Norcitalopram

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S.p. Hume - One of the best experts on this subject based on the ideXlab platform.

  • Citalopram: labelling with carbon-11 and evaluation in rat as a potential radioligand for in vivo PET studies of 5-HT re-uptake sites.
    International journal of radiation applications and instrumentation. Part B Nuclear medicine and biology, 1991
    Co-Authors: S.p. Hume, C. Pascali, Victor W. Pike, D. R. Turton, R. G. Ahier, Ralph Myers, D. M. Bateman, J. E. Cremer, Luisa G. Manjil, Raymond J. Dolan
    Abstract:

    Abstract In vivo autoradiography of [N-methly-3H]citalopram in rat brain shows a differential regional localization which correlates with the localization of 5-HT re-uptake binding sites defined in vitro. A comparison of the biodistribution of [N-mrthyl-3H]citalopram over 2 h after i.v. injection in (1) control rats (2) rats pre-dosed with either citalopram or paroxetine and (3) rats chemically-lesioned with p-chloroamphetamine provides an estimate of specific binding relative to total binding in vivo. The ratio of binding in certain regions (e.g. cingulate) to binding in a reference tissue (e,g, cerebellum) at 30–120 min post injection is c. 1.4. In view of these results a method was developed for labelling citalopram with carbon-11 ( t 1 2 = 20.3 min, β+ = 99.8%) to provide a potential radioligand for studies using positron emission tomography. Thus, reaction of nca [11C]iodomethane, prepared from cyclotron-produced [11C]carbon dioxide, with Norcitalopram in ethanol containing 2,2,6,6-tetramethyl-piperidine for 5 min at 95 °C gives crude [N-methyl-11C]citalopram in 60% radiochemical yield, decay-corrected. HPLC on silica gel provides radiochemically and chemically pure [N-methyl-11C]citalopram, as assessed by TLC, HPLC and MS. This product (isolated radiochemical yield, 49%) is easily formulated for i.v. injection. Up to 2GBq of formulated product with a specific activity of c. 15 GBq/μmol have been prepared within 40min from the end of radionuclide production. The described radiosynthesis has also been applied to give the single biologically active (+)-enantiomer of [N-methyl-11C]citalopram rather than the racemate. This product gives enhanced specific signal in the rat following i.v. injection, the ratio of uptake in regions of interest relative to cerebellum approaching 2 at 90 min.

C. Pascali - One of the best experts on this subject based on the ideXlab platform.

  • Citalopram: labelling with carbon-11 and evaluation in rat as a potential radioligand for in vivo PET studies of 5-HT re-uptake sites.
    International journal of radiation applications and instrumentation. Part B Nuclear medicine and biology, 1991
    Co-Authors: S.p. Hume, C. Pascali, Victor W. Pike, D. R. Turton, R. G. Ahier, Ralph Myers, D. M. Bateman, J. E. Cremer, Luisa G. Manjil, Raymond J. Dolan
    Abstract:

    Abstract In vivo autoradiography of [N-methly-3H]citalopram in rat brain shows a differential regional localization which correlates with the localization of 5-HT re-uptake binding sites defined in vitro. A comparison of the biodistribution of [N-mrthyl-3H]citalopram over 2 h after i.v. injection in (1) control rats (2) rats pre-dosed with either citalopram or paroxetine and (3) rats chemically-lesioned with p-chloroamphetamine provides an estimate of specific binding relative to total binding in vivo. The ratio of binding in certain regions (e.g. cingulate) to binding in a reference tissue (e,g, cerebellum) at 30–120 min post injection is c. 1.4. In view of these results a method was developed for labelling citalopram with carbon-11 ( t 1 2 = 20.3 min, β+ = 99.8%) to provide a potential radioligand for studies using positron emission tomography. Thus, reaction of nca [11C]iodomethane, prepared from cyclotron-produced [11C]carbon dioxide, with Norcitalopram in ethanol containing 2,2,6,6-tetramethyl-piperidine for 5 min at 95 °C gives crude [N-methyl-11C]citalopram in 60% radiochemical yield, decay-corrected. HPLC on silica gel provides radiochemically and chemically pure [N-methyl-11C]citalopram, as assessed by TLC, HPLC and MS. This product (isolated radiochemical yield, 49%) is easily formulated for i.v. injection. Up to 2GBq of formulated product with a specific activity of c. 15 GBq/μmol have been prepared within 40min from the end of radionuclide production. The described radiosynthesis has also been applied to give the single biologically active (+)-enantiomer of [N-methyl-11C]citalopram rather than the racemate. This product gives enhanced specific signal in the rat following i.v. injection, the ratio of uptake in regions of interest relative to cerebellum approaching 2 at 90 min.

