A deeper understanding of the pharmacokinetic and pharmacodynamic properties of a drug candidate is a pivotal component of drug discovery and development. Autoradiography, is an excellent technique allowing exploiting the advantages of the use of radioisotopes in the drug discovery field. The introduction of phosphor imaging technology has revolutionized the handling of drug distribution studies providing high-resolution images. Specifically, quantitative whole body autoradioluminography (QWBA) is employed for preclinical study where the aim is to obtain information about the route of elimination and tissue distribution of a drug candidate. Autoradioluminography is also the technique of choice pursued to deal with all the issue that it is possible to encounter in all stage of drug development (i.e: site-specific drug localization and retention, drug-drug interactions, penetration into specific target, specific tissue binding, crossing of brain blood barrier, placental transfer. The purpose of this review is to give a picture of how autoradiography is employed in our laboratory as a key tool for advances in the assessment of the drug disposition and to validate new experimental models.

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放射自显影，一种强大而可靠的药物开发工具：Accelera 的经验

深入了解候选药物的药代动力学和药效学特性是药物发现和开发的关键组成部分。放射自显影是一项出色的技术，可以利用放射性同位素在药物发现领域的优势。荧光粉成像技术的引入彻底改变了提供高分辨率图像的药物分布研究的处理方式。具体而言，定量全身放射自显影 (QWBA) 用于临床前研究，其目的是获取有关候选药物的消除途径和组织分布的信息。放射自显影也是处理药物开发所有阶段可能遇到的所有问题的首选技术（即：特定部位的药物定位和保留，药物相互作用，渗透到特定靶点，特定组织结合，脑血屏障穿越，胎盘转移。本综述的目的是描述我们实验室如何将放射自显影作为药物处置评估进展和验证新实验模型的关键工具。