PET imaging of central 5-HT(2A) receptors with carbon-11-MDL 100,907

Journal of Nuclear Medicine

Volumn 39, Issue 1, 1998, Pages 208-214

  Ito, Hiroshi ^a   Nyberg, Svante ^a   Halldin, Christer ^a   Lundkvist, Camilla ^a   Farde, Lars ^a  

^a KAROLINSKA UNIVERSITY HOSPITAL   (Sweden)

Author keywords

Brain; PET; Schizophrenia; Serotonergic receptor

Indexed keywords

ALPHA (2,3 DIMETHOXYPHENYL) 1 [2 (4 FLUOROPHENYL)ETHYL] 4 PIPERIDINEMETHANOL; CARBON 11; METHYL IODIDE; NEUROLEPTIC AGENT; RADIOLIGAND; SEROTONIN 2A ANTAGONIST; SEROTONIN 2A RECEPTOR;

ADULT; ARTICLE; COMPARTMENT MODEL; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; HUMAN; HUMAN EXPERIMENT; INTRAVENOUS DRUG ADMINISTRATION; LIGAND BINDING; MALE; NEOCORTEX; NORMAL HUMAN; NUCLEAR MAGNETIC RESONANCE IMAGING; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; RADIOISOTOPE DISTRIBUTION; RECEPTOR DENSITY; RECEPTOR OCCUPANCY; SCHIZOPHRENIA;

ADULT; BRAIN; CARBON RADIOISOTOPES; FLUOROBENZENES; HUMANS; MALE; PIPERIDINES; RADIOPHARMACEUTICALS; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTORS, SEROTONIN; SCHIZOPHRENIA; SEROTONIN ANTAGONISTS; TOMOGRAPHY, EMISSION-COMPUTED;

EID: 0031930011     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (37)

1. Meltzer HY. Clinical studies on the mechanism of action of clozapine: the dopamine-serotonin hypothesis of schizophrenia. Psychopharmacology 1989;99(suppl):S18-S27.
2. Csernansky JG, Poscher M, Faull KF. Serotonin in schizophrenia. In: Coccaro EF, Murphy DL, eds. Serotonin in major psychiatric disorders. Washington, DC: American Psychiatric Press; 1990:209-230.
3. 2A receptors in antipsychotic activity. Life Sci 1995;56:2209-2222.
4. 2 receptor and alpha 1-adrenoreceptor antagonism. J Clin Psychopharmacol 1995;15:11S-18S.
5. Wong DF, Wagner HN Jr, Dannals RF, et al. Effects of age on dopamine and serotonin receptors measured by positron tomography in the living human brain. Science 1984;226:1393-1396.
6. 2 dopamine receptor occupancy in the living human brain. A PET study with risperidone. Psychopharmacology 1993;110:265-272.
7. 18F-labeled setoperone. J Neurochem 1990;54:1744-1754.
8. 2 receptors in humans using positron emission tomography. Eur J Nucl Med 1994;21:937-946.
9. 2 serotonin receptors in cerebral cortex. J Neurosci 1986;6:2941-2949.
10. 2 antidopaminergic activity of alkylating and nonalkylating derivatives of spiperone in rat brain. Mol Pharmacol 1992;42:856-863.
11. 2 receptor antagonist MDL 100907 as a putative atypical antipsychotic: behavioral, electrophysiological and neurochemical studies. J Pharmacol Exp Ther 1993;266:684-691.
12. 2A receptor antagonist, MDL 100,907, increases dopamine efflux in the prefrontal cortex of the rat. Eur J Pharmacol 1995;273:273-279.
13. 2A antagonist with a favorable CNS safety profile. J Pharmacol Exp Ther 1996;277:968-981.
14. 2A receptors with positron emission tomography. Life Sci 1996;58:PL187-PL192.
15. Wienhard K, Dahlbom M, Eriksson L, et al. The ECAT EXACT HR: performance of a new high resolution positron scanner. J Comput Assist Tomogr 1994;18:110-118.
16. Bergström M, Boethius J, Eriksson L, Greitz T, Ribbe T, Widen L. Head fixation device for reproducible position alignment in transmission CT and positron emission tomography. J Comput Assist Tomogr 1981;5:136-141.
17. Eriksson L, Holte S, Bohm C, Kesselberg M, Hovander B. Automatic blood sampling systems for positron emission tomography. IEEE Trans Nucl Sci 1988;35:703-707.
18. 11C]raclopride binding to D2-dopamine receptors studied by PET: a comparison to the equilibrium analysis. J Cereb Blood Flow Metab 1989;9:696-708.
19. 11C]SCH23390. Identification of two radiolabelled metabolites with HPLC. Hum Psychopharmacol 1994;9:25-31.
20. Halldin C, Swahn C-G, Farde L, Sedvall G. Radioligand disposition and metabolism: key information in early drug development. In: Comer D, ed. PET for drug development and evaluation. Dordrecht, The Netherlands: Kluwer Academic Publisher; 1995:55-65.
21. Mintun MA, Raichle ME, Kilbourn MR, Wooten GF, Welch MJ. A quantitative model for the in vivo assessment of drug binding sites with positron emission tomography. Ann Neurol 1984;15:217-227.
22. Huang SC, Barrio JR, Phelps ME. Neuroreceptor assay with positron emission tomography: equilibrium versus dynamic approaches. J Cereb Blood Flow Metab 1986;6:515-521.
23. Wong DF, Gjedde A, Wagner HN Jr. Quantification of neuroreceptors in the living human brain. I. Irreversible binding of ligands. J Cereb Blood Flow Metab 1986;6: 137-146.
24. 123I]iomazenil binding to benzodiazepine receptors in nonhuman primates: I. Kinetic modeling of single bolus experiments. J Cereb Blood Flow Metab 1994;14:439-452.
25. Marquardt D. An algorithm for least-squares estimation of nonlinear parameters. J Soc Ind Appl Math 1963;11:431-441.
26. Onishi Y, Yonekura Y, Mukai T, et al. Simple quantification of benzodiazepine receptor binding and ligand transport using iodine-123-iomazenil and two SPECT scans. J Nucl Med 1995;36:1201-1210.
27. 2-receptors in human brain. Brain Res 1983;276:231-235.
28. 2 recognition sites. Brain Res 1986;376:97-107.
29. Pazos A, Probst A, Palacios JM. Serotonin receptors in the human brain-IV. Autoradiographic mapping of serotonin-2 receptors. Neuroscience 1987;21:123-139.
30. Akaike H. A new look at the statistical model identification. IEEE Trans Automat Contr 1974;19:716-723.
31. Schwarz G. Estimating the dimension of a model. Ann Stat 1978;6:461-464.
32. Hawkins RA, Phelps ME, Huang SC. Effects of temporal sampling, glucose metabolic rates, and disruptions of the blood-brain barrier on the FDG model with and without a vascular compartment: studies in human brain tumors with PET. J Cereb Blood Flow Metab 1986;6:170-183.
33. 11C]aminocyclohexanecarboxylate for the measurement of amino acid uptake and distribution volume in human brain. J Cereb Blood Flow Melab 1990;10:727-739.
34. Leenders KL, Perani D, Lammertsma AA, et al. Cerebral blood flow, blood volume and oxygen utilization. Normal values and effect of age. Brain 1990;113:27-47.
35. 11C-methyl]-(-)-cocaine PET studies in human subjects. J Cereb Blood Flow Metab 1990;10:740-747.
36. 2 receptor sites on human blood platelets. Biochem Pharmacol 1984;33:2807-2811.
37. 18F]setoperone. Brain 1993;116:497-510.