Synthesis of GR 125487, a selective 5-HT4 receptor antagonist |
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Authors: | Ramakrishna Nirogi Shankar Reddy Gagginapally Anil K. Shinde |
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Affiliation: | Discovery Research, Suven Life Sciences Ltd., Hyderabad, India |
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Abstract: | 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. |
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Keywords: | Alzheimer’s disease animal models of cognition GR 125487 selective 5-HT4R antagonist |
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