CORE--BIOLOGY

核心--生物学

• 批准号: 6410203
• 负责人: URSULA SCHEFFEL
• 金额: $ 22.84万
• 依托单位: JOHNS HOPKINS UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2001
• 资助国家: 美国
• 起止时间: 2001-01-01 至 2002-12-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6410203
• 关键词: autoradiography; baboons; biomedical facility; brain imaging /visualization /scanning; laboratory mouse; laboratory rat; ligands; microdialysis; pharmacokinetics; positron emission tomography; radionuclides; radiopharmacology; radiotracer; receptor binding; technetium; tissue /cell culture

The biology core is responsible for in vivo and in vitro characterization and validation of new ligands and radiotracers prepared in this program project, for carrying out pharmacokinetic evaluation of the ligands for organ dosimetry calculations, and for assisting with the preparation of physician-sponsored Investigation of New Drug applications (IND's). Specifically, the biology core tests analogs of known receptor binding compounds using in vitro binding assays for receptor affinity, density, and specificity; performs in vitro receptor autoradiography with promising radioligands to determine their regional distribution; tests the radiolabeled analogs of known receptor ligands for their in vivo distribution and binding to various receptors in the brains of rodents and baboons, and compares them with their radiolabeled parent compounds (when available); validates pharmacologically the tracer as a ligand for a particular binding site; examines the in vivo metabolism of the radiotracers, and determines the whole body biodistribution in rodents to make radiation dose estimates which are necessary for human studies.

生物学核心负责体内和体外表征 并验证本计划中制备的新配体和放射性示踪剂 项目，用于进行药物代谢动力学评价的配体， 器官剂量计算，并协助准备 医生申办的新药申请研究（IND）。 具体来说，生物学核心测试已知受体结合的类似物， 使用体外结合试验测定化合物的受体亲和力、密度和 特异性;进行体外受体放射自显影， 放射性配体，以确定其区域分布;测试 已知受体配体的放射性标记的类似物，用于其体内 分布和结合到啮齿动物脑中的各种受体， 狒狒，并将它们与它们的放射性标记的母体化合物（当 可用）;验证示踪剂是否作为 特定的结合位点;检查体内代谢的 放射性示踪剂，并确定啮齿动物的全身生物分布， 进行人体研究所需的辐射剂量估算。