Synthesis, radiolabeling and preliminary biological evaluation of radiolabeled 5-methyl-6-nitroquipazine, a potential radioligand for the serotonin transporter

Johan Sandell; Meixiang Yu; Patrick Emond; Lucette Garreau; Sylvie Chalon; Kjell Någren; Denis Guilloteau; Christer Halldin

doi:10.1016/S0960-894X(02)00787-4

Synthesis, radiolabeling and preliminary biological evaluation of radiolabeled 5-methyl-6-nitroquipazine, a potential radioligand for the serotonin transporter

Johan Sandell, Meixiang Yu, Patrick Emond, Lucette Garreau, Sylvie Chalon, Kjell Någren, Denis Guilloteau, Christer Halldin

Research output: Contribution to journal › Article › peer-review

19 Scopus citations

Abstract

5-Methyl-6-nitroquipazine, a novel analogue of the potent and selective serotonin transporter inhibitor 6-nitroquipazine was synthesized and radiolabeled with tritium and the positron emitter carbon-11. [³H]5-methyl-6-nitroquipazine was found to have a K_d=51±7 pM. The high affinity and the facile labeling of [¹¹C]5-methyl-6-nitroquipazine makes it a promising radioligand for visualization of the serotonin transporter with positron emission tomography.

Original language	English (US)
Pages (from-to)	3611-3613
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	12
Issue number	24
DOIs	https://doi.org/10.1016/S0960-894X(02)00787-4
State	Published - Dec 2002

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0960-894X(02)00787-4

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Sandell, J., Yu, M., Emond, P., Garreau, L., Chalon, S., Någren, K., Guilloteau, D., & Halldin, C. (2002). Synthesis, radiolabeling and preliminary biological evaluation of radiolabeled 5-methyl-6-nitroquipazine, a potential radioligand for the serotonin transporter. Bioorganic and Medicinal Chemistry Letters, 12(24), 3611-3613. https://doi.org/10.1016/S0960-894X(02)00787-4

Synthesis, radiolabeling and preliminary biological evaluation of radiolabeled 5-methyl-6-nitroquipazine, a potential radioligand for the serotonin transporter. / Sandell, Johan; Yu, Meixiang; Emond, Patrick et al.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 12, No. 24, 12.2002, p. 3611-3613.

Research output: Contribution to journal › Article › peer-review

Sandell, J, Yu, M, Emond, P, Garreau, L, Chalon, S, Någren, K, Guilloteau, D & Halldin, C 2002, 'Synthesis, radiolabeling and preliminary biological evaluation of radiolabeled 5-methyl-6-nitroquipazine, a potential radioligand for the serotonin transporter', Bioorganic and Medicinal Chemistry Letters, vol. 12, no. 24, pp. 3611-3613. https://doi.org/10.1016/S0960-894X(02)00787-4

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title = "Synthesis, radiolabeling and preliminary biological evaluation of radiolabeled 5-methyl-6-nitroquipazine, a potential radioligand for the serotonin transporter",

abstract = "5-Methyl-6-nitroquipazine, a novel analogue of the potent and selective serotonin transporter inhibitor 6-nitroquipazine was synthesized and radiolabeled with tritium and the positron emitter carbon-11. [3H]5-methyl-6-nitroquipazine was found to have a Kd=51±7 pM. The high affinity and the facile labeling of [11C]5-methyl-6-nitroquipazine makes it a promising radioligand for visualization of the serotonin transporter with positron emission tomography.",

author = "Johan Sandell and Meixiang Yu and Patrick Emond and Lucette Garreau and Sylvie Chalon and Kjell N{\aa}gren and Denis Guilloteau and Christer Halldin",

note = "Funding Information: The authors would like to thank Mr G{\"o}ran Printz and Mr Christer Dupuis for assistance with the radionuclide production, and Mr Arsalan Amir for technical assistance. This work was supported by grants from the Swedish Medical Research Council (12983-02B), the Region Centre (France), the French Ministry of Research and Technology, COST B12 Action, and Karolinska institutet.",

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doi = "10.1016/S0960-894X(02)00787-4",

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AU - Yu, Meixiang

AU - Emond, Patrick

AU - Garreau, Lucette

AU - Chalon, Sylvie

AU - Någren, Kjell

AU - Guilloteau, Denis

AU - Halldin, Christer

N1 - Funding Information: The authors would like to thank Mr Göran Printz and Mr Christer Dupuis for assistance with the radionuclide production, and Mr Arsalan Amir for technical assistance. This work was supported by grants from the Swedish Medical Research Council (12983-02B), the Region Centre (France), the French Ministry of Research and Technology, COST B12 Action, and Karolinska institutet.

PY - 2002/12

Y1 - 2002/12

N2 - 5-Methyl-6-nitroquipazine, a novel analogue of the potent and selective serotonin transporter inhibitor 6-nitroquipazine was synthesized and radiolabeled with tritium and the positron emitter carbon-11. [3H]5-methyl-6-nitroquipazine was found to have a Kd=51±7 pM. The high affinity and the facile labeling of [11C]5-methyl-6-nitroquipazine makes it a promising radioligand for visualization of the serotonin transporter with positron emission tomography.

AB - 5-Methyl-6-nitroquipazine, a novel analogue of the potent and selective serotonin transporter inhibitor 6-nitroquipazine was synthesized and radiolabeled with tritium and the positron emitter carbon-11. [3H]5-methyl-6-nitroquipazine was found to have a Kd=51±7 pM. The high affinity and the facile labeling of [11C]5-methyl-6-nitroquipazine makes it a promising radioligand for visualization of the serotonin transporter with positron emission tomography.

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Synthesis, radiolabeling and preliminary biological evaluation of radiolabeled 5-methyl-6-nitroquipazine, a potential radioligand for the serotonin transporter

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