A 967079是一种有效的TRPA1受体选择性拮抗剂，对人和大鼠 TRPA1 受体的IC50分别为 67 nM 和 289 nM。A 967079具有良好的CNS 穿透性。

A 967079 is a potent, selective, and bioavailable inhibitor of the TRPA1 channel, with IC50 values of 67 and 289 nM for the human and rat isoforms, respectively.

Systemic injection of A 967079 (30 micromol/kg) decreased the responses of wide dynamic range (WDR), and nociceptive specific (NS) neurons following noxious pinch stimulation of the ipsilateral hind paw in uninjured and CFA-inflamed rats. Similarly, A-967079 reduced the responses of WDR neurons to high-intensity mechanical stimulation (300 g von Frey hair) of the knee joint in both OA and OA-sham rats. WDR neuronal responses to low-intensity mechanical stimulation (10 g von Frey hair) were also reduced by A-967079 administration to CFA-inflamed rats, but no effect was observed in uninjured rats. Additionally, the spontaneous activity of WDR neurons was decreased after A-967079 injection in CFA-inflamed rats but was unaltered in uninjured, OA, and OA-sham animals[1].

Separated by 5 min each, to specific stimulation of the neuronal RF were recorded. Spontaneous and evoked neuronal activity was then measured 5, 15, 25, and 35 min after systemic injection of A-967079 (30 μmol/kg) or vehicle (polyethylene glycol). The intravenous injection of A-967079 or vehicle was completed over a 6-7 min period. The i.v. dose of A-967079 was selected based on extrapolated plasma levels that were effective in behavioral studies . Except for 2 experiments in which two easily distinguished neurons were simultaneously recorded on one electrode, only one neuron was studied per rat. Since only one vehicle was used in these experiments, vehicle data was combined when a clear "no effect' was observed in at least 2-3 animals from a particular subset of groups (OA and sham OA)[1].

1170613-55-4

C12H14FNO

207.24

(1E,3E)-1-(4-氟苯基)-2-甲基-1-戊烯-3-酮肟

DMSO:100 mg/mL (482.53 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years