TRPV1 Inhibitor

Tivanisiran (SYL1001) is a small interfering RNA (siRNA) targeting TRPV1 . Tivanisiran induces the degradation of TRPV1 mRNA, thereby inhibiting protein synthesis. Tivanisiran alleviates ocular discomfort and pain, and improves ocular hyperemia and tear quality. Tivanisiran is applicable to research related to dry eye disease.

Tivanisiran sodium (SYL1001 sodium) is a small interfering RNA (siRNA) targeting TRPV1 . Tivanisiran sodium induces the degradation of TRPV1 mRNA, thereby inhibiting protein synthesis. Tivanisiran sodium alleviates ocular discomfort and pain, and improves ocular hyperemia and tear quality. Tivanisiran sodium is applicable to research related to dry eye disease.

(±)-Eriodictyol ((±)-Huazhongilexone; Dihydroluteolin) is an orally active TRPV1 receptor antagonist (IC₅₀=44-47 nM, rTRPV1) with antioxidant and anti-inflammatory activities. (±)-Eriodictyol effectively inhibits lipid peroxidation and the release of proinflammatory cytokines by specifically antagonizing the TRPV1 receptor and activating the Nrf2 signaling pathway. (±)-Eriodictyol reduces the levels of ICAM-1, VEGF, eNOS and TNF-α in the retina and maintains the integrity of the blood-retinal barrier. (±)-Eriodictyol alleviates oxidative stress-induced apoptosis and hyperalgesia, enhances the activity and cytotoxicity of immune cells (such as B lymphocytes, NK cells and macrophages), and increases the levels of antioxidant enzymes simultaneously. (±)-Eriodictyol can be used in the research of diabetic retinopathy, acute lung injury and various pain-related diseases.

Chrysin 6-C-glucoside 8-C-arabinoside can inhibit the CGRP releasing and the activation of TRPV1 channel. Chrysin 6-C-glucoside 8-C-arabinoside can be used for anti-migraine research.

FAAH/TRPV1 blocker-1 (compound 2R) is a dual FAAH/TRPV1 blocker, with IC₅₀ of 0.12 and 94.9 μM, respectively. FAAH/TRPV1 blocker-1 plays an important role in analgesic and anti-inflammatory research.

TL-119 (A-3302-B) is a polypeptide. TL-119 can be isolated from the bacteria Micromonospora sp. MAG 9-7 and Saccharomonospora sp. CNQ-490. TL-119 inhibits TRPV-1. TL-119 exhibits antiviral activity against HSV-2. TL-119 possesses anticancer activity against gastric cancer and colorectal cancer.

Ovalicin is a multi-target inhibitor that targets MetAP2, HRH2, JAK2 and TRPV1, with anti-inflammatory and anti-atopic dermatitis activities. Ovalicin covalently binds to MetAP2 to inhibit its function, thereby blocking the