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Transient receptor potential (TRP) channel modulators act on cation channels that sense heat, cold and irritants. The mammalian family has six subfamilies, including vanilloid (TRPV), ankyrin (TRPA), canonical (TRPC) and melastatin (TRPM) channels. TRP channels respond to temperature, touch, osmotic changes and plant-derived compounds, so they are often described as cellular sensors. Cloning of the capsaicin receptor TRPV1 in 1997 identified it as a heat-activated ion channel in pain-sensing neurons. AMG517 and SB-705498 are TRPV1 antagonists, while A 967079 blocks TRPA1 and optovin activates TRPA1 when exposed to light. Pyr10 inhibits TRPC3, and Pico145 inhibits channels formed by TRPC1, TRPC4 and TRPC5. The spider toxin peptide GsMTx4, an inhibitor of mechanosensitive channels, is also listed under Piezo Channel.
(-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca2+-permeable nonselective cation channel, to increase [Ca2+]i. Antitumor activity.
Synonyms: JNJ-39439335
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.
RQ-00203078 is a highly selective, potent and orally available TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively), exhibits >350-fold selectivity for TRPM8 over TRPV4, TRPV1 and TRPA1.
Synonyms: GSK101
GSK1016790A is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells.
SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist.
Synonyms: D-(+)-Camphor; (1R)-(+)-Camphor
Camphor is a waxy, flammable, white or transparent solid with a strong aroma, often used to relieve pain, reduce itching and treat fungal infections. It can activate TRPV1 and TRPV3
Synonyms: B 2796; Lomerizine HCl
Lomerizine dihydrochloride is a antagonist at L-type and T-type Ca 2+ channels and TRp5 channels used to treat migraines and vertigo.
Synonyms: SKF96365
SKF-96365 hydrochloride is a non-selective TRP Channel blocker.
AM-0902 is a potent and selective Transient Receptor Potential A1 (TRPA1) Antagonist.
WS-12 is a potent TRPM8 agonist that acts as a cooling agent (EC50 = 193 nM).
WS 3 is TRPM8 receptors agonist (EC50 = 3.7 μM) and cooling agent.
Synonyms: SAR-7334
SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels that opens new opportunities for the investigation of TRPC channel function in vivo. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50 s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected.
Synonyms: (±)-Camphor
Camphor ((±)-Camphor) is recognized as a TRP channel agonist, primarily targeting TRPV3. This compound exhibits notable antiviral, antitussive, and anticancer activities, making it valuable for various research applications. Although utilized topically for its anti-infective and anti-pruritic properties, caution is advised as camphor can be toxic when ingested. Its diverse biological activities make it a significant candidate for studies related to TRPV channel modulation.
Nonivamide is a capsaicin analogue that exhibits anti-inflammatory properties in peripheral blood mononuclear cells and U-937 macrophages. Nonivamide is a agonist, which exhibits 4d-EC50 value of 5.1 mg/L in static toxicity tests.
Vanillyl butyl ether serves as a repellent agent primarily through its modulation of TRPV1 and TRPM8 channels in mammalian systems. This compound exhibits notable activity against pests such as Tribolium castaneum, T. confusum, and L. bostrychophila, demonstrating its potential in pest control applications. Additionally, it acts as a mild warming agent, promoting enhanced blood circulation while retaining its eco-friendly and non-toxic profile.
Synonyms: phenanthren-9-ol
Selective TRPM4 blocker (IC50 = 20 μM in HEK293 cells). Exhibits no effect on CFTR or TRPM5 (at 0.25 and 1 mM respectively). Abolishes arrhythmias induced by hypoxia in a mouse heart model.
1,4-Cineole is an oxygenated monoterpene that acts as an agonist for the human TRPM8 and TRPA1 channels. It facilitates an increase in intracellular calcium concentration, leading to its potential therapeutic effects. 1,4-Cineole has demonstrated anti-anxiety and anti-depressive properties, making it a candidate for research into neurological diseases, particularly depression.
Citronellyl acetate is a monoterpene compound that serves as an orally active antinociceptive agent. It modulates various targets including TRPV1, TRPM8, ASIC, and glutamate receptors, along with protein kinase pathways PKC and PKA, contributing to its effects on nociception. This compound is valuable for research focused on understanding and managing acute pain mechanisms.
Synonyms: 2-Aminoethyl Diphenylborinate
2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of IP3R. 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca2+ (SOC) channel and activates some TRP channels (V1, V2 and V3).
Synonyms: BRN 4261852; cis-Capsaicin; Civamide; Zucapsaicin; trade name Civanex.
Zucapsaicin, also known as cis-Capsaicin, is a medication used to treat osteoarthritis of the knee and other neuropathic pain. It is applied three times daily for a maximum of three months. It reduces pain, and improves articular functions.
TRPM8 antagonist 2 is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.
AMG2850 is a potent, orally bioavailable and selective transient receptor potential melastatin 8 (TRPM8) antagonist.
JT010 is a potent agonist of TRPA1 with an EC50 of 0.65 nM.
HC-070 is an antagonist of TRPC4/TRPC5, with IC50s of 9.3 nM and 46 nM for hTRPC5 and hTRPC4 in cells, respectively.
