Initial Evaluation of an Adenosine A 2A Receptor Ligand, 11 C-Preladenant, in Healthy Human Subjects

• Published in: Journal of Nuclear Medicine Vol. 58; no. 9; pp. 1464 - 1470
• Main Authors: Sakata, Muneyuki, Ishibashi, Kenji, Imai, Masamichi, Wagatsuma, Kei, Ishii, Kenji, Zhou, Xiaoyun, de Vries, Erik F.J., Elsinga, Philip H., Ishiwata, Kiichi, Toyohara, Jun
• Format: Journal Article
• Language: English
• Published: United States 01.09.2017
• Subjects: Adult; Brain - diagnostic imaging; Brain - metabolism; Carbon Radioisotopes; Healthy Volunteers; Humans; Ligands; Male; Positron-Emission Tomography; Pyrimidines - adverse effects; Pyrimidines - metabolism; Pyrimidines - pharmacokinetics; Radiometry; Receptor, Adenosine A2A - metabolism; Safety; Tissue Distribution; Triazoles - adverse effects; Triazoles - metabolism; Triazoles - pharmacokinetics; Whole Body Imaging; Young Adult; human brain; 11C-preladenant; adenosine A2A receptor; positron emission tomography; radiation dosimetry

C-preladenant is a selective antagonist for mapping of cerebral adenosine A receptors (A Rs) by PET. This is a first-in-human study to examine the safety, radiation dosimetry, and brain imaging of C-preladenant in healthy human subjects. Dynamic C-preladenant PET scans (90 min) were obtained in 5 he...