A comparison of the brain uptake of N-(cyclopropyl[11C]methyl)norbuprenorphine ([11C]buprenorphine) and N-(cyclopropyl[11C]methyl)nordiprenorphme ([11C]diprenorphine) in baboon using PET |
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| Affiliation: | 1. Chemistry Department, Brookhaven National Laboratory, Upton, NY 11973, U.S.A.;2. Visiting Scholar from the Institute of Atomic Energy, Beijing, People''s Republic of China;3. Visiting Scholar from the Institute of Modern Physics, Academia Sinica, Lanzhou, People''s Republic of China;4. Department of Psychiatry, New York University Medical Center, New York, NY 10016, U.S.A.;1. Departamento de Morfología y Biología Celular, Grupo SINPOS, Universidad de Oviedo, Spain;2. Servicio de Anatomía Patológica, Complejo Asistencial Universitario de Salamanca, Salamanca, Spain;3. Facultad de Ciencias de la Salud, Universidad Autónoma de Chile, Chile;1. Department of Children Health Care, Children’s Hospital, Zhejiang University School of Medicine, Hangzhou, 310003, China;2. Institute of Neuroscience, School of Medicine, Zhejiang University, Hangzhou, 310058, China;3. Department of Neurology, Children’s Hospital, Zhejiang University School of Medicine, Hangzhou, 310003, China;1. Department of Neuropaediatrics, Developmental Neurology, Social Paediatrics, University Children''s Hospital Tübingen, Germany;2. Department of Medical Genetics and Applied Genomics, University of Tübingen, Germany;3. Rare Disease Center Tübingen, University of Tübingen, Germany;4. Clinic for Paediatric Nephrology, Hepatology and Metabolic Disorders, Hannover Medical School, Carl-Neuberg-Strasse 1, 30625 Hannover, Germany;5. Institute of Clinical Genetics, University of Dresden, Germany;1. Department of Psychology, University of Maryland, College Park, MD 20742, USA;2. Department of Electrical and Computer Engineering, University of Maryland, College Park, MD 20742, USA |
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| Abstract: | Buprenorphine and diprenorphine were radiolabeled with 11C and their distributions in the baboon brain were studied using positron emission tomography (PET). Specific binding was demonstrated in the striatum (but not in the cerebellum) by pretreating the baboon with (−)naloxone. The absolute striatal uptakes and time courses were similar for these two radioligands but the ratio of radioactivity in the striatum to cerebellum in the baboon was higher for [11C]diprenorphine than for [11C]buprenorphine. Analysis of baboon plasma indicated that both [11C]diprenorphine and [11CJbuprenorphine are rapidly metabolized. Analysis of radioactivity in mouse brain indicated that these two radioligands are stable to metabolic transformation. At 30 min after injection, 86–90% of extracted radioactivity was due to unchanged 11C-labeled radioligands. These results suggest that both [11C]diprenorphine and [11C]buprenorphine may be useful radioligands for studying opioid receptors in humans, although [11C]diprenorphine may be a better radioligand than [11C]buprenorphine for this purpose because of its more rapid clearance from the cerebellum. |
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