Camilla Lundkvist

Karolinska Institutet

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Christer Halldin

Karolinska Institutet

Lars Farde

Karolinska Institutet

Carl‐Gunnar Swahn

Karolinska Institutet

Nathalie Ginovart

University of Geneva

Victor W. Pike

National Institute of Mental Health

Julie A. McCarron

National Institutes of Health

Kjell Någren

Odense Municipality

Håkan Hall

Weatherford College

Johan Sandell

University of Pittsburgh

Per Karlsson

University of Gothenburg

Cooperative Institutions

Karolinska Institutet

Karolinska University Hospital

Hammersmith Hospital

Commissariat à l'Énergie Atomique et aux Énergies Alternatives

Kuopio University Hospital

Institut d'Imagerie Biomédicale

Inserm

University of Helsinki

Cyclotron (Netherlands)

University of Eastern Finland

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[ 11 C]PE2I: a highly selective radioligand for PET examination of the dopamine transporter in monkey and human brain

European Journal of Nuclear Medicine and Molecular Imaging (2003)

Christer Halldin Nina Erixon-Lindroth Stefan Pauli Yuan-Hwa Chou Yoshiro Okubo

Radioligand

Binding potential

Radioligand Assay

10.1007/s00259-003-1212-3

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Citations (107)

Development of PET Radioligands for the Quantitation of Serotonin Receptors in the Human Brain

Springer eBooks (1998)

Christer Halldin Lars Farde Camilla Lundkvist Hiroshi Ito Nathalie Ginovart

Radioligand

Human brain

10.1007/978-94-011-4996-9_7

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Citations (0)

[11C]?-CIT-FE, a radioligand for quantitation of the dopamine transporter in the living brain using positron emission tomography

Synapse (1996)

Christer Halldin Lars Farde Camilla Lundkvist Nathalie Ginovart Yoshifumi Nakashima

The cocaine analogue β-CIT-FE (N-(2-fluoroethyl)-2β-carbomethoxy-3β-(4-iodophenyl)nortropane) was labeled with 11C for positron emission tomography (PET) studies of the dopamine transporter. After intravenous administration to a cynomolgus monkey, [11C]β-CIT-FE accumulated in the striatum with a striatum-to-cerebellum ratio of about 9 after 60 min. Pseudoequilibrium of specific [11C]β-CIT-FE binding in the striatum was obtained within 30–50 min. The radioactivity ratios of the thalamus to the cerebellum and the neocortex to the cerebellum were about 2 and 1.5, respectively. In displacement and pretreatment experiments, radioactivity in the striatum but not in the cerebellum was reduced after injection of β-CIT or the dopamine transporter inhibitor GBR 12909, indicating that striatal radioactivity following injection of [11C]β-CIT-FE represents reversible binding to dopamine transporter sites. After displacement or pretreatment with cocaine there was a marked effect not only in the striatum but also in the thalamus and neocortex. [11C]β-CIT-FE has potential as a useful PET radioligand for quantitation of the dopamine transporter in the primate brain in vivo. © 1996 Wiley-Liss, Inc.

Radioligand

10.1002/(sici)1098-2396(199604)22:4<386::aid-syn10>3.0.co;2-w

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Citations (89)

Improved syntheses of the PET radioligands, [11C]FLB 457, [11C]MDL 100907 and [11C]β-CIT-FE, by the use of [11C]methyl triflate

Journal of Labelled Compounds and Radiopharmaceuticals (1998)

Camilla Lundkvist Johan Sandell Kjell Någren Victor W. Pike Christer Halldin

The highly reactive labelling agent, [11C]methyl triflate, was used to synthesise three recently developed PET radioligands. The labelling reactions were 11C-methylations of phenols for the preparations of the D2 receptor radioligand, [11C]FLB 457, and the 5-HT2A receptor radioligand, [11C]MDL 100907, and 11C-methylation of a carboxylic acid for the preparation of the dopamine transporter radioligand, [11C]β-CIT-FE. The synthesis of the 5-HT1A receptor radioligand, [O-methyl-11C]WAY-100635, was used to establish general reaction conditions for the methylation of phenols with [11C]methyl triflate. Compared to the previous use of [11C]methyl iodide in these radiosyntheses, [11C]methyl triflate demanded less precursor, allowed faster reactions and improved radiochemical yields. Normal-phase HPLC was used to speed up product purifications (except for [11C]β-CIT-FE). Hence, preparation times were shorter, resulting in radioligands with higher specific radioactivity. © 1998 John Wiley & Sons, Ltd.

Radioligand

Methyl iodide

Trifluoromethanesulfonate

Radiosynthesis

Radioligand Assay

10.1002/(sici)1099-1344(199806)41:6<545::aid-jlcr99>3.3.co;2-z

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Characterization of C-11 or I-123 Labelled ?-CIT-FP and ?-CIT-FE Metabolism Measured in Monkey and Human Plasma. Identification of Two Labelled Metabolites with HPLC

Human Psychopharmacology Clinical and Experimental (1996)

Kim A. Bergstr�m Christer Halldin Camilla Lundkvist Carl-Gunnar Swahn Kari K. �kerman

