147700-11-6

8-(3-Chlorostyryl)caffeine (CSC) is an adenosine A₂ receptor antagonist (K_i = 54 nM). 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 in a rat model of Parkinson’s disease induced by 6-OHDA . 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.

8-(3-Chlorostyryl)caffeine is a selective Adenosine A2A-R and MAO-B inhibitor.

ChEBI: 8-(3-chlorostyryl)caffeine is caffeine substituted at its 8-position by an (E)-3-chlorostyryl group. It has a role as an adenosine A2A receptor antagonist and an EC 1.4.3.4 (monoamine oxidase) inhibitor. It is a trimethylxanthine and a member of monochlorobenzenes. It is functionally related to a caffeine.

A2AR; MAO-B: 70 nM (Ki)

Store at -20°C

[1] KENNETH A. JACOBSON. 8-(3-Chlorostyryl)caffeine (CSC) is a selective A2-adenosine antagonist in vitro and in vivo[J]. FEBS Letters, 1993, 323 1: Pages 141-144. DOI: 10.1016/0014-5793(93)81466-d
[2] LU SONG . Inhibitory effect of 8-(3-chlorostryryl) caffeine on levodopa-induced motor fluctuation is associated with intracellular signaling pathway in 6-OHDA-lesioned rats[J]. Brain Research, 2009, 1276: Pages 171-179. DOI: 10.1016/j.brainres.2009.04.028
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