Uses
A 740003 is a potent, selective and competitive P2X7 receptor antagonist.
General Description
A-740003 is a highly affine and selective P2X7 receptor antagonist and is best for the progression of a radiotracer for imaging of neuroinflammation by positron emission tomography.
Biological Activity
Potent, selective and competitive P2X 7 receptor antagonist (IC 50 values are 18 and 40 nM for rat and human receptors respectively). Displays selectivity over a variety of P2X and P2Y receptors up to a concentration of 100 μ M. Reduces nociception in animal models of persistent neuropathic and inflammatory pain.
Biochem/physiol Actions
A-740003 is a selective P2X7 purinoceptor antagonist.
References
[1]. prisca honore, diana donnelly-roberts, marian t. namovic, et al. a-740003 [n-(1-{[(cyanoimino)(5-quinolinylamino)methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective p2x7 receptor antagonist, dose-dependently reduces neuropathic pain in the rat. journal of pharmacology and experimental therapeutics, 2006, 319:1376-1385.
