This talk focuses on advancing biomedical imaging sciences, a cornerstone for translating pre-clinical discoveries to clinical applications, by developing targeted probes and therapeutics for central nervous system (CNS) disorders and oncology. It leverages in vivo Positron Emission Tomography (PET) and in vitro quantitative autoradiography to drive innovation, with key highlights: a novel autoradiography method to precisely quantify dopamine D2/D3 receptor density ratios, establishing sigma-2 receptor as a reliable imaging biomarker for cell proliferation, and developing its antagonists to mitigate Aβ oligomer toxicity in human neurons for Alzheimer’s therapy, plus insights into cutting-edge pre-clinical research integrating quantitative imaging, biochemistry, radiomics and proteomics to accelerate disease diagnosis and treatment progress.