Efficient synthesis and formulation of (R)-(-)-[11C]Deprenyl, a selective radioligand for the quantification of MAO-B activity using PET

Frédéric Dolle; Yann Bramoulle; Françoise Hinnen; Joanna S. Fowler

doi:10.1002/jlcr.604

Efficient synthesis and formulation of (R)-(-)-[¹¹C]Deprenyl, a selective radioligand for the quantification of MAO-B activity using PET

Frédéric Dolle, Yann Bramoulle, Françoise Hinnen, Joanna S. Fowler

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

13 Scopus citations

Abstract

Carbon-11 labeled (R)-(-)-Deprenyl is the tracer of reference for the quantification of monoamine oxidase (MAO)-B activity with PET. In this paper, its radiosynthesis is re-investigated and oriented towards the preparation of multi-milliCuries of radiotracer. Typically, using no-carrier-added [¹¹C]methyl triflate as the alkylating agent, 140-190 mCi (5.1-7.0 GBq) of (R)-(-)-[¹¹C]Deprenyl was obtained within 30 min of radiosynthesis (including HPLC purification and formulation) with specific radioactivities ranging from 0.8 to 1.2 Ci/μmol (29.644.4 GBq/μmol). The high efficiency of these radiosyntheses allows for multi-injection protocols and kinetic approaches for absolute quantification of the tracer.

Original language	English
Pages (from-to)	803-811
Number of pages	9
Journal	Journal of Labelled Compounds and Radiopharmaceuticals
Volume	45
Issue number	10
DOIs	https://doi.org/10.1002/jlcr.604
State	Published - Sep 2002
Externally published	Yes

Keywords

Carbon-11
Deprenyl
MAO
Monoamine oxidase
PET
Positron emission tomography

Access to Document

10.1002/jlcr.604

Cite this

@article{f86259ac845c40afa1b39e425f0d32e9,

title = "Efficient synthesis and formulation of (R)-(-)-[11C]Deprenyl, a selective radioligand for the quantification of MAO-B activity using PET",

abstract = "Carbon-11 labeled (R)-(-)-Deprenyl is the tracer of reference for the quantification of monoamine oxidase (MAO)-B activity with PET. In this paper, its radiosynthesis is re-investigated and oriented towards the preparation of multi-milliCuries of radiotracer. Typically, using no-carrier-added [11C]methyl triflate as the alkylating agent, 140-190 mCi (5.1-7.0 GBq) of (R)-(-)-[11C]Deprenyl was obtained within 30 min of radiosynthesis (including HPLC purification and formulation) with specific radioactivities ranging from 0.8 to 1.2 Ci/μmol (29.644.4 GBq/μmol). The high efficiency of these radiosyntheses allows for multi-injection protocols and kinetic approaches for absolute quantification of the tracer.",

keywords = "Carbon-11, Deprenyl, MAO, Monoamine oxidase, PET, Positron emission tomography",

author = "Fr{\'e}d{\'e}ric Dolle and Yann Bramoulle and Fran{\c c}oise Hinnen and Fowler, \{Joanna S.\}",

year = "2002",

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doi = "10.1002/jlcr.604",

language = "English",

volume = "45",

pages = "803--811",

journal = "Journal of Labelled Compounds and Radiopharmaceuticals",

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TY - JOUR

T1 - Efficient synthesis and formulation of (R)-(-)-[11C]Deprenyl, a selective radioligand for the quantification of MAO-B activity using PET

AU - Dolle, Frédéric

AU - Bramoulle, Yann

AU - Hinnen, Françoise

AU - Fowler, Joanna S.

PY - 2002/9

Y1 - 2002/9

N2 - Carbon-11 labeled (R)-(-)-Deprenyl is the tracer of reference for the quantification of monoamine oxidase (MAO)-B activity with PET. In this paper, its radiosynthesis is re-investigated and oriented towards the preparation of multi-milliCuries of radiotracer. Typically, using no-carrier-added [11C]methyl triflate as the alkylating agent, 140-190 mCi (5.1-7.0 GBq) of (R)-(-)-[11C]Deprenyl was obtained within 30 min of radiosynthesis (including HPLC purification and formulation) with specific radioactivities ranging from 0.8 to 1.2 Ci/μmol (29.644.4 GBq/μmol). The high efficiency of these radiosyntheses allows for multi-injection protocols and kinetic approaches for absolute quantification of the tracer.

AB - Carbon-11 labeled (R)-(-)-Deprenyl is the tracer of reference for the quantification of monoamine oxidase (MAO)-B activity with PET. In this paper, its radiosynthesis is re-investigated and oriented towards the preparation of multi-milliCuries of radiotracer. Typically, using no-carrier-added [11C]methyl triflate as the alkylating agent, 140-190 mCi (5.1-7.0 GBq) of (R)-(-)-[11C]Deprenyl was obtained within 30 min of radiosynthesis (including HPLC purification and formulation) with specific radioactivities ranging from 0.8 to 1.2 Ci/μmol (29.644.4 GBq/μmol). The high efficiency of these radiosyntheses allows for multi-injection protocols and kinetic approaches for absolute quantification of the tracer.

KW - Carbon-11

KW - Deprenyl

KW - MAO

KW - Monoamine oxidase

KW - PET

KW - Positron emission tomography

UR - https://www.scopus.com/pages/publications/0036736198

U2 - 10.1002/jlcr.604

DO - 10.1002/jlcr.604

M3 - Article

AN - SCOPUS:0036736198

SN - 0362-4803

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EP - 811

JO - Journal of Labelled Compounds and Radiopharmaceuticals

JF - Journal of Labelled Compounds and Radiopharmaceuticals

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