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.
생물학적 활성
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.