Indole Analogs as Novel Appetite Suppressants

作为新型食欲抑制剂的吲哚类似物

• 批准号: 8010783
• 负责人: HOWARD P SARD
• 金额: $ 9.63万
• 依托单位: ORGANIX, INC.
• 依托单位国家: 美国
• 财政年份: 2010
• 资助国家: 美国
• 起止时间: 2010-01-20 至 2010-06-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8010783
• 关键词: Acute; Adverse effects; Affect; Agonist; American; Animal Model; Anti-Obesity Agents; Appetite Depressants; Award; Biodistribution; Biological; Biological Availability; Cell Nucleus; Chronic; Clinical; Desire for food; Development; Dexfenfluramine; Disease; Drug Kinetics; Epidemic; Evaluation; FDA approved; Felis catus; Fenfluramine; Goals; Grant; HTR2A gene; Health; Heart Valve Diseases; In Vitro; Indoles; Lead; Licensing; Lipase; Marketing; Meridia; Modification; Molecular; Mus; Norepinephrine; Obesity; Pancreas; Pharmaceutical Preparations; Pharmacologic Substance; Pharmacotherapy; Phase; Preparation; Program Development; Property; Protein Isoforms; Redux; Research; Resources; Selective Serotonin Reuptake Inhibitor; Serotonin Receptor 5-HT2B; Serotonin Receptor 5-HT2C; Site; Small Business Innovation Research Grant; Societies; Staging; Structure; Structure-Activity Relationship; Testing; Time; Toxic effect; United States; Weight; Withdrawal; Work; Xenical; analog; base; design; drug candidate; feeding; health economics; improved; in vivo; inhibitor/antagonist; inorganic phosphate; novel; obesity treatment; orlistat; programs; psilocin; receptor; receptor binding; sibutramine

DESCRIPTION (provided by applicant): Obesity affects millions of people in the U.S. and worldwide, and this disease has enormous health and economic consequences for our society. Existing treatments show limited efficacy, can possess troubling side effects, and often require long-term therapy. Discovery of a new treatment for obesity would have a very considerable scientific and commercial value. One approach to pharmacotherapy for appetite suppression is the development of 5-HT2C receptor agonists, which was the focus of our Phase One work. In Phase Two, we propose to optimize and further develop these leads through a Structure-Activity Relationship (SAR) program of synthesis and biological evaluation. From this project we specifically aim to discover one or more indole analogs showing efficacy in our animal model for appetite suppression that is equal to or better than approved medications. Such leads will also display favorable drug-like properties. The long-term goal of this project is to discover a new, improved pharmaceutical agent for treatment of obesity that can be licensed and developed for ultimate market approval. 7. Project Narrative Obesity is a serious health problem in the Unites States, and the existing drugs to help people lose weight are often not effective and have side effects. We are carrying out research to discover and develop a new drug for obesity. If we are successful, doctors will have another option to help obese people with their weight problem.

描述（由申请人提供）：肥胖会影响美国和世界范围内数以百万计的人，这种疾病对我们的社会产生了巨大的健康和经济后果。现有治疗方法显示有限的功效，可能具有令人不安的副作用，并且通常需要长期治疗。发现肥胖的新疗法将具有非常可观的科学和商业价值。抑制食欲的药物疗法的一种方法是开发5-HT2C受体激动剂，这是我们第一阶段工作的重点。在第二阶段，我们建议通过合成和生物学评估的结构 - 活性关系（SAR）计划来优化和进一步发展这些导线。从这个项目中，我们特别旨在发现一个或多个吲哚类似物在我们的动物模型中表现出对食欲抑制的功效，该抑制与批准的药物相同或更好。这样的潜在客户还将显示出有利的药物样特性。该项目的长期目标是发现一种新的，改进的药物治疗肥胖症，可以获得许可和开发以获得最终的市场认可。 7.项目叙述性肥胖是团结州的严重健康问题，现有的帮助人们减肥的药物通常无效并且有副作用。我们正在进行研究，以发现和开发一种用于肥胖症的新药。如果我们取得成功，医生将有另一种选择来帮助肥胖的人有自己的体重问题。