GRC-17536 (GRC 17536) is a potent and selective TRPA1 antagonist, inhibits citric acid -induced Ca+2 influx with IC50 of 8.2 nM in cell-based assays.
GRC-17536 displays no significant activity against TRPV1, TRPV3, TRPV4, TRPM8 at 1 uM.
GRC 17536 (10 nM and 1 µM) inhibited LPS + AITC, Loxoribine + AITC and ssRNA40 + AITC induced 45Ca+2 uptake by 51.3% & 98.4%, 56.6% & 98.6% and 63.0% & 96.1% respectively in hTRPA1/CHO cells.
GRC 17536 blocked citric acid mediated cough in Guinea pigs, showed 79 and 89% inhibition of cough at 60 and 100 mg/kg respectively compared to the vehicle treated animal group.
