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

ABT 102 (CHEMBL398338) is a selective antagonist of transient receptor potential vanilloid 1 (TRPV1) receptor.

ABT-239 is a novel, highly efficacious antagonist belonging to the non-imidazole class of histamine H3 receptor (H3R) antagonists. It also acts as a transient receptor potential vanilloid type 1 (TRPV1) antagonist.

JTS-653 is a potent and selective in vitro and in vivo antagonist of transient receptor potential vanilloid 1 (TRPV1). It effectively attenuates chronic pain resistant to non-steroidal anti-inflammatory drugs.

α-Spinasterol is a transient receptor potential vanilloid 1 (TRPV1) antagonist, has anti-inflammatory, antidepressant, antioxidant and antinociceptive effects. α-Spinasterol inhibits COX-1 andCOX-2 activities with IC50 values of 16.17 μM and 7.76 μM, respectively.

TRPV1-Tat, a peptide antagonist targeting transient receptor potential vanilloid 1 (TRPV1), is composed of amino acids 736-745 derived from TRPV1's A-kinase anchor protein (AKAP)-binding domain, combined with the HIV Tat-derived cell-penetrating peptide sequence. At a concentration of 200 µM, TRPV1-Tat effectively inhibits heat or phorbol 12-myristate 13-acetate (PMA014)-induced currents in primary mouse dorsal root ganglia via whole-cell patch-clamp assays. Additionally, when administered at dosages of 10 or 30 µM, it elevates the mechanical pain threshold in the hind paws of rats.

JNJ-38893777 is a potent and selective transient receptor potential vanilloid 1 (TRPV1) channel antagonist.

GSK3395879 is a selective and orally bioavailable antagonist of transient receptor potential vanilloid-4 (TRPV4) (IC50: 1 nM for hTRPV4).

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

SB 452533 is an antagonist of the vanilloid receptor 1(pKb: 7.8).

Capsaicin is the primary active component of the heat and pain-eliciting lipid soluble fraction of the Capsicum pepper. Capsaicin signals are transduced by a heat-activated ion channel, the vanilloid receptor 1 (VR1), or transient receptor potential vanilloid 1 (TRPV1). CAY10448 is an iodinated nonivamide, a potent capsaicin receptor antagonist with an IC50 value of approximately 10 nM.

Potent and selective TRPV1 antagonist. Blocks Ca2+ uptake by CHO cells expressing TRPV1 receptors and acid-induced Ca2+ uptake, respectively). Exhibits >4000-fold selectivity for TRPV1 over other TRP channels. Blocks capsaicin-induced flinch response and causes hyperthermia in rats. Orally available and non-CNS penetrant. Tamayo et al (2008) Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. J.Med.Chem. 51 2744 PMID:18386885 |Gavva et al (2007) The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation. J.Neurosci. 27 3366 PMID:17392452

AS1928370 is an antagonist of transient receptor potential vanilloid 1 (TRPV1).

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).

L-R4W2 TFA acts as a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), demonstrating significant inhibitory activity with an IC50 value of 0.1 μM. This compound potentially offers powerful analgesic properties [1] [2].

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).