A-438079 HCl
P2X7 antagonist / A-438079 (899431-18-6) is a competitive P2X7 receptor antagonist (pIC50 = 6.9).1 Displayed antinociceptive effects in a rat model of neuropathic pain.2 A-438079 prevented the LPS-induced release of IL-1ß and attenuated LPS-induced (via intrathecal lumbar injection) mechanical hyperalgesia in rat hindpaws.3 It prevented mechanical hyperalgesia following peripheral nerve injury.4 A-438079 protected against cerebral ischemia/reperfusion injury in a rat model via reduction of the neuroinflammatory response.5
Biochemicals & reagents
899431-18-6
1) Nelson et al. (2006) Structure-activity relationship studies on a series of novel, substitutes 1-benzyl-5-phenyltetrazole P2X7 antagonists; J. Med. Chem. 49 3659 2) McGaraughty et al. (2007) P2X7-related modulation of pathological nociception in rats; Neuroscience 146 1817 3) Clark et al. (2010) P2X7-dependent release of interleukin-1beta and nociception in the spinal cord following lipopolysaccharide; J. Neurosci. 30 573 4) Kobayashi et al. (201) Induction of the P2X7 receptor in spinal microglia in a neuropathic pain model; Neurosci. Lett. 504 57 5) Chu et al. (2012) Inhibition of P2X7 receptor ameliorates transient global cerebral ischemia/reperfusion injury via modulating inflammatory responses in the rat hippocampus; J. Neuroinflammation 9 69
-20°C
TARGET: Ion channel -- PATHWAY: Cytokine; Calcium signaling; Cation channel -- RESEARCH AREA: Neuroscience; Oxidative stress -- DISEASE AREA: Pain; InflammationIschemia; Cancer