UCM-05194 is an agonist of lysophosphatidic acid receptor 1 (LPA1).1 It induces calcium mobilization in RH7777 cells expressing LPA1 (EC50 = 0.24 ?M). It is selective for LPA1 over LPA2 and LPA3 at 10 ?M and is 10-fold selective over LPA5 and 50-fold selective over LPA4, LPA6, and autotaxin. UCM-05194 (1 ?M) induces neurite retraction in, and migration of, B103 rat neuroblastoma cells overexpressing LPA1. It induces receptor internalization and neuronal desensitization in the same cells when used at a concentration of 1 ?M and reduces the firing activity of primary rat neonatal dorsal root ganglia (DRG) neurons with repeated application at 10 ?M. UCM-05194 (10 mg/kg) reduces acetic acid-induced writhing and hind paw mechanical hypersensitivity in mice.
References:
[1]. González-Gil, I., Zian, D., Vázquez-Villa, H., et al.A novel agonist of the type 1 lysophosphatidic acid receptor (LPA1), UCM-05194, shows efficacy in neuropathic pain ameliorationJ. Med. Chem.63(5)2372-2390(2020).