In vivo evaluation of a new ligand with picomolar affinity for the serotonin tran

对血清素反式具有皮摩尔亲和力的新配体的体内评价

• 批准号: 7547066
• 负责人: GILLES D TAMAGNAN
• 金额: $ 25万
• 依托单位: MOLECULAR NEUROIMAGING, LLC
• 依托单位国家: 美国
• 财政年份: 2008
• 资助国家: 美国
• 起止时间: 2008-01-01 至 2010-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7547066
• 关键词: Affect; Affinity; Anxiety; Area; Binding; Biodistribution; Blood - brain barrier anatomy; Brain; Brain imaging; Brain region; Bulimia; Clinical Data; Data; Diagnosis; Disease; Dose; Drug Kinetics; Evaluation; Goals; Human; Image; In Vitro; Life; Ligands; Measurement; Measures; Midbrain structure; Modeling; Monitor; Outcome; Papio; Pharmaceutical Preparations; Photons; Physiological; Play; Process; Psychotic Disorders; Research; Research Project Grants; Role; Seasonal Affective Disorder; Serotonin; Site; Structure-Activity Relationship; Tracer; Tropanes; base; clinical efficacy; density; depression; diencephalon; in vivo; monoamine; radiation absorbed dose; radiotracer; research study; response; serotonin transporter; single photon emission computed tomography; tomography; uptake

DESCRIPTION (provided by applicant): The goal of this research project is to validate in humans a new ligand with picomolar affinity for the serotonin transporter. It will permit quantitative measurement of serotonin transporter (5- HTT) sites in living brain by imaging with single photon emission tomography (SPECT). The serotonin transporter is known to play a critical role in several physiological and pathophysiological processes, including depression, anxiety, seasonal affective disorder, bulimia, and psychosis, as demonstrated by post-mortem data, clinical efficacy of therapies affecting this target site, and imaging studies. A radiotracer that binds specifically to 5-HTT is of great utility in diagnosis, monitoring treatment, and research of these disorders. There is a need for better tracers that allow quantitation in areas of the brain with low 5-HTT densities such as the cortex.

描述（由申请人提供）：本研究项目的目的是在人体中验证一种对5-羟色胺转运蛋白具有皮摩尔亲和力的新配体。它将允许定量测量5-羟色胺转运蛋白（5- HTT）的网站在活的大脑成像与单光子发射断层扫描（SPECT）。已知5-羟色胺转运蛋白在几种生理和病理生理过程中起关键作用，包括抑郁症、焦虑症、季节性情感障碍、贪食症和精神病，如尸检数据、影响该靶位点的治疗的临床疗效和成像研究所证明的。特异性结合5-HTT的放射性示踪剂在这些疾病的诊断、监测治疗和研究中具有很大的实用性。需要更好的示踪剂，其允许在具有低5-HTT密度的大脑区域（例如皮质）中进行定量。