CORE--BIOLOGY

生物核心负责体内和体外的表征 以及本计划中制备的新的配体和放射性示踪剂的验证 项目，对以下配体进行药代动力学评估 器官剂量学计算，并协助准备 医生赞助的新药申请调查(IND)。 具体地说，生物核心测试已知受体结合的类似物 使用体外结合试验测定受体亲和力、密度和 特异性；进行体外受体放射自显影，前景看好 放射性配基以确定其区域分布；测试 放射性标记的已知受体配体在体内的类似物 啮齿类动物脑内各种受体的分布和结合 并将它们与其放射性标记的母体化合物(当 可用)；从药理上验证示踪剂作为一种 特定的结合部位；检查体内的代谢 放射性示踪剂，并测定啮齿类动物的全身生物分布 进行人体研究所需的辐射剂量估算。

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.