Radiosynthesis of (N-[11C]methyl)benperidol for PET investigation of D2 receptor binding

Stephen M. Moerlein; Joel S. Perlmutter; Michael J. Welch

doi:10.1524/ract.92.4.333.35584

Radiosynthesis of (N-[¹¹C]methyl)benperidol for PET investigation of D2 receptor binding

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

Abstract

A procedure for the reliable production of the novel PET D2 receptor ligand (N-[¹¹C]methyl)benperidol ([¹¹C]NMB) is described. The method is based on N-methylation of benperidol using [¹¹C]methyl iodide from the PETtrace MeI MicroLab, with product purification via normal-phase HPLC. Batch yields of 2.5 ± 0.9 GBq (68 ± 25 mCi) of [¹¹C]NMB are routinely (n = 16) obtained, with a radiochemical purity > 98% and an average specific activity of over 40.7 TBq (1100 Ci)/mmol. The overall radiosynthesis, purification, and pre-release quality control testing is accomplished within 50 minutes. The procedure described herein produces a radiopharmaceutical product that is suitable for D2 receptor studies using PET or microPET imaging.

Original language	English
Pages (from-to)	333-339
Number of pages	7
Journal	Radiochimica Acta
Volume	92
Issue number	4-6
DOIs	https://doi.org/10.1524/ract.92.4.333.35584
State	Published - 2004

Keywords

(N-[C]methyl)benperidol
Dopamine
Dopamine D2 receptors
PET
Radiopharmaceutical
[C]NMB

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10.1524/ract.92.4.333.35584

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@article{9af3f638b6c14b999d7412bf881d7cee,

title = "Radiosynthesis of (N-[11C]methyl)benperidol for PET investigation of D2 receptor binding",

abstract = "A procedure for the reliable production of the novel PET D2 receptor ligand (N-[11C]methyl)benperidol ([11C]NMB) is described. The method is based on N-methylation of benperidol using [11C]methyl iodide from the PETtrace MeI MicroLab, with product purification via normal-phase HPLC. Batch yields of 2.5 ± 0.9 GBq (68 ± 25 mCi) of [11C]NMB are routinely (n = 16) obtained, with a radiochemical purity > 98\% and an average specific activity of over 40.7 TBq (1100 Ci)/mmol. The overall radiosynthesis, purification, and pre-release quality control testing is accomplished within 50 minutes. The procedure described herein produces a radiopharmaceutical product that is suitable for D2 receptor studies using PET or microPET imaging.",

keywords = "(N-[C]methyl)benperidol, Dopamine, Dopamine D2 receptors, PET, Radiopharmaceutical, [C]NMB",

author = "Moerlein, \{Stephen M.\} and Perlmutter, \{Joel S.\} and Welch, \{Michael J.\}",

note = "Funding Information: Acknowledgment. We thank the Division of Radiological Sciences for their excellent support, especially C. Dence for helpful discussions regarding the MeI Microlab, K. Lechner for HPLC expertise, and W. Margenau and D. Ficke for radioisotope production. This work was supported by the Greater St. Louis Chapter of the American Parkinson Disease Association (APDA), the APDA Center for Advanced Research in Parkinson Disease, the Ruth Kopolow Fund, the Barnes-Jewish Hospital Foundation (Jack Buck Fund for PD Research), the Elliot H. Stein Family Fund, and by an internal grant from the Mallinckrodt Institute of Radiology.",

year = "2004",

doi = "10.1524/ract.92.4.333.35584",

language = "English",

volume = "92",

pages = "333--339",

journal = "Radiochimica Acta",

issn = "0033-8230",

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AU - Moerlein, Stephen M.

AU - Perlmutter, Joel S.

AU - Welch, Michael J.

N1 - Funding Information: Acknowledgment. We thank the Division of Radiological Sciences for their excellent support, especially C. Dence for helpful discussions regarding the MeI Microlab, K. Lechner for HPLC expertise, and W. Margenau and D. Ficke for radioisotope production. This work was supported by the Greater St. Louis Chapter of the American Parkinson Disease Association (APDA), the APDA Center for Advanced Research in Parkinson Disease, the Ruth Kopolow Fund, the Barnes-Jewish Hospital Foundation (Jack Buck Fund for PD Research), the Elliot H. Stein Family Fund, and by an internal grant from the Mallinckrodt Institute of Radiology.

PY - 2004

Y1 - 2004

N2 - A procedure for the reliable production of the novel PET D2 receptor ligand (N-[11C]methyl)benperidol ([11C]NMB) is described. The method is based on N-methylation of benperidol using [11C]methyl iodide from the PETtrace MeI MicroLab, with product purification via normal-phase HPLC. Batch yields of 2.5 ± 0.9 GBq (68 ± 25 mCi) of [11C]NMB are routinely (n = 16) obtained, with a radiochemical purity > 98% and an average specific activity of over 40.7 TBq (1100 Ci)/mmol. The overall radiosynthesis, purification, and pre-release quality control testing is accomplished within 50 minutes. The procedure described herein produces a radiopharmaceutical product that is suitable for D2 receptor studies using PET or microPET imaging.

AB - A procedure for the reliable production of the novel PET D2 receptor ligand (N-[11C]methyl)benperidol ([11C]NMB) is described. The method is based on N-methylation of benperidol using [11C]methyl iodide from the PETtrace MeI MicroLab, with product purification via normal-phase HPLC. Batch yields of 2.5 ± 0.9 GBq (68 ± 25 mCi) of [11C]NMB are routinely (n = 16) obtained, with a radiochemical purity > 98% and an average specific activity of over 40.7 TBq (1100 Ci)/mmol. The overall radiosynthesis, purification, and pre-release quality control testing is accomplished within 50 minutes. The procedure described herein produces a radiopharmaceutical product that is suitable for D2 receptor studies using PET or microPET imaging.

KW - (N-[C]methyl)benperidol

KW - Dopamine

KW - Dopamine D2 receptors

KW - PET

KW - Radiopharmaceutical

KW - [C]NMB

UR - https://www.scopus.com/pages/publications/3142744557

U2 - 10.1524/ract.92.4.333.35584

DO - 10.1524/ract.92.4.333.35584

M3 - Article

AN - SCOPUS:3142744557

SN - 0033-8230

VL - 92

SP - 333

EP - 339

JO - Radiochimica Acta

JF - Radiochimica Acta

IS - 4-6

ER -

Radiosynthesis of (N-[¹¹C]methyl)benperidol for PET investigation of D2 receptor binding

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