human biodistribution and dosimetry of 11c-cumi-101, an agonist radioligand for serotonin-1a receptors in brain人类biodistribution和剂量测定法101年11 c - cumi serotonin-1a的受体激动剂放射性配体受体在大脑.pdfVIP

human biodistribution and dosimetry of 11c-cumi-101, an agonist radioligand for serotonin-1a receptors in brain人类biodistribution和剂量测定法101年11 c - cumi serotonin-1a的受体激动剂放射性配体受体在大脑.pdf

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human biodistribution and dosimetry of 11c-cumi-101, an agonist radioligand for serotonin-1a receptors in brain人类biodistribution和剂量测定法101年11 c - cumi serotonin-1a的受体激动剂放射性配体受体在大脑

Human Biodistribution and Dosimetry of 11C-CUMI-101, an Agonist Radioligand for Serotonin-1A Receptors in Brain Christina S. Hines, Jeih-San Liow, Paolo Zanotti-Fregonara, Jussi Hirvonen, Cheryl Morse, Victor W. Pike, Robert B. Innis* Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland, United States of America Abstract As a reported agonist,11C-CUMI-101 is believed to selectively bind the G-protein-coupled state of the serotonin-1A (5- HT1A) receptor, thereby providing a measure of the active subset of all 5-HT1A receptors in brain. Although 11C-CUMI-101 has been successfully used to quantify 5-HT1A receptors in human and monkey brain, its radiation exposure has not previously been reported. The purpose of this study was to calculate the radiation exposure to organs of the body based on serial whole-body imaging with positron emission tomography (PET) in human subjects. Methods: Nine healthy volunteers were injected with 428684 MBq (mean 6 SD) 11C-CUMI-101 and then imaged with a PET-only device for two hours from head to mid-thigh. Eleven source organs (brain, heart, liver, pancreas, stomach, spleen, lungs, kidneys, lumbar spine L1-5, thyroid, and urinary bladder) were identified on whole body images and used to calculate radiation doses using the software program OLINDA/EXM 1.1. To confirm that we had correctly identified the pancreas, a tenth subject was imaged on a PET/CT device. Results: Brain had high uptake (,11% of injected activity (IA)) at 10 min. Although liver had the highest uptake (,35% IA at 120 min), excretion of this activity was not visible in gall bladder or intestine during the scanning session. Organs which received the highest doses (microSv/MBq) were pancreas (32.0), liver (18.4), and spleen (14.5). The effective dose of 11C- CUMI-101 was 5.3 60.5 microSv/MBq.

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