[O-methyl-11C]β-CIT-FP, a potential radioligand for quantitation of the dopamine transporter: Preparation, autoradiography, metabolite studies, and positron emission tomography examinations

Lundkvist, Camilla; Halldin, Christer; Swahn, Carl‐Gunnar; Hall, Håkan; Karlsson, Per; Nakashima, Yoshifumi; Wang, Shaoyin; Milius, Richard A.; Neumeyer, John L.; Farde, Lars

doi:10.1016/0969-8051(95)00029-w

Cited by 61 publications

(37 citation statements)

References 22 publications

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“…To date, FP-b-CIT studies with PET have only been analysed using simple radioactivity ratios at a fixed time interval after bolus injection (Lundkvist et al, 1995(Lundkvist et al, , 1997Ma et al, 2002), or using plasma and reference tissue input Logan based linearized methods (Kazumata et al, 1998;Logan et al, 1990Logan et al, , 1996. Although more comprehensive tracer kinetic models are available (Gunn et al, 2001), they have not been evaluated for quantification of FP-b-CIT data.…”

Section: Introductionmentioning

confidence: 99%

Quantification of Dopamine Transporter Binding Using [¹⁸F]FP-β-CIT and Positron Emission Tomography

Yaqub

Boellaard

Berckel

et al. 2006

J Cereb Blood Flow Metab

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The purpose of this study was to compare different kinetic and semi-quantitative methods for analysing human [18 F]FP-b-CIT studies: plasma input models, simplified (SRTM) and full (FRTM) reference tissue models, standard uptake values (SUV) and SUV ratios (SUVr). Both simulations and clinical evaluations were performed to determine the effects of noise, scan duration and blood volume on Akaike model selection, and on precision and accuracy of estimated parameters. For typical noise levels (COVB2.5%) and scan durations ( < 90 mins), simulations provided poor fits (Akaike criterion) in case of reversible plasma input models showing a relatively high number of outliers compared with the two-tissue irreversible model. Reference tissue models provided more reliable fits, which were nearly independent of noise and scan duration. For clinical data, two tissue irreversible and reversible plasma input models fitted striatum curves equally well (Akaike criterion). BP with plasma input models were less precise and contained more outliers than BP obtained with SRTM or FRTM. Among all methods tested, SRTM showed the highest contrast between patients and controls. When differentiating between patients and controls, SUVr performed almost equally well as SRTM, although contrast between striatum and background was lower. In conclusion, SRTM provided BP estimates with the highest precision and accuracy. Moreover, SRTM provided good contrast between patients and controls, and between striatum and background. SRTM is therefore the method of choice for quantitative [18 F]FP-b-CIT studies. SUVr might be an alternative for larger clinical trials.

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Section: Introductionmentioning

confidence: 99%

Quantification of Dopamine Transporter Binding Using [¹⁸F]FP-β-CIT and Positron Emission Tomography

Yaqub

Boellaard

Berckel

et al. 2006

J Cereb Blood Flow Metab

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“…56 However, the exchange between methyl iodide and silver triflate does not always seem to be complete, as the reported conversion yields imply. Recently, in an automated synthesis of [C-11]-raclopride (26, 1500-2000 Ci mmol…”

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confidence: 89%

Isotopic methylation

Bolton

2001

Labelled Comp Radiopharmac

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SummaryThis review reports recent methods by which organic compounds, and especially pharmaceuticals, have been isotopically labelled by the incorporation of carbon or hydrogen isotopes in methylation processes. Particular attention is paid to the incorporation of carbon-11; both the synthesis of such labelled methylating agents and applications of their use are discussed. The review has reported reagents and conditions by which a number of organic compounds have been obtained recently. It also assesses the limitations of reported methods and proposes some alternative techniques and innovations.The application of catalysts such as Ag + and conditions such as microwave irradiation to encourage these reactions are also included, with suggestions of other, potentially beneficial, ways to assist them. In many cases, the radio-chemical yield and purity of the labelled product are given along with an estimate of the total reaction time.

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“…18 Both are potent GAT-1 inhibitors (IC 50 values for inhibition of [ 3 H]GABA uptake of 0.13 and 0.26 mM) compared to GAT-3 inhibition (1990 and 333 mM, respectively). 18 Until now, no information is available about the analogous binding characteristics of the 11 C-and 18 F-labelled derivatives of SK&F 89976A 9 and CI-966. 6 However, 11 C-methylation of SK&F 89976A 9 or the exchange of the guvacine structure element with nipecotic acid in the case of CI-966 6 for example, not necessarily influence the subtype specificity of the ligands.…”

mentioning

confidence: 96%

“…Still, DAT-ligands provide valuable additional tools for quantifying dopaminergic function in vivo. [6][7][8][9][10][11] GABA is synthesised in vivo via enzymatic decarboxylation of glutamate, stored in vesicles and finally released into the synaptic cleft where it interacts with GABA A and GABA B receptors. Its action is terminated by high-affinity transporters.…”

mentioning

confidence: 99%

Radiosynthesis of (±)‐(2‐((4‐(2‐[¹⁸F]fluoro‐ethoxy)phenyl)bis(4‐methoxy‐phenyl)methoxy)ethylpiperidine‐3‐carboxylic acid: a potential GAT‐3 PET ligand to study GABAergic neuro‐transmission in vivo

Schirrmacher

Hamkens

Piel

et al. 2001

Labelled Comp Radiopharmac

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[O-methyl-11C]β-CIT-FP, a potential radioligand for quantitation of the dopamine transporter: Preparation, autoradiography, metabolite studies, and positron emission tomography examinations

Cited by 61 publications

References 22 publications

Quantification of Dopamine Transporter Binding Using [¹⁸F]FP-β-CIT and Positron Emission Tomography

Quantification of Dopamine Transporter Binding Using [¹⁸F]FP-β-CIT and Positron Emission Tomography

Isotopic methylation

Radiosynthesis of (±)‐(2‐((4‐(2‐[¹⁸F]fluoro‐ethoxy)phenyl)bis(4‐methoxy‐phenyl)methoxy)ethylpiperidine‐3‐carboxylic acid: a potential GAT‐3 PET ligand to study GABAergic neuro‐transmission in vivo

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[O-methyl-11C]β-CIT-FP, a potential radioligand for quantitation of the dopamine transporter: Preparation, autoradiography, metabolite studies, and positron emission tomography examinations

Cited by 61 publications

References 22 publications

Quantification of Dopamine Transporter Binding Using [18F]FP-β-CIT and Positron Emission Tomography

Quantification of Dopamine Transporter Binding Using [18F]FP-β-CIT and Positron Emission Tomography

Isotopic methylation

Radiosynthesis of (±)‐(2‐((4‐(2‐[18F]fluoro‐ethoxy)phenyl)bis(4‐methoxy‐phenyl)methoxy)ethylpiperidine‐3‐carboxylic acid: a potential GAT‐3 PET ligand to study GABAergic neuro‐transmission in vivo

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Quantification of Dopamine Transporter Binding Using [¹⁸F]FP-β-CIT and Positron Emission Tomography

Quantification of Dopamine Transporter Binding Using [¹⁸F]FP-β-CIT and Positron Emission Tomography

Radiosynthesis of (±)‐(2‐((4‐(2‐[¹⁸F]fluoro‐ethoxy)phenyl)bis(4‐methoxy‐phenyl)methoxy)ethylpiperidine‐3‐carboxylic acid: a potential GAT‐3 PET ligand to study GABAergic neuro‐transmission in vivo