trpv1

Vocacapsaicin hydrochloride (CA-008 hydrochloride) is a non-opioid TRPV1 agonist, a raw material for capsaicin, and is used for pain relief.

Nonivamide (Nonanoic acid vanillylamide) is found in herbs and spices. Nonivamide is an alkaloid from Capsicum species Nonivamide is a flavoring ingredient. Nonivamide is an organic compound and a capsaicinoid. It is an amide of pelargonic acid and vanillylamine. It is present in chili peppers, but is commonly manufactured synthetically. It is more heat-stable than capsaicin.

MSP3 is an agonist of TRPV1 (EC50 = 0.87 μM) and shows antinociceptive and neuroprotective effects.

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.

TRPV1-IN-2 (( R ) -32) is an inhibitor of TRPV1. It provides protective effects in the ED epilepsy model.

TRPV1 CB2 agonist 1 (compound 41) is a dual agonist targeting hTRPV1 and CB2 receptors, with an EC50 value of 26.8 μM for hTRPV1. It is applicable in research related to the nervous system.

TRPV1 Activator-1 (Compound 8), a capsaicin analog featuring a modified neck structure, specifically interacts with the T551 residue [1].

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].

TRPV1-IN-3 (compound 14) is a TRPV1 inhibitor utilized in idiopathic pulmonary fibrosis research. It demonstrates antifibrotic activity in vitro (IC50 = 0.51 μM) by inhibiting the TGF-β Smads and MAPK pathways, thereby affecting the expression of fibrosis markers collagen I and α-SMA. In vivo, TRPV1-IN-3 significantly reduces collagen deposition in lung tissue, improves alveolar structure, and increases survival rates in mice with Bleomycin-induced pulmonary fibrosis.

TRPV1 activator-2 (Compound 9), a capsaicin head analog, engages in targeted interactions with channel residues at the lipid-water interface [1].

Capsaicin ((E)-Capsaicin) is a natural product extracted from Capsicum annuum, and is a TRPV1 agonist (EC50=0.29 μM). Capsaicin has antitumor, anti-inflammatory, antioxidant and neuroprotective activities.

Resiniferatoxin ((+)-Resiniferatoxin) is a highly potent synthetic TRPV1 agonist that inhibits the production of Th1 cytokines and has anti-inflammatory activity, reducing serum levels of IL-12, INF-γ, IL-1β, TNF-α, NO, and PGE.

N-Oleoyl Glutamine (Oleoyl-L-glutamine) is an N-acyl amino acid involved in the regulation of PM20D1 and antagonizes TRPV1 of the transient receptor potential (TRP) calcium channel.

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

PALDA (N-Palmitoyl dopamine) is a fatty acid dopamine found in the mammalian brain that is inactive against TRPV1 and inactivates at TRPV(1)R. It is used in the study of duodenal ulcers.

MK-2295 is a potent TRPV1 antagonist. MK-2295 can be used in studies about the treatment of chronic pain.

N-[(1S)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-N'-1H-indazol-4-ylurea is a potent TRPV1 antagonist, blocking activation of TRPV1 by capsaicin with the IC50 of 123 nM.

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

OMDM-6 is a dual agonist of TRPV1(EC50 = 75 nM) and CB1 (Ki = 3.2 μM). OMDM-6 inhibits anandamide cellular uptake with a Ki of 7.0 μM.

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

Methyl salicylate (Gaultheria oil) is an organic ester naturally produced by many species of plants, particularly wintergreens. For acute joint and muscular pain, methyl salicylate is used as a rubefacient and analgesic in deep heating liniments.

2-Aminoethyl diphenylborinate (2-APB) is a chemical compound that inhibits IP3 receptors and TRP channels, though it activates TRPV1, TRPV2, and TRPV3 at higher concentrations.

Imperatorin (8-Isopentenyloxypsoralene) is a modulator of p38, ERK pathway. Imperatorin increases BMP-2 expression (mRNA) and increases bone density volume and mineralization in vivo.

Caffeic Acid is an orally bioavailable, hydroxycinnamic acid derivative and polyphenol, with potential anti-oxidant, anti-inflammatory, and antineoplastic activities.