Synthesis and pet‐studies of (R)‐and (S)‐[<sup>11</sup>C]verapamil for measuring PGP function in MDR1A(+/+)/B(+/+) and MDR1A(‐/‐)/B(‐/‐) mice

Luurtsema, Geert; Windhorst, Albert D.; Herscheid, J. D. M.; Molthoff, Carla F. M.; Boellaard, Rol; Smit, Henk; Schinkel, AH; Lammertsma, Adriaan A.; Franssen, Ejf

doi:10.1002/jlcr.25804401110

Cited by 3 publications

(2 citation statements)

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“…No significant effects were observed. 18 An overall radiochemical yield of 13.3 AE 3.4% (n=3) was obtained. For practical reasons 1.5 mg (R/S) 1 in a volume of 500 ml of dry acetonitrile was maintained.…”

Section: Automated Radiosynthesismentioning

confidence: 91%

“…14 The diluted product was passed through an activated tC 18 Sep Pak cartridge using a helium overpressure, which was subsequently washed with 20 ml of sterile H 2 O. Compound 2 was eluted from the Sep Pak with 1 ml of ethanol followed by 9 ml saline and filtered through a sterile 0.22 mm filter using a helium overpressure yielding a sterile and pyrogen free-ready for injection solution.…”

Section: Automated Radiosynthesismentioning

confidence: 99%

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Fully automated high yield synthesis of (R)‐ and (S)‐[¹¹C]verapamil for measuring P‐glycoprotein function with positron emission tomography

Luurtsema

Windhorst

Mooijer

et al. 2002

Labelled Comp Radiopharmac

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SummaryRacemic ( AE ) verapamil is a well characterized substrate for P-glycoprotein (P-gp). However, the in vivo pharmacokinetics and pharmacodynamics of both enantiomers are reported to be different. In the preparation of evaluation studies of both enantiomers in animals and humans, the purpose of the present study was to optimize and automate the synthesis of (R)-and (S)- guidelines. Optimal yields of 60-70% for the methylation reaction were obtained using 1.5 mg of the free base of (R)-or (S)-desmethyl-verapamil in 0.5 ml of acetonitrile at 508C for 5 min with [ 11 C]methyltriflate as methylating agent. Under the same reaction conditions, but with a reaction temperature of 1008C, the radiochemical yield starting with [ 11 C]methyliodide as methylation reagent was 40%. The specific activity of (R)-and (S)-[ 11 C]verapamil was >20 GBq/mmol and the radiochemical purity was >99%for both methods. The total synthesis time was 45 min. The automated high yield synthesis of (R)-and (S)-[ 11 C]verapamil provides the means for evaluating both enantiomers as in vivo tracers of P-gp function.

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Section: Automated Radiosynthesismentioning

confidence: 91%

Section: Automated Radiosynthesismentioning

confidence: 99%

Fully automated high yield synthesis of (R)‐ and (S)‐[¹¹C]verapamil for measuring P‐glycoprotein function with positron emission tomography

Luurtsema

Windhorst

Mooijer

et al. 2002

Labelled Comp Radiopharmac

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An improved method for the preparation of [11C]verapamil

Wegman

Maas

Elsinga

et al. 2002

Applied Radiation and Isotopes

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Fluoro-, bromo-, and iodopaclitaxel derivatives: synthesis and biological evaluation

Kiesewetter

Jagoda

Kao

et al. 2003

Nuclear Medicine and Biology

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Synthesis and pet‐studies of (R)‐and (S)‐[¹¹C]verapamil for measuring PGP function in MDR1A(+/+)/B(+/+) and MDR1A(‐/‐)/B(‐/‐) mice

Cited by 3 publications

References 0 publications

Fully automated high yield synthesis of (R)‐ and (S)‐[¹¹C]verapamil for measuring P‐glycoprotein function with positron emission tomography

Fully automated high yield synthesis of (R)‐ and (S)‐[¹¹C]verapamil for measuring P‐glycoprotein function with positron emission tomography

An improved method for the preparation of [11C]verapamil

Fluoro-, bromo-, and iodopaclitaxel derivatives: synthesis and biological evaluation

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Synthesis and pet‐studies of (R)‐and (S)‐[11C]verapamil for measuring PGP function in MDR1A(+/+)/B(+/+) and MDR1A(‐/‐)/B(‐/‐) mice

Cited by 3 publications

References 0 publications

Fully automated high yield synthesis of (R)‐ and (S)‐[11C]verapamil for measuring P‐glycoprotein function with positron emission tomography

Fully automated high yield synthesis of (R)‐ and (S)‐[11C]verapamil for measuring P‐glycoprotein function with positron emission tomography

An improved method for the preparation of [11C]verapamil

Fluoro-, bromo-, and iodopaclitaxel derivatives: synthesis and biological evaluation

Contact Info

Product

Resources

About

Synthesis and pet‐studies of (R)‐and (S)‐[¹¹C]verapamil for measuring PGP function in MDR1A(+/+)/B(+/+) and MDR1A(‐/‐)/B(‐/‐) mice

Fully automated high yield synthesis of (R)‐ and (S)‐[¹¹C]verapamil for measuring P‐glycoprotein function with positron emission tomography

Fully automated high yield synthesis of (R)‐ and (S)‐[¹¹C]verapamil for measuring P‐glycoprotein function with positron emission tomography