rat lpa1

ASP6432 is an antagonist of type 1 lysophosphatidic acid receptor (LPA1). For human LPA1 and rat LPA1, the IC50s are 11 nM and 30 nM , respectively.

UCM-05194 (ammonium) is an agonist for the lysophosphatidic acid receptor 1 (LPA1). It induces calcium mobilization in RH7777 cells expressing LPA1, with an EC50 of 0.24 µM. In B103 rat neuroblastoma cells that overexpress LPA1, UCM-05194 (ammonium) promotes neurite retraction and cell migration. Additionally, it alleviates acetic acid-induced writhing and mechanical hyperalgesia in mice.

ONO-0300302 is a slow tight binding LPA1 antagonist (IC50: 0.16 nM) used to treat Benign Prostatic Hyperplasia. ONO-0300302 inhibits significantly an LPA-induced increase of intraurethral pressure (IUP) in rat (3 mg/kg, p.o.) and dog (1 mg/kg, p.o.) over