human trpv1

Oleoyl Serotonin is an antagonist of hTRPV1 with an IC50 of 2.57 μM.

SB705498 is a TRPV1 antagonist for hTRPV1. SB-705498 has been investigated for the treatment of Rhinitis, Chronic Cough, and Non-allergic Rhinitis.

OMDM-5 is a selective anandamide cellular uptake (ACU)inhibitor(Ki of 4.8 μM).

A-1165442 is a competitive TRPV1 antagonist. For human TRPV, the IC50 values is 9 nM.

A-889425 is a selectively active oral TRPV1 receptor antagonist with IC50 values of 335 nM (rat) and 34 nM (human). This compound effectively penetrates the central nervous system, reducing mechanical allodynia and the response of spinal neurons to mechanical stimuli in rat paws following inflammation induced by Complete Freund's Adjuvant.

DWP-05195 is a TRPV1 antagonist capable of inhibiting pain signal transduction. Additionally, it induces ER stress-dependent apoptosis in human ovarian cancer cells via the ROS-p38-CHOP pathway.

MDR-652 is a highly specific and efficacious agonist of nonpungent transient receptor potential vanilloid 1 (TRPV1), with Ki values of 11.4 nM and 23.8 nM for hTRPV1 and rTRPV1, respectively, and EC50s of 5.05 nM and 93 nM for hTRPV1 and rTRPV1, respectively. MDR-652 is a potent topical analgesic.

RN-9893 is an antagonist of transient receptor potential vanilloid 4 (TRPV4; IC50s = 0.42 and 0.66 μM, respectively, for the human and rat receptors).1 It is selective for TRPV4 over TRPV1, TRPV3, and TRPM8 (IC50s = 10, >30, and 30 μM, respectively). RN-9893 reduces rat TRPV4 activity induced by 4α-phorbol 12,13-didecanoate or hypotonicity (IC50s = 0.57 and 2.1 μM, respectively, in cell free assays). |1. Wei, Z.L., Nguyen, M.T., O'Mahony, D.J., et al. Identification of orally-bioavailable antagonists of the TRPV4 ion-channel. Bioorg. Med. Chem. Lett. 25(18), 4011-4015 (2015).

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].

AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1) (IC50s = 24.5 and 85.6 nM for human and rat TRPV1, respectively).

PF-05089771 is a voltage-gated sodium channel 1.7 (Nav1.7) blocker (IC50: 11, 16, 33, and 20 nM for 5N11S, 5A11L, 5A11S, and 5A11L Nav1.7 splice variants, respectively). It is selective for Nav1.7 over Nav1.1-1.6 and 1.8 channels (IC50: 0.11-25 μM), L-typ

JNJ-17203212 is a potent and selective antagonist of TRPV1 (human TRPV1 and rat TRPV1, IC50 of 65 nM and 102 nM).

Mambalgin 1 TFA, a selective inhibitor of ASIC1a (with IC50 values of 192 nM for human ASIC1a and 72 nM for the ASIC1a 1b dimer), preferentially binds to the channel in its closed inactive state. It demonstrates selectivity for ASIC1a over a range of other channels, including ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2, and Kv1.2. In vivo, Mambalgin 1 TFA effectively prolongs the latency of the withdrawal response in mouse tail-flick and paw-flick tests.

Selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Binds to closed/inactive channel. Selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Increases late