8-(3-Chlorostyryl)caffeine

8-(3-Chlorostyryl)caffeine (CSC) is an adenosine A₂ receptor antagonist (K_i = 54 nM).¹ It is selective for adenosine A₂ over A₁ receptors (K_i = 28 µM). CSC reverses locomotor depression induced by the adenosine A_2A agonist APEC in mice (ED₅₀ = 16 µg/kg, i.p.). It increases locomotion in mice when administered at a dose of 5 mg/kg. CSC (5 mg/kg) reverses the shortening of the rotational motor response and increases in striatal adenosine A₂ receptor levels induced by L-DOPA (Item No. 13248) in a rat model of Parkinson’s disease induced by 6-OHDA (Item No. 25330).² It also inhibits monoamine oxidase B (MAO-B; K_i = 100 nM) and reduces MAO-B activity in brain mitochondrial preparations from wild-type and A_2A^-/- mice.³

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1. Jacobson, K.A., Nikodijević, O., Padgett, W.L., et al. 8-(3-Chlorostyryl)caffeine (CSC) is a selective A₂-adenosine antagonist in vitro and in vivo. FEBS Lett. 323(1-2), 141-144 (1993).

2. Song, L., Kong, M., Ma, Y., et al. Inhibitory effect of 8-(3-chlorostryryl) caffeine on levodopa-induced motor fluctuation is associated with intracellular signaling pathway in 6-OHDA-lesioned rats. Brain Res. 1276, 171-179 (2009).

3. Chen, J.-F., Steyn, S., Staal, R., et al. 8-(3-Chlorostyryl)caffeine may attenuate MPTP neurotoxicity through dual actions of monoamine oxidase inhibition and A_2A receptor antagonism. The Journal of Biological Chemisty 277(39), 36040-36044 (2002).