UCM-05194 (ammonium salt)

UCM-05194 is an agonist of lysophosphatidic acid receptor 1 (LPA₁).¹ It induces calcium mobilization in RH7777 cells expressing LPA₁ (EC₅₀ = 0.24 µM). It is selective for LPA₁ over LPA₂ and LPA₃ at 10 µM and is 10-fold selective over LPA₅ and 50-fold selective over LPA₄, LPA₆, and autotaxin. UCM-05194 (1 µM) 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 µM and reduces the firing activity of primary rat neonatal dorsal root ganglia (DRG) neurons with repeated application at 10 µM. UCM-05194 (10 mg/kg) reduces acetic acid-induced writhing and hind paw mechanical hypersensitivity in mice.

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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 amelioration. J. Med. Chem. 63(5), 2372-2390 (2020).