Synthesis of suicide inhibitors of monoamine oxidase: Carbon‐11 labeled clorgyline, L‐deprenyl and D‐deprenyl

R. R. Macgregor; J. S. Fowler; A. P. Wolf; C. Halldin; B. Langström

doi:10.1002/jlcr.2580250102

Synthesis of suicide inhibitors of monoamine oxidase: Carbon‐11 labeled clorgyline, L‐deprenyl and D‐deprenyl

R. R. Macgregor, J. S. Fowler, A. P. Wolf, C. Halldin, B. Langström

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66 Scopus citations

Abstract

The suicide inhibitors of monoamine oxidase type A and B, clorgyline and L‐deprenyl have been labeled with carbon‐11 by [¹¹C]methylation of the norbases with [¹¹C]H₃I. The less active enantiomer of deprenyl (D‐deprenyl) was also labeled using this procedure. The synthesis time was 35 minutes, the radiochemical yield was 25–40% and the specific activity was 0.8–2.0 Ci/μmol (calculated to EOB). Procedures for synthesis of the precursor norbases as well as the synthesis of unlabeled clorgyline, L‐deprenyl and D‐deprenyl are given.

Original language	English
Pages (from-to)	1-9
Number of pages	9
Journal	Journal of Labelled Compounds and Radiopharmaceuticals
Volume	25
Issue number	1
DOIs	https://doi.org/10.1002/jlcr.2580250102
State	Published - Jan 1988
Externally published	Yes

Keywords

Monoamine Oxidase A and B
Suicide Inhibitors
[C]Clorgyline
[C]‐D‐Deprenyl
[C]‐L‐Deprenyl

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10.1002/jlcr.2580250102

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title = "Synthesis of suicide inhibitors of monoamine oxidase: Carbon‐11 labeled clorgyline, L‐deprenyl and D‐deprenyl",

abstract = "The suicide inhibitors of monoamine oxidase type A and B, clorgyline and L‐deprenyl have been labeled with carbon‐11 by [11C]methylation of the norbases with [11C]H3I. The less active enantiomer of deprenyl (D‐deprenyl) was also labeled using this procedure. The synthesis time was 35 minutes, the radiochemical yield was 25–40% and the specific activity was 0.8–2.0 Ci/μmol (calculated to EOB). Procedures for synthesis of the precursor norbases as well as the synthesis of unlabeled clorgyline, L‐deprenyl and D‐deprenyl are given.",

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author = "Macgregor, {R. R.} and Fowler, {J. S.} and Wolf, {A. P.} and C. Halldin and B. Langstr{\"o}m",

year = "1988",

month = jan,

doi = "10.1002/jlcr.2580250102",

language = "English",

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T1 - Synthesis of suicide inhibitors of monoamine oxidase

T2 - Carbon‐11 labeled clorgyline, L‐deprenyl and D‐deprenyl

AU - Macgregor, R. R.

AU - Fowler, J. S.

AU - Wolf, A. P.

AU - Halldin, C.

AU - Langström, B.

PY - 1988/1

Y1 - 1988/1

N2 - The suicide inhibitors of monoamine oxidase type A and B, clorgyline and L‐deprenyl have been labeled with carbon‐11 by [11C]methylation of the norbases with [11C]H3I. The less active enantiomer of deprenyl (D‐deprenyl) was also labeled using this procedure. The synthesis time was 35 minutes, the radiochemical yield was 25–40% and the specific activity was 0.8–2.0 Ci/μmol (calculated to EOB). Procedures for synthesis of the precursor norbases as well as the synthesis of unlabeled clorgyline, L‐deprenyl and D‐deprenyl are given.

AB - The suicide inhibitors of monoamine oxidase type A and B, clorgyline and L‐deprenyl have been labeled with carbon‐11 by [11C]methylation of the norbases with [11C]H3I. The less active enantiomer of deprenyl (D‐deprenyl) was also labeled using this procedure. The synthesis time was 35 minutes, the radiochemical yield was 25–40% and the specific activity was 0.8–2.0 Ci/μmol (calculated to EOB). Procedures for synthesis of the precursor norbases as well as the synthesis of unlabeled clorgyline, L‐deprenyl and D‐deprenyl are given.

KW - Monoamine Oxidase A and B

KW - Suicide Inhibitors

KW - [C]Clorgyline

KW - [C]‐D‐Deprenyl

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Synthesis of suicide inhibitors of monoamine oxidase: Carbon‐11 labeled clorgyline, L‐deprenyl and D‐deprenyl

Abstract

Keywords

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