Victor W. Pike - One of the best experts on this subject based on the ideXlab platform.

  • Citalopram: labelling with carbon-11 and evaluation in rat as a potential radioligand for in vivo PET studies of 5-HT re-uptake sites.
    International journal of radiation applications and instrumentation. Part B Nuclear medicine and biology, 1991
    Co-Authors: S.p. Hume, C. Pascali, Victor W. Pike, D. R. Turton, R. G. Ahier, Ralph Myers, D. M. Bateman, J. E. Cremer, Luisa G. Manjil, Raymond J. Dolan
    Abstract:

    Abstract In vivo autoradiography of [N-methly-3H]citalopram in rat brain shows a differential regional localization which correlates with the localization of 5-HT re-uptake binding sites defined in vitro. A comparison of the biodistribution of [N-mrthyl-3H]citalopram over 2 h after i.v. injection in (1) control rats (2) rats pre-dosed with either citalopram or paroxetine and (3) rats chemically-lesioned with p-chloroamphetamine provides an estimate of specific binding relative to total binding in vivo. The ratio of binding in certain regions (e.g. cingulate) to binding in a reference tissue (e,g, cerebellum) at 30–120 min post injection is c. 1.4. In view of these results a method was developed for labelling citalopram with carbon-11 ( t 1 2 = 20.3 min, β+ = 99.8%) to provide a potential radioligand for studies using positron emission tomography. Thus, reaction of nca [11C]iodomethane, prepared from cyclotron-produced [11C]carbon dioxide, with Norcitalopram in ethanol containing 2,2,6,6-tetramethyl-piperidine for 5 min at 95 °C gives crude [N-methyl-11C]citalopram in 60% radiochemical yield, decay-corrected. HPLC on silica gel provides radiochemically and chemically pure [N-methyl-11C]citalopram, as assessed by TLC, HPLC and MS. This product (isolated radiochemical yield, 49%) is easily formulated for i.v. injection. Up to 2GBq of formulated product with a specific activity of c. 15 GBq/μmol have been prepared within 40min from the end of radionuclide production. The described radiosynthesis has also been applied to give the single biologically active (+)-enantiomer of [N-methyl-11C]citalopram rather than the racemate. This product gives enhanced specific signal in the rat following i.v. injection, the ratio of uptake in regions of interest relative to cerebellum approaching 2 at 90 min.

D. R. Turton - One of the best experts on this subject based on the ideXlab platform.

  • Citalopram: labelling with carbon-11 and evaluation in rat as a potential radioligand for in vivo PET studies of 5-HT re-uptake sites.
    International journal of radiation applications and instrumentation. Part B Nuclear medicine and biology, 1991
    Co-Authors: S.p. Hume, C. Pascali, Victor W. Pike, D. R. Turton, R. G. Ahier, Ralph Myers, D. M. Bateman, J. E. Cremer, Luisa G. Manjil, Raymond J. Dolan
    Abstract:

