The synthesis of [O-methyl-11C]venlafaxine: A non-classical, fast-acting antidepressant

A. D. Gee, D. F. Smith, A. Gjedde

Research output: Contribution to journalArticle

Abstract

As part of our program to develop PET tracers for the 5-HT reuptake site, venlafaxine, a non-classical, fast-acting antidepressant, was selected as a candidate for labelling with 11C for in vivo evaluation. [O-methyl-11C]venlafaxine was produced by the alkylation of O-desmethyl venlafaxine with [11C]methyl iodide followed by HPLC purification and formulation. Radiochemically pure [O-methyl-11C]venlafaxine was obtained in a 30 ± 5 % decay corrected radiochemical yield and a specific activity > 50 GBq/μmol (1.4 Ci/μmol) at the end of synthesis. For a typical production starting with 46 GBq (1.3 Ci) [11C]CO2, 5.2 GBq (140 mCi) [O-methyl-11C]venlafaxine was obtained as a sterile, formulated solution in a synthesis time of 30 min (counted from EOB).

Original languageEnglish (US)
Pages (from-to)89-95
Number of pages7
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume39
Issue number1
DOIs
StatePublished - Jan 1997
Externally publishedYes

Fingerprint

Antidepressive Agents
Alkylation
Labeling
Purification
Serotonin
High Pressure Liquid Chromatography
Venlafaxine Hydrochloride

Keywords

  • 5-HT reuptake
  • C
  • antidepressants
  • PET
  • Venlafaxine

ASJC Scopus subject areas

  • Clinical Biochemistry
  • Molecular Medicine
  • Analytical Chemistry
  • Organic Chemistry
  • Drug Discovery
  • Pharmacology

Cite this

The synthesis of [O-methyl-11C]venlafaxine : A non-classical, fast-acting antidepressant. / Gee, A. D.; Smith, D. F.; Gjedde, A.

In: Journal of Labelled Compounds and Radiopharmaceuticals, Vol. 39, No. 1, 01.1997, p. 89-95.

Research output: Contribution to journalArticle

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