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Titolo:
[C-11] MDL-100907, A RADIOLIGAND FOR SELECTIVE IMAGING OF 5-HT2A RECEPTORS WITH POSITRON EMISSION TOMOGRAPHY
Autore:
LUNDKVIST C; HALLDIN C; GINOVART N; NYBERG S; SWAHN CG; CARR AA; BRUNNER F; FARDE L;
Indirizzi:
KAROLINSKA INST,KAROLINSKA HOSP,DEPT CLIN NEUROSCI,SECT PSYCHIAT S-17176 STOCKHOLM SWEDEN HOECHST MARION ROUSSEL INC CINCINNATI OH 00000 HOECHST MARION ROUSSEL,CLIN PHARMACOL CH-8320 FEHRALTORF SWITZERLAND
Titolo Testata:
Life sciences
fascicolo: 10, volume: 58, anno: 1996,
pagine: 187 - 192
SICI:
0024-3205(1996)58:10<187:[MARFS>2.0.ZU;2-#
Fonte:
ISI
Lingua:
ENG
Soggetto:
LIVING HUMAN-BRAIN; SEROTONIN RECEPTORS; PET; 5-HT(2); AFFINITY; BINDING;
Keywords:
SEROTONIN RECEPTORS; MDL 100907; POSITRON EMISSION TOMOGRAPHY; MONKEY BRAIN;
Tipo documento:
Letter
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
21
Recensione:
Indirizzi per estratti:
Citazione:
C. Lundkvist et al., "[C-11] MDL-100907, A RADIOLIGAND FOR SELECTIVE IMAGING OF 5-HT2A RECEPTORS WITH POSITRON EMISSION TOMOGRAPHY", Life sciences, 58(10), 1996, pp. 187-192

Abstract

The highly selective 5-HT2A receptor antagonist, MDL 100907 enyl)methyl)-N-2-(4-fluorophenylethyl)piperidine), was labeled with C-11 for Positron Emission Tomography (PET) studies. After i.v. injection of (R)-(+)-[3-OCH3-C-11]MDL 100907 ([C-11]MDL 100907) in Cynomolgus monkeys amarked 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 occured 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 [C-11]MDL 100907 represents specific binding to 5-HT2A receptors. There was no evident effect on neocortical binding after pretreatment with raclopride or SCH 23390. [C-11]MDL 100907 has potential to become the first selective radioligand for PET-quantitation of 5-HT2A receptors in the human brain invivo.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 06/04/20 alle ore 09:20:33