Development of [3H] 2-Carboxy-4, 6-dichloro-1 H-indole-3-propionic Acid ([3H] PSB-12150): A Useful Tool for Studying GPR17

…, K Ritter, K Thiemke, M Gillard, E Kostenis…

文献索引：Koese, Meryem; Ritter, Kirsten; Thiemke, Katharina; Gillard, Michel; Kostenis, Evi; Mueller, Christa E. ACS Medicinal Chemistry Letters, 2014 , vol. 5, # 4 p. 326 - 330

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被引用次数: 2

摘要

The recently described synthetic GPR17 agonist 2-carboxy-4, 6-dichloro-1 H-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 [3H] 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 ...