    Abstract In vivo autoradiography of [N-methly-3H]citalopram in rat brain shows a differential regional localization which correlates with the localization of 5-HT re-uptake binding sites defined in vitro. A comparison of the biodistribution of [N-mrthyl-3H]citalopram over 2 h after i.v. injection in (1) control rats (2) rats pre-dosed with either citalopram or paroxetine and (3) rats chemically-lesioned with p-chloroamphetamine provides an estimate of specific binding relative to total binding in vivo. The ratio of binding in certain regions (e.g. cingulate) to binding in a reference tissue (e,g, cerebellum) at 30–120 min post injection is c. 1.4. In view of these results a method was developed for labelling citalopram with carbon-11 ( t 1 2 = 20.3 min, β+ = 99.8%) to provide a potential radioligand for studies using positron emission tomography. Thus, reaction of nca [11C]iodomethane, prepared from cyclotron-produced [11C]carbon dioxide, with Norcitalopram in ethanol containing 2,2,6,6-tetramethyl-piperidine for 5 min at 95 °C gives crude [N-methyl-11C]citalopram in 60% radiochemical yield, decay-corrected. HPLC on silica gel provides radiochemically and chemically pure [N-methyl-11C]citalopram, as assessed by TLC, HPLC and MS. This product (isolated radiochemical yield, 49%) is easily formulated for i.v. injection. Up to 2GBq of formulated product with a specific activity of c. 15 GBq/μmol have been prepared within 40min from the end of radionuclide production. The described radiosynthesis has also been applied to give the single biologically active (+)-enantiomer of [N-methyl-11C]citalopram rather than the racemate. This product gives enhanced specific signal in the rat following i.v. injection, the ratio of uptake in regions of interest relative to cerebellum approaching 2 at 90 min.

R. G. Ahier - One of the best experts on this subject based on the ideXlab platform.

  • Citalopram: labelling with carbon-11 and evaluation in rat as a potential radioligand for in vivo PET studies of 5-HT re-uptake sites.
    International journal of radiation applications and instrumentation. Part B Nuclear medicine and biology, 1991
    Co-Authors: S.p. Hume, C. Pascali, Victor W. Pike, D. R. Turton, R. G. Ahier, Ralph Myers, D. M. Bateman, J. E. Cremer, Luisa G. Manjil, Raymond J. Dolan
    Abstract:

    Abstract In vivo autoradiography of [N-methly-3H]citalopram in rat brain shows a differential regional localization which correlates with the localization of 5-HT re-uptake binding sites defined in vitro. A comparison of the biodistribution of [N-mrthyl-3H]citalopram over 2 h after i.v. injection in (1) control rats (2) rats pre-dosed with either citalopram or paroxetine and (3) rats chemically-lesioned with p-chloroamphetamine provides an estimate of specific binding relative to total binding in vivo. The ratio of binding in certain regions (e.g. cingulate) to binding in a reference tissue (e,g, cerebellum) at 30–120 min post injection is c. 1.4. In view of these results a method was developed for labelling citalopram with carbon-11 ( t 1 2 = 20.3 min, β+ = 99.8%) to provide a potential radioligand for studies using positron emission tomography. Thus, reaction of nca [11C]iodomethane, prepared from cyclotron-produced [11C]carbon dioxide, with Norcitalopram in ethanol containing 2,2,6,6-tetramethyl-piperidine for 5 min at 95 °C gives crude [N-methyl-11C]citalopram in 60% radiochemical yield, decay-corrected. HPLC on silica gel provides radiochemically and chemically pure [N-methyl-11C]citalopram, as assessed by TLC, HPLC and MS. This product (isolated radiochemical yield, 49%) is easily formulated for i.v. injection. Up to 2GBq of formulated product with a specific activity of c. 15 GBq/μmol have been prepared within 40min from the end of radionuclide production. The described radiosynthesis has also been applied to give the single biologically active (+)-enantiomer of [N-methyl-11C]citalopram rather than the racemate. This product gives enhanced specific signal in the rat following i.v. injection, the ratio of uptake in regions of interest relative to cerebellum approaching 2 at 90 min.