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 ?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).