaulieu, Christian, Sawyer, Nicole, Denis, Danielle, Greig, Gillian, Malebranche, A. Daniel, O'Neill, Gary P. |
| المصدر: | Molecular Pharmacology; June 2005, Vol. 67 Issue: 6 p1834-1839, 6p |
| مستخلص: | The chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells (CRTH2) is a G protein-coupled receptor whose function in vivo has been incompletely characterized. One of the reasons is that its current known ligands, prostaglandin D2 and some of its metabolites, have either poor selectivity for CRTH2 or are metabolically unstable in vivo. In this study, we describe the biological and pharmacological properties of L-888,607, the first synthetic potent and selective CRTH2 agonist. We show that L-888,607 exhibits 1) subnanomolar affinity for the human CRTH2 receptor, 2) high selectivity over all other prostanoid receptors and other receptors tested, 3) agonistic activity on recombinant and endogenously expressed CRTH2 receptor, and 4) relative stability in vivo. L-888,607 thus represents a suitable tool to investigate the in vivo function of CRTH2. |
| قاعدة البيانات: | Supplemental Index |
| تدمد: | 0026895X 15210111 |
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