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- W1994536229 abstract "The dihydrophyridines S12968 ((−)-S11568, absolute configuration S) and S12967 ((+)-S11568, absolute configuration R), 3-ethyl 5-methyl (−/+)-2-[(2-(2-aminoethoxy)ethoxy)methyl]-4-(2,3-dichlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate, have both an in vitro profile of high potency and of high selectivity for the low-voltage-dependent L-type calcium channel. In this paper, the radiosynthesis of both enantiomers, S12968 and S12967, with carbon-11, a positron-emitting isotope (half-life : 20.4 min) was investigated and oriented towards the preparation of multi milliCuries of radiotracer. Typically, 130–250 mCi (4.81–9.25 GBq) of [11C]S12968 and [11C]S12967 were obtained within 30 min of radiosynthesis (HPLC purification included) with specific radioactivities ranging from 500 to 1000 mCi/μmol (18.5–37.0 GBq/μmol) using no-carrier-added [11C]methyl triflate as the alkylating agent and the appropriate, enantiomerically pure carboxylic acid precursor at 100°C for 1 min. Based on preliminary PET experiments, only the levo enantiomer S12968 ((−)-[11C]-1) appears to be suitable for myocardial PET imaging as demonstrated in vivo in beagle dogs: with S12968, 85% of the uptake of [11C]S12968 could be inhibited in pretreatment experiments and up to 70% of [11C]S12968 could be displaced. Further investigations are currently underway in order to provide an absolute quantification of ventricular calcium channels with PET. Copyright © 2001 John Wiley & Sons, Ltd." @default.
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- W1994536229 date "2001-01-01" @default.
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- W1994536229 title "Highly efficient synthesis of [11C]S12968 and [11C]S12967, for thein vivo imaging of the cardiac calcium channels using PET" @default.
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- W1994536229 doi "https://doi.org/10.1002/jlcr.476" @default.
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