CORE--BIOLOGY

核心--生物学

• 批准号: 5207162
• 负责人: URSULA SCHEFFEL
• 金额: --
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/5207162
• 关键词: Rodentias; autoradiography; baboons; biomedical facility; chemical kinetics; iodine; ligands; microdialysis; neurotoxins; nuclear medicine; pharmacokinetics; positron emission tomography; radiation dosage; 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 以及在此程序中准备的新配体和放射性示例的验证 项目，用于对配体的药代动力学评估 器官剂量计计算，并协助准备 医师赞助的新药应用研究（IND）。 具体而言，生物学核心测试已知受体结合的类似物 使用体外结合测定法进行受体亲和力，密度和 特异性；表演体外受体放射自显影 确定其区域分布的放射线；测试 已知受体配体的放射性标记类似物的体内 分布并结合啮齿动物的大脑中的各种受体， 狒狒，并将其与放射性标记的父型化合物进行比较（当 可用的）;在药理学上验证示踪剂作为A的配体 特定的结合位点；检查体内代谢 放射性示例，并确定啮齿动物的整个身体生物分布 进行人类研究所需的辐射剂量估计值。