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Synthesis and properties of a new water-soluble prodrug of the adenosine A 2A receptor antagonist MSX-2.

Molecules (Basel, Switzerland) (2008-02-29)
Karl Vollmann, Ramatullah Qurishi, Jörg Hockemeyer, Christa E Müller
RÉSUMÉ

The compound L-valine-3-{8-[(E)-2-[3-methoxyphenyl)ethenyl]-7-methyl-1-propargylxanthine-3-yl}propyl ester hydrochloride (MSX-4) was synthesized as an amino acid ester prodrug of the adenosine A2A receptor antagonist MSX-2. It was found to be stable in artificial gastric acid, but readily cleaved by pig liver esterase.

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Sigma-Aldrich
Esterase from porcine liver, ammonium sulfate suspension, ≥150 units/mg protein (biuret)