GDC-0334 is a selective TRPA1 antagonist. GDC-0334 inhibits TRPA1 function on airway smooth muscle and sensory neurons by decreasing cough and allergic airway inflammation in rats and guinea pigs. GDC-0334 can be used for TRPA1-mediated diseases research, such as pain or asthma.
GDC-0334 (0-150 mg/kg; i.v.) decreases edema, dermal blood flow (DBF), cough, and allergic airway inflammation in rats[1].
GDC-0334 (0.5/1 mg/kg for i.v., 1/5 mg/kg mg/kg for p.o.) shows a T1/2 of 11.9 h in mice and 9.79 h in rats by i.v., and oral bioavailability (F%) of 45.0% in mice and 46.2% in rats [1].
Pharmacokinetic parameters for GDC-0334 in mouse/rat/dog/monkey [1]
References:
[1]. Estrada A, et al. 1-(het)arylsulfonyl-(pyrrolidine or piperidine)-2-carboxamide derivatives and their use as trpa1 antagonists. WO2016128529 A1.
[2]. Balestrini A, et.al A TRPA1 inhibitor suppresses neurogenic inflammation and airway contraction for asthma treatment. J Exp Med. 2021 Apr 5;218(4):e20201637.