A 438079 is a competitive P2X7 receptor antagonist (pIC50 = 6.9 for the inhibition of Ca2+ influx in the human recombinant P2X7 cell line).
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ATP is a key neurotransmitter in this process of inducing and maintaining chronic pain. P2X7 is the glial ATP receptor modulating the pathological pain. A 438079 can inhibits P2X7 with an IC50 of 321nM in 1321N1 cells. In pharmacokinetic rats, treatment of 10 μM/kg showed low mean plasma and brain levels of the drug, suggesting 84% binding rate to plasma protein. In SNL and CCI rats, treatment of 100 and 300 μM/kg significantly improved withdrawal thresholds with the ED50 of 76 and 100 μM/kg respectively without affecting rat rotarod performance. Treatment of 80 μM/kg this drug in SNL rats didn't affect the von Frey-related discharges of hmWDR and mWDR but was effective against high intensity stimulation. Such an treatment also attenuated the evoked responses of neurons to thermal stimulation and decreased the level of spontaneous firing. Besides, A 438079 with concentration of 1 μM reduced the P2X7 receptor agonist in non-neuronal DRG cells. IL-1β release was also inhibited by 75.6% at concentration of 3 μM in a dose- dependent manner[1]. The drug also showed effect on seizure in P10 rat model with the dose range from 0.5 to 50 mg/kg in a dose-dependent manner. And seizure damage was also reduced at either 5 or 15 mg/kg as well as reduced TUNEL staining and decreasing score for neuronal damage. The plasma levels declined rapidly to 2.3 μg/mL within 10 min with the initial concentration of 5 mg/kg of A 438079 in the model, which did not affect cell apoptosis at either 5 or 50 mg/kg[2].
A 438079 动物研究
Dose
Mice: 80 mg/kg[3], 50-200 μmol/kg[4] Rats: min = 5 mg/kg[2], max = 30 mg/kg[5]
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