Automated radiosynthesis of [11C]morphine for clinical investigation

Jinda Fan; Konrad Meissner; Gregory G. Gaehle; Shihong Li; Evan D. Kharasch; Robert H. Mach; Zhude Tu

doi:10.1016/j.apradiso.2010.11.003

Automated radiosynthesis of [¹¹C]morphine for clinical investigation

Jinda Fan, Konrad Meissner, Gregory G. Gaehle, Shihong Li, Evan D. Kharasch, Robert H. Mach, Zhude Tu

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

2 Scopus citations

Abstract

To meet a multiple-dose clinical evaluation of the P-gp modulation of [¹¹C]morphine delivery into the human brain, radiosynthesis of [¹¹C]morphine was accomplished on an automated system by N-methylation of normorphine with [¹¹C]CH₃I. A methodology employing optimized solid phase extraction of the HPLC eluent was developed. Radiosynthesis took 45min with a radiochemical yield ranging from 45% to 50% and specific activity ranging from 20 to 26Ci/γmol (decay corrected to end-of-bombardment); radiochemical and chemical purities were >95% (n=28).

Original language	English
Pages (from-to)	431-435
Number of pages	5
Journal	Applied Radiation and Isotopes
Volume	69
Issue number	2
DOIs	https://doi.org/10.1016/j.apradiso.2010.11.003
State	Published - Feb 2011

Keywords

Automated radiosynthesis
Positron emission tomography
[C]morphine

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10.1016/j.apradiso.2010.11.003

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title = "Automated radiosynthesis of [11C]morphine for clinical investigation",

abstract = "To meet a multiple-dose clinical evaluation of the P-gp modulation of [11C]morphine delivery into the human brain, radiosynthesis of [11C]morphine was accomplished on an automated system by N-methylation of normorphine with [11C]CH3I. A methodology employing optimized solid phase extraction of the HPLC eluent was developed. Radiosynthesis took 45min with a radiochemical yield ranging from 45% to 50% and specific activity ranging from 20 to 26Ci/γmol (decay corrected to end-of-bombardment); radiochemical and chemical purities were >95% (n=28).",

keywords = "Automated radiosynthesis, Positron emission tomography, [C]morphine",

author = "Jinda Fan and Konrad Meissner and Gaehle, {Gregory G.} and Shihong Li and Kharasch, {Evan D.} and Mach, {Robert H.} and Zhude Tu",

note = "Funding Information: This work was supported by the grant K24 DA00417 and R01DA14211 awarded by the National Institutes of Health and the grant from the Federation for Anesthesia Education and Research (FAER) to Konrad Meissner.",

year = "2011",

month = feb,

doi = "10.1016/j.apradiso.2010.11.003",

language = "English",

volume = "69",

pages = "431--435",

journal = "Applied Radiation and Isotopes",

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T1 - Automated radiosynthesis of [11C]morphine for clinical investigation

AU - Fan, Jinda

AU - Meissner, Konrad

AU - Gaehle, Gregory G.

AU - Li, Shihong

AU - Kharasch, Evan D.

AU - Mach, Robert H.

AU - Tu, Zhude

N1 - Funding Information: This work was supported by the grant K24 DA00417 and R01DA14211 awarded by the National Institutes of Health and the grant from the Federation for Anesthesia Education and Research (FAER) to Konrad Meissner.

PY - 2011/2

Y1 - 2011/2

N2 - To meet a multiple-dose clinical evaluation of the P-gp modulation of [11C]morphine delivery into the human brain, radiosynthesis of [11C]morphine was accomplished on an automated system by N-methylation of normorphine with [11C]CH3I. A methodology employing optimized solid phase extraction of the HPLC eluent was developed. Radiosynthesis took 45min with a radiochemical yield ranging from 45% to 50% and specific activity ranging from 20 to 26Ci/γmol (decay corrected to end-of-bombardment); radiochemical and chemical purities were >95% (n=28).

AB - To meet a multiple-dose clinical evaluation of the P-gp modulation of [11C]morphine delivery into the human brain, radiosynthesis of [11C]morphine was accomplished on an automated system by N-methylation of normorphine with [11C]CH3I. A methodology employing optimized solid phase extraction of the HPLC eluent was developed. Radiosynthesis took 45min with a radiochemical yield ranging from 45% to 50% and specific activity ranging from 20 to 26Ci/γmol (decay corrected to end-of-bombardment); radiochemical and chemical purities were >95% (n=28).

KW - Automated radiosynthesis

KW - Positron emission tomography

KW - [C]morphine

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EP - 435

JO - Applied Radiation and Isotopes

JF - Applied Radiation and Isotopes

IS - 2

ER -

Automated radiosynthesis of [¹¹C]morphine for clinical investigation

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