AS-2717638 is a lysophosphatidic acid receptor 5 (LPA5) antagonist (IC50 = 0.038 ?M).1 It is selective for LPA5 over LPA1, LPA2, and LPA3 (IC50s = >10 ?M for all) but also binds to adenosine A1 and μ-opioid receptors at 10 ?M. It induces analgesia in a rat model of allodynia induced by LPA or geranylgeranyl pyrophosphate when administered at doses of 3, 10, and 30 mg/kg. AS-2717638 (10 and 30 mg/kg) inhibits allodynia induced by prostaglandin E2 , PGF2α, or AMPA in rats. It increases the paw withdrawal threshold and latency in the von Frey hair and plantar tests, respectively, in rats when administered at a dose of 10 mg/kg.
1.Murai, N., Hiyama, H., Kiso, T., et al.Analgesic effects of novel lysophosphatidic acid receptor 5 antagonist AS2717638 in rodentsNeuropharmacology12697-107(2017)