[11C]MDL 100907, a radioligand for selective imaging of 5-HT2A receptors with positron emission tomography
1996; Elsevier BV; Volume: 58; Issue: 10 Linguagem: Inglês
10.1016/0024-3205(96)00013-6
ISSN1879-0631
AutoresCamilla Lundkvist, Christer Halldin, Nathalie Ginovart, Svante Nyberg, Carl‐Gunnar Swahn, Albert A. Carr, Françoise Brunner, Lars Farde,
Tópico(s)Neuroscience and Neuropharmacology Research
ResumoThe highly selective 5-HT2A receptor antagonist, MDL 100907 ((R)-(+)-4 -(l-hydroxy-1-(2,3-dimethoxyphenyl)methyl)-N -2-(4-fluorophenylethyl)piperidine), was labeled with 11C for Positron Emission Tomography (PET) studies. After i.v. injection of (R)-(+)-[3-OCH3-11C]MDL 100907 [11C]MDL 100907) in Cynomolgus monkeys a marked accumulation in the 5-HT2A receptor rich neocortical regions was obtained with a neocortex to cerebellum ratio of 3.5-4.5 after 60-80 minutes. In the neocortical regions a transient equilibrium occurred within 40-60 minutes. Radioactivity in the neocortex, but not in the cerebellum, was reduced after injection of ketanserin, indicating that neocortical radioactivity following injection of [11C]MDL 100907 represents specific binding to 5-HT2A receptors. There was no evident effect on neocortical binding after pretreatment with raclopride or SCH 23390. [11C]MDL 100907 has potential to become the first selective radioligand for PET-quantitation of 5-HT2A receptors in the human brain in vivo.
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