caa a22 4500 469120061 CHVBK 20180323133136.0 cr unu---uuuuu 170328e19920701xx s 000 0 eng 10.1007/BF02245279 doi (NATIONALLICENCE)springer-10.1007/BF02245279 [11C]Ro 15-4513, a ligand for visualization of benzodiazepine receptor binding [Elektronische Daten] Preparation, autoradiography and positron emission tomography [Christer Halldin, Lars Farde, Jan-Eric Litton, Håkan Hall, Göran Sedvall] Ro 15-4513, a partial inverse agonist at the benzodiazepine (BZ) receptor site was labelled with11C and used for in vitro autoradiography on human post mortem brain sections and for positron emission tomography (PET) on Cynomolgus monkeys. The total radiochemical yield of [11C]Ro 15-4513 was 30-40% with an overall synthesis time of 40 min. The specific radioactivity was about 1000 Ci/mmol at end of synthesis. In vitro autoradiography showed that [11C]Ro 15-4513 bound specifically predominately in the neocortex of the human brain. Specific binding was also demonstrated in the basal ganglia and the cerebellar cortex. Flumazenil (Ro 15-1788) and clonazepam inhibited the binding in cerebral regions, but a significant proportion in the cerebellum was not inhibited by these agents. This proportion may represent α6-containing BZ receptors. PET examination of [11C]Ro 15-4513 binding in Cynomolgus monkeys demonstrated high uptake of radioactivity in neocortex. The uptake of radioactivity was markedly displaced by high doses of Ro 15-4513 or clonazepam. [11C]Ro 15-4513 should be a useful ligand to examine BZ receptor characteristics in the living human brain by PET. Springer-Verlag, 1992 Benzodiazepine receptors nationallicence Ro 15-4513 nationallicence 11C nationallicence Positron emission tomography nationallicence PET nationallicence In vitro autoradiography nationallicence Monkey brain nationallicence Human brain nationallicence Halldin Christer Department of Psychiatry and Psychology, Karolinska Hospital, S-10401, Stockholm, Sweden aut Farde Lars Department of Psychiatry and Psychology, Karolinska Hospital, S-10401, Stockholm, Sweden aut Litton Jan-Eric Department of Psychiatry and Psychology, Karolinska Hospital, S-10401, Stockholm, Sweden aut Hall Håkan Department of Psychiatry and Psychology, Karolinska Hospital, S-10401, Stockholm, Sweden aut Sedvall Göran Department of Psychiatry and Psychology, Karolinska Hospital, S-10401, Stockholm, Sweden aut Psychopharmacology Springer-Verlag 108/1-2(1992-07-01), 16-22 0033-3158 108:1-2<16 1992 108 213 https://doi.org/10.1007/BF02245279 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF02245279 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Halldin Christer Department of Psychiatry and Psychology, Karolinska Hospital, S-10401, Stockholm, Sweden aut NATIONALLICENCE 700 1- Farde Lars Department of Psychiatry and Psychology, Karolinska Hospital, S-10401, Stockholm, Sweden aut NATIONALLICENCE 700 1- Litton Jan-Eric Department of Psychiatry and Psychology, Karolinska Hospital, S-10401, Stockholm, Sweden aut NATIONALLICENCE 700 1- Hall Håkan Department of Psychiatry and Psychology, Karolinska Hospital, S-10401, Stockholm, Sweden aut NATIONALLICENCE 700 1- Sedvall Göran Department of Psychiatry and Psychology, Karolinska Hospital, S-10401, Stockholm, Sweden aut NATIONALLICENCE 773 0- Psychopharmacology Springer-Verlag 108/1-2(1992-07-01), 16-22 0033-3158 108:1-2<16 1992 108 213 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer