TRPV

A-889425 is a selective TRPV1 receptor antagonist. A-889425 blocks TRPV1 channels with an IC50 of 335 nM (rat) and 34 nM (human).

ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist.

GSK2193874 was identified as a selective, orally active TRPV4 blocker that inhibits Ca(2+) influx through recombinant TRPV4 channels and native endothelial TRPV4 currents.

Linoleylethanolamide is an endocannabinoid that also binds to TRPV1 (Ki = 5.60 uM).

MRS1477 is a TRPV1 positive allosteric modulator.

Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6.

A-1165442 is a potent, competitive and orally available TRPV1 antagonist with an IC50 of 9 nM for human TRPV1.