8-(3-Chlorostyryl)caffeine (CSC) is an adenosine A receptor antagonist (K = 54 nM). It is selective for adenosine A over A receptors (K = 28 µM). CSC reverses locomotor depression induced by the adenosine A agonist APEC in mice (ED = 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 A 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 = 100 nM) and reduces MAO-B activity in brain mitochondrial preparations from wild-type and A mice.
8-(3-Chlorostyryl)caffeine is a MAO-B inhibitor and adenosine A2A receptor antagonist. 8-(3-Chlorostyryl)caffeine inhibits the activity of monoamine oxidase B through a pathway independent of adenosine A2A receptor antagonism. 8-(3-Chlorostyryl)caffeine can be used in research related to Parkinson's disease.
IC50&Target
A2AR MAO-B
70 nM (Ki)
体外研究
8- (3-Chlorostyryl) caffeine (different inhibitor concentrations; When MMTP was used as a substrate for 15 minutes, MAO-B in baboon liver mitochondria was effectively and competitively inhibited, with a Ki value of 128 nM [1].
8- (3-Chlorostyryl) caffeine (different inhibitor concentrations; When using benzylamine as a substrate for 8 minutes, it can effectively and competitively inhibit monoamine oxidase B (MAO-B) in baboon liver mitochondria, with a Ki value of 148 nM [1].