到目前为止,已经鉴定出六种类型的受体LPA 1 -6,它们负责LPA的大部分生物活性。近年来对小鼠基因靶向和这些受体家族疾病的研究表明,LPA参与了多种病理生理状态。LPA拮抗剂已经引起了相当大的关注,并且已经报道了许多具有LPA拮抗活性的小分子。Ki 16425是LPA 1和LPA 3受体的拮抗剂,对LPA 2具有中等活性。参考文献:由Bioz提供技术支持查看Bioz 1的更多详情。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“溶血磷脂酸受体1拮抗剂Ki 16425在腹膜脓毒症小鼠模型中阻断腹部和全身炎症”转化研究2015 166(1)80 - 88
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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.References: Powered by Bioz See more details on Bioz1. 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