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MSX-2
A selective adenosine A2A receptor antagonist From Wikipedia, the free encyclopedia
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MSX-2 is a selective adenosine A2A receptor antagonist used in scientific research.[1] It is a xanthine and a derivative of the non-selective adenosine receptor antagonist caffeine.[1][2]
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The affinities (Ki) of MSX-2 for the human adenosine receptors are 5.38 to 14.5 nM for the adenosine A2A receptor, 2,500 nM for the adenosine A1 receptor (172- to 465-fold lower than for the A2A receptor), and >10,000 nM for the adenosine A2B and A3 receptors (>690-fold lower than for the A2A receptor).[3][4]
MSX-2 has poor water solubility, which has limited the use of MSX-2 itself.[1][5] Water-soluble ester prodrugs of MSX-2, including MSX-3 (a phosphate ester prodrug) and MSX-4 (an amino acid ester prodrug), have been developed and used in place of MSX-2.[1][5] MSX-3 is best-suited for use by intravenous administration, whereas MSX-4 can be administered by oral administration.[5][6]
MSX-3 and MSX-4 reverse motivational deficits in animals and hence have the capacity to produce pro-motivational effects.[7][8][9]
MSX-2 and MSX-3 were first described in the scientific literature by 1998.[10][11] Subsequently, MSX-4 was developed and described by 2008.[5][6]
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