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: 7399724
• 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 2009-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7399724
• 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; Mental Depression; 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; diencephalon; human study; 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)：本研究项目的目标是在人类身上验证一种与5-羟色胺转运体具有皮摩尔亲和力的新配体。它将允许通过单光子发射断层扫描(SPECT)成像来定量测量活体大脑中的5-HTT位点。已知5-羟色胺转运体在几个生理和病理生理过程中发挥关键作用，包括抑郁、焦虑、季节性情感障碍、暴食症和精神病，尸检数据、影响这个靶点的治疗的临床疗效和成像研究证明了这一点。一种与5-HTT特异结合的放射性示踪剂在这些疾病的诊断、监测、治疗和研究中非常有用。需要更好的示踪剂，以便在大脑皮质等5-HTT密度较低的区域进行定量。