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CAS No. : 1190217-35-6
MCE 国际站:ASP7663
产品活性:ASP7663 是具有口服活性的、选择性的 TRPA1 激动剂。ASP7663 具有抗便秘和抗腹痛的活性。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点:TRP Channel
In Vitro: ASP7663 concentration dependently increases intracellular Ca2+ concentration in human, rat, and mouse TRPA1 expressed in HEK293 cells in a similar manner, with respective EC50 values (95% confidence interval [CI]) of 0.51 (0.40–0.66), 0.54 (0.41–0.72), and 0.50 (0.41–0.63) μmol/L.
ASP7663 concentration-dependently stimulates 5-HT release from QGP-1 cells, a lineage of TRPA1-expressing EC cells, with an EC50 value of 72.5 (52.6–99.9) μmol/L.
In Vivo: ASP7663 significantly improves the loperamide-induced delay in colonic transit in mice.
ASP7663 (orally, 0.3 and 1 mg/kg) significantly shortens the prolonged bead expulsion time caused by loperamide.
ASP7663 (orally, 1 and 3 mg/kg) exhibits inhibitory effects on colorectal distension in rat.
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