LPA5 antagonist 2 (compound 65) is a high aqueous solubility LPA5 (lysophosphatidic acid receptor 5) antagonist. LPA5 antagonist 2 significantly attenuates nociceptive persensitivity and it can be used for the research of inflammatory and neuropathic pains.
LPA5 antagonist 2 (0-10 μM) inhibits hLPA5 calcium mobilization with an IC50 value of 69 nM and inhibits hLPA5 cAMP with an IC50 value of 340 nM[1].LPA5 antagonist 2 (0-10 μM) shows no significant affinity for other receptors, exhibits good target selectivity for LPA5[1].
LPA5 antagonist 2 (5.3-17.8 mg/kg; i.p. once) alleviates CFA-induced inflammatory pain in vivo[1].
References:
[1]. Zhang DH, et al. Isoquinolone derivatives as lysophosphatidic acid receptor 5 (LPA5) antagonists: Investigation of structure-activity relationships, ADME properties and analgesic effects. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. 2022.