To date, six types of receptors, LPA1-6 have been identified and are responsible for most of the biological activities of LPA. Recent studies on gene targeting in mice and family diseases of these receptors revealed that LPA is involved in various patho-physiological states. LPA antagonists have attracted considerable attention and numerous small molcules having LPA antagonistic activity have been reported. Ki16425 is an antagonist of LPA1 and LPA3 receptors with moderate activity against LPA2.
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1. Hideo Ohta, et al “Ki16425, a Subtype-Selective Antagonist for EDG-Family Lysophosphatidic Acid Receptors” Molecular Pharmacology, 2003, 166(4), 994-10052. Jing Zhao, et al “Lysophosphatidic Acid Receptor 1 antagonist Ki16425 Blunts Abdominal and Systemic Inflammation in a Mouse Model of Peritoneal Sepsis” Translational Research, 2015, 166(1), 80–88