trpv antagonist 1

TRPV antagonist 1 is an antagonist of transient receptor potential vanilloid (TRPV; IC50 < 250 nM).

TRPV1 antagonist 10 is a potent, orally active TRPV1 antagonist with an IC50 of 33.06 nM and serves as a moderate to weak inhibitor of URAT1 (IC50 = 22.51 μM) and GLUT9 (inhibition of 60.25% at 50 μM). It exhibits analgesic and urate-lowering properties and is applicable for research in hyperuricemia and inflammatory pain.

TRPV1 antagonist 11 (compound 2ac) is a highly potent TRPV1 antagonist with an IC50 of 29.3 nM. It also acts as a μ-opioid receptor (MOR) agonist with a Ki of 60.3 nM. This pyrimidinylpiperazine compound provides analgesic effects by antagonizing TRPV1 and activating MOR. In mouse models of formalin-induced pain, TRPV1 antagonist 11 demonstrates effective dose-dependent antinociceptive properties.

TRPV1 antagonist 6 (compound 51) is a modality-selective TRPV1 antagonist that exhibits antagonistic activity against capsaicin activation with an IC50 of 2.85 nM and demonstrates an inhibition rate of 28.48% against proton activation at a concentration of 3 µM.

TRPV1 antagonist 7 (Compound 36) is a selective TRPV1 inhibitor that effectively blocks capsaicin activation with an IC50 of 2.31 nM. It is useful for research in pain relief.

TRPV1 antagonist 3 (Compound 7q) is a highly potent TRPV1 receptor antagonist with an IC50 of 2.66 nM against capsaicin. It exhibits selectivity in its mode of action, is orally bioavailable (60%), and can penetrate the central nervous system [1].

TRPA1 Antagonist 1 is an antagonist of TRPA1(IC50: 8 nM) and is a methylene phosphate prodrug which converts to its active parent drug.

Vanilloid receptor antagonist 1 (4-(7-Hydroxy-2-isopropyl-4-oxoquinazolin-3(4H)-yl)benzonitrile) is a potent vanilloid receptor TRPV1 antagonist.