CAY10680 is a dopamine-sparing, benzothiazinone compound that selectively inhibits both MAO-B activity (IC₅₀ = 34.9 nM in human) and adenosine A_2A receptors (K_i = 39.5 nM in human).¹ It demonstrates significantly less potent inhibitory values for other adenosine receptor subtypes (K_is > 1 µM) and MAO-A (IC₅₀ ≥ 10 µM).¹ At 1-20 µM, CAY10680 has been shown to abolish cAMP accumulation in CHO cells transfected with adenosine A_2A receptors.¹ In the central nervous system adenosine A_2A receptor expression is localized to dopamine-innervated areas where heteromeric complexes are formed with dopamine D₂ receptors. Because inhibition of adenosine A_2A receptors has been shown to enhance D₂ receptor function, the blockade of adenosine A_2A receptors has emerged as a potential treatment for Parkinson’s disease. An additional strategy in the treatment of Parkinson’s disease has been to block the activity of monoamine oxidase B (MAO-B), the enzyme involved in dopamine catabolism.

≥98%

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1.Stössel, A.,Schlenk, M.,Hinz, S., et al. Dual targeting of adenosine A_2A receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. Journal of Medicinal Chemistry 56(11), 4580-4596 (2013).