Adenosine A2A receptor antagonists

The adenosine A2A receptor is a member of the P1 GPCR family that modulates striatal output in the indirect basal ganglia pathway. Inhibition of adenosine A2A receptors produces motor stimulant effects, and in both the MPTP and 6-OHDA models of PD, adenosine A2A receptor antagonists have positive effects on motor impairment, potentiating DA agonist-stimulated behavior and thus acting as indirect DA agonists.

Istradefylline (KW-6002: 77) is an orally available, xanthine-based adenosine A2A receptor antagonist (Ki = 2.2 nM) that is in Phase III clinical trials for PD.73 It has shown positive benefit in reducing the tremor duration and general slowness/ stiffness in advanced PD patients. V-2006 (78) is a more potent and selective, nonxanthine adenosine A2A receptor antagonist that has recently entered Phase II clinical studies. ST1535 79 is an earlier stage A2A receptor antagonist.

Blood Pressure Health

Blood Pressure Health

Your heart pumps blood throughout your body using a network of tubing called arteries and capillaries which return the blood back to your heart via your veins. Blood pressure is the force of the blood pushing against the walls of your arteries as your heart beats.Learn more...

Get My Free Ebook


Post a comment