Human 5HT 1E Serotonin Receptor Drug Development (RMI)

人类 5HT 1E 血清素受体药物开发 (RMI)

• 批准号: 7057555
• 负责人: Milton Teitler
• 金额: $ 0.47万
• 依托单位: ALBANY MEDICAL COLLEGE
• 依托单位国家: 美国
• 财政年份: 2005
• 资助国家: 美国
• 起止时间: 2005-09-15 至 2006-09-14
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7057555
• 关键词: cell line; combinatorial chemistry; drug design /synthesis /production; forskolin; high throughput technology; neurotransmitter agonist; radiotracer; receptor expression; serotonin inhibitor; serotonin receptor; technology /technique development

DESCRIPTION (provided by applicant): The 5HT1E serotonin receptor is one of fourteen serotonin receptors expressed in humans. It is especially highly expressed in human cortical brain tissue, indicating modulation of this receptor by drugs may produce robust effects on cognition and/or mood. There has been surprisingly little information on the inherent function of this receptor, presumably due to the lack of selective drugs to stimulate or antagonize the 5HT1E receptor. In order to advance the field of 5HT1E receptor pharmacology we propose to develop a high throughput screen (NTS) for selective agonists and antagonists for the human 5HT1E receptor. The specific aims of this proposal are to demonstrate that the recombinant cell line possesses the properties that will allow the application of HTS using SPA (Scintillation Proximity Assays) to the development of novel, specific agonists and antagonists for this understudied human brain serotonin receptor. Selective agonists and antagonists for the 5HT1E receptor should, at the least, provide information on the function of this highly expressed receptor, and may lead to novel therapeutics for brain dysfunction.

描述（由申请人提供）：5 HT 1 E 5-羟色胺受体是人类表达的14种5-羟色胺受体之一。它在人类皮质脑组织中特别高表达，表明药物对这种受体的调节可能对认知和/或情绪产生强烈影响。令人惊讶的是，关于这种受体的固有功能的信息很少，可能是由于缺乏刺激或拮抗5 HT 1 E受体的选择性药物。为了推进5 HT 1 E受体药理学领域，我们建议开发用于人5 HT 1 E受体的选择性激动剂和拮抗剂的高通量筛选（NTS）。本提案的具体目的是证明重组细胞系具有允许使用SPA（闪烁邻近测定）应用HTS开发这种未充分研究的人脑5-羟色胺受体的新型特异性激动剂和拮抗剂的特性。5 HT 1 E受体的选择性激动剂和拮抗剂至少应该提供关于这种高表达受体的功能的信息，并且可能导致脑功能障碍的新疗法。