CAY10680 is a dopamine-sparing, benzothiazinone compound that selectively inhibits both MAO-B activity (IC50 = 34.9 nM in human) and adenosine A2A receptors (Ki = 39.5 nM in human). It demonstrates significantly less potent inhibitory values for other adenosine receptor subtypes (Kis > 1 µM) and MAO-A (IC50 10 µM). At 1-20 µM, CAY10680 has been shown to abolish cAMP accumulation in CHO cells transfected with adenosine A2A receptors. In the central nervous system adenosine A2A receptor expression is localized to dopamine-innervated areas where heteromeric complexes are formed with dopamine D2 receptors. Because inhibition of adenosine A2A receptors has been shown to enhance D2 receptor function, the blockade of adenosine A2A receptors has emerged as a potential treatment for Parkinsons disease. An additional strategy in the treatment of Parkinsons disease has been to block the activity of monoamine oxidase B (MAO-B), the enzyme involved in dopamine catabolism.
Molekulargewicht:
324.4
CAS Nummer:
[1439488-21-7]
Formel:
C18H16N2O2S
Target-Kategorie:
Others|||Monoamine Oxidase|||Adenosine Receptor
T37354
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