β-CIT-FP and β-CIT-FE which are novel fluoroalkyl derivatives of 2β-carbomethoxy-3β-(4-iodophenyl)tropane (β-CIT), have recently been labelled with11C or123I and used for imaging the dopamine transporter with positron emission tomography (PET) or single photon emission tomography (SPET). The metabolite pattern of these novel tracers was studied with HPLC in plasma in monkeys and in urine and plasma in humans. Four labelled metabolites were found of which two were identified, the123I-labelled free acid and11C- or123I-labelled nor-β-CIT. The latter was detected only in small amounts (<4 per cent). Furthermore, a polar metabolite and an unknown lipophilic11C- or123I-labelled metabolite were found. The amount of this unidentified labelled metabolite of [11C]β-CIT-FP or [11C]β-CIT-FE in monkey plasma was 21±8 per cent and 16±9 per cent at 60 min after injection, respectively. In conclusion, four types of labelled metabolites were found after injection of11C- or123I-labelled β-CIT-FP and β-CIT-FE in monkeys and humans of which one may hamper the quantitation of the dopamine transporter by PET or SPET.

Tropane

10.1002/(sici)1099-1077(199611)11:6<483::aid-hup818>3.0.co;2-9

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Citations (24)

Preparation of [18F]β-CFT-FP and [11C]β-CFT-FP, selective radioligands for visualisation of the dopamine transporter using positron emission tomography (PET)

Journal of Labelled Compounds and Radiopharmaceuticals (2000)

Eeva‐Liisa Kämäräinen Teija Kyllönen Anu J. Airaksinen Camilla Lundkvist Meixiang Yu

In this study the N-fluoropropyl analogue of the cocaine congener β-CFT (I), N-(3-fluoropropyl)-2β-carbomethoxy-3β-(4-fluorophenyl)nortropane (β-CFT-FP, III), was labelled with 18F or 11C. Syntheses of the precursors nor-β-CFT (II) and β-CFT-FP acid (IV) as well as III itself are described. [18F]β-CFT-FP was prepared starting from I using two different labelling reagents: [18F]fluoropropyl bromide (V) and [18F]fluoropropyl tosylate (VI). A reversed-phase HPLC system proved to be effective in separating the labelled product from precursor II. The radiochemical incorporation of V or VI to yield [18F]β-CFT-FP (18F-III) was in general 30–50% and the radiochemical purity was higher than 99%. [11C]β-CFT-FP (11C-III) was synthesised by esterification of IV using [11C]methyl triflate (VII). An HPLC-purification system using a reversed-phase column proved to be effective in separating the product from the acid precursor. The radiochemical yield starting from [11C]carbon dioxide was 30–40% and the radiochemical purity was better than 99%. 18F-III and 11C-III have potential as radioligands for visualisation of the dopamine transporter (DAT) using Positron Emission Tomography (PET). Copyright © 2000 John Wiley & Sons, Ltd.

Trifluoromethanesulfonate

10.1002/1099-1344(20001030)43:12<1235::aid-jlcr411>3.0.co;2-9

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Citations (21)

Autoradiographic localization of 5-HT2A receptors in the human brain using [3H]M100907 and [11C]M100907

Synapse (2000)

H�kan Hall Lars Farde Christer Halldin Camilla Lundkvist G�ran Sedvall

M100907 (MDL 100907, R-(+)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol) is a new selective antagonist of 5-HT2A receptors. The compound has been labeled with 11C and proved useful for in vivo studies of 5-HT2A receptors using positron emission tomography (PET). In the present study the distribution of 5-HT2A receptors was examined in the postmortem human brain using whole hemisphere autoradiography and [3H]M100907 and [11C]M100907. The autoradiograms showed very dense binding to all neocortical regions, whereas the hippocampus was only weakly labeled with [3H]M100907. Other central brain regions, such as the basal ganglia and thalamus, showed low [3H]M100907 binding, reflecting low densities of 5-HT2A receptors. The cerebellum or structures of the brain stem were virtually devoid of 5-HT2A receptors. [11C]M100907 gave images qualitatively similar to those of [3H]M100907, although with lower spatial resolution. The labeling of human 5-HT2A receptors with [3H]M100907 was inhibited by the addition of the 5-HT2A receptor blockers ketanserin or SCH 23390 (10 μM), leaving a very low background of nonspecific binding. The 5-HT1A receptor antagonist WAY-100635 and the D2-dopamine receptor antagonist raclopride had no effect on the binding of [3H]M100907. The selective labeling of 5-HT2A receptors with [3H]M100907 clearly shows that this compound is suitable for further studies of the human 5-HT2A receptor subtype in vitro. The in vitro autoradiography of the distribution of 5-HT2A receptors obtained with radiolabeled M100907 provides detailed qualitative and quantitative information on the distribution of 5-HT2A-receptors in the human brain as well as reference information for the interpretation of previous initial results at much lower resolution in humans in vivo with PET and [11C]M100907. Synapse 38:421–431, 2000. © 2000 Wiley-Liss, Inc.

Ketanserin

Raclopride

Human brain

10.1002/1098-2396(20001215)38:4<421::aid-syn7>3.0.co;2-x

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Citations (124)

Different brain radioactivity curves in a PET study with [11C]β-CIT labelled in two different positions

Nuclear Medicine and Biology (1999)

Camilla Lundkvist Christer Halldin Carl‐Gunnar Swahn Nathalie Ginovart Lars Farde

10.1016/s0969-8051(98)00111-5

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Citations (20)