Synthesis and preliminary biological evaluation of radiolabeled 5-BDBD analogs as new candidate PET radioligands for P2X4 receptor

• Published in: Bioorganic & medicinal chemistry Vol. 25; no. 14; pp. 3835 - 3844
• Main Authors: Wang, Min, Gao, Mingzhang, Meyer, Jill A., Peters, Jonathan S., Zarrinmayeh, Hamideh, Territo, Paul R., Hutchins, Gary D., Zheng, Qi-Huang
• Format: Journal Article
• Language: English
• Published: OXFORD Elsevier Ltd 15.07.2017; Elsevier
• Subjects: Adenosine Triphosphate - chemistry; Adenosine Triphosphate - metabolism; Azirines - chemical synthesis; Azirines - chemistry; Azirines - metabolism; Binding, Competitive; Biochemistry & Molecular Biology; Carbon Radioisotopes - chemistry; Chemistry; Chemistry, Medicinal; Chemistry, Organic; Competitive binding assay; Dihydropyridines - chemical synthesis; Dihydropyridines - chemistry; Dihydropyridines - metabolism; Fluorine Radioisotopes - chemistry; HEK293 Cells; Humans; Isotope Labeling; Life Sciences & Biomedicine; P2X4 receptor; Pharmacology & Pharmacy; Physical Sciences; Positron emission tomography (PET); Positron-Emission Tomography; Protein Binding; Radiolabeled 5-BDBD analogs; Radioligand depletion experiment; Radiopharmaceuticals - chemical synthesis; Radiopharmaceuticals - chemistry; Radiopharmaceuticals - metabolism; Radiosynthesis; Receptors, Purinergic P2X4 - chemistry; Receptors, Purinergic P2X4 - genetics; Receptors, Purinergic P2X4 - metabolism; Recombinant Proteins - biosynthesis; Recombinant Proteins - chemistry; Science & Technology; Competitive binding assay; Positron emission tomography (PET); Radiolabeled 5-BDBD analogs; Radioligand depletion experiment; P2X4 receptor; Radiosynthesis; AGENT; 1ST RADIOSYNTHESIS; BROMINATION; FULLY AUTOMATED SYNTHESIS; TAU TRACER; PURINERGIC RECEPTORS

[Display omitted] P2X4 receptor has become an interesting molecular target for treatment and PET imaging of neuroinflammation and associated brain diseases such as Alzheimer’s disease. This study reports the first design, synthesis, radiolabeling and biological evaluation of new candidate PET P2X4 r...