REVIEW KI16425 is a Lysophosphatidic acid receptor antagonist with selectivity for LPA1 and LPA3. At 10 µM, it significantly blocks the response of a variety of cancer cell lines to LPA-induced cell migration. Ki16425 inhibits the LPA-induced Ca(2+) response in THP-1 cells, 3T3 fibroblasts and A431 cells, and also inhibited LPA-induced long-term responses, including DNA synthesis and cell migration. Significantly, Ki16425 also reduced the NGF-induced stimulation of p42/p44 MAPK and inhibited NGF-stimulated neurite outgrowth.
Ma, Lin; Matsumoto, Misaki; Xie, Weijiao; Inoue, Makoto; Ueda, Hiroshi. Evidence for lysophosphatidic acid 1 receptor signaling in the early phase of neuropathic pain mechanisms in experiments using Ki-16425, a lysophosphatidic acid 1 receptor antagonist. Journal of Neurochemistry. (2009) 109(2): 603-610.
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Ueno, Akihiro; Nagao, Rika; Watanabe, Tomoko; Ohta, Hideo; Yagi, Mikio Preparation of novel isoxazoles and thiazoles as LPA receptor antagonists and use thereof as remediesPCT Int. Appl. (2001), WO 2001060819 A1 20010823
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