Synthesis of GR 125487, a selective 5-HT₄ receptor antagonist

The 5-HT₄ receptor (5-HT₄R) agonists are important in treating gastrointestinal motility disorders. Their role is currently being evaluated for the treatment of cognitive and mood disorders. A selective 5-HT₄R antagonist GR 125487 is used in many biological assays to cross confirm the 5-HT₄R agonist’s activity. A practical synthesis of GR 125487 is developed so as to have it in desired quantities. The synthesis consists of seven steps starting from commercially available methyl 5-fluoroindole 3-carboxylate. The GR 125487 thus synthesized was used in blocking the activity of 5-HT₄R agonist compound in animal models of cognition.5-羟色胺4受体（5-HT₄ receptor，简称5-HT₄R）激动剂在胃肠道动力障碍的治疗中具有重要应用价值。目前，这类激动剂用于认知与情感障碍治疗的潜力正被广泛评估。选择性5-羟色胺4受体拮抗剂GR 125487被广泛应用于多种生物学实验，用于交叉验证5-HT₄R激动剂的活性。为获取足量的GR 125487，研究人员开发了一套实用的合成路线：该路线以市售的5-氟吲哚-3-甲酸甲酯为起始原料，共包含7步反应。所合成得到的GR 125487可用于在认知功能动物模型中阻断5-HT₄R激动剂的活性。

搜集汇总

背景与挑战

背景概述

该数据集详细描述了选择性5-HT4受体拮抗剂GR 125487的合成方法，包括七个步骤的实用合成过程，起始原料为商业可得的甲基5-氟吲哚-3-羧酸酯。GR 125487用于生物测定中以确认5-HT4受体激动剂活性，并在认知障碍的动物模型中应用，属于生物化学、药理学和神经科学领域的研究数据。