Radiolabeling and biodistribution of methyl 2-(methoxycarbonyl)-2-(methylamino) bicyclo [2.1.1] - hexane -5-carboxylate, a potential neuroprotective drug

Meixiang Max Yu, Kjell Någren, Y. Iris Chen, Elijahu Livni, David Elmaleh, Alan Kozikowski, Xukui Wang, Kimmo Jokivarsi, Anna Liisa Brownell

Research output: Contribution to journalArticle

4 Scopus citations

Abstract

Methyl 2-(methoxycarbonyl) -2-(methylamino) bicyclo[2.1.1] -hexane -5-carboxylate (MMMHC) is developed as a potential neuroprotective drug. It was labeled with C-11 from the desmethyl precursor methyl 2-(methoxycarbonyl)-2-amino bicyclo[2.1.1]-hexane-5-carboxylate with [11C]methyl triflate in acetone solution at 60°C with labeling yield of 69% and with radiochemical purity of >99%. Positron Emission Tomography (PET) studies in a normal rat showed that Methyl 2-(methoxycarbonyl)-2-([11C]methylamino)bicyclo[2.1.1]-hexane-5- ca2rboxylate ([11C] MMMHC) accumulated mainly in the cortical brain areas after iv administration. Frontal cortex/cerebellum ratios in a rat brain were 8.0/6.0, 6.8/4.2, 6.3/4.3, 5.5/4.2 and 5.2/4.5 percent of the injected dose in 100 ml at 2 min, 5 min, 10 min, 20 min and 40 min respectively after i.v. injection. During 20-40 min, 2.9 ± 0.4% of the total activity stayed in the brain. These results showed that MMMHC could be labeled with C-11 with high yield, and it passed the brain-blood barrier and accumulated in several brain regions.

Original languageEnglish (US)
Pages (from-to)1577-1585
Number of pages9
JournalLife sciences
Volume73
Issue number12
DOIs
StatePublished - Aug 8 2003

Keywords

  • Carbon-11
  • Metabotropic glutamate receptors
  • Neuroprotection
  • Positron emission tomography

ASJC Scopus subject areas

  • Pharmacology

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