8-(3-Chlorostyryl)caffeine (CSC) is an adenosine A2 receptor antagonist (Ki = 54 nM). It is selective for adenosine A2 over A1 receptors (Ki = 28 μM). CSC reverses locomotor depression induced by the adenosine A2A 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; Ki = 100 nM) and reduces MAO-B activity in brain mitochondrial preparations from wild-type and A2A-/- 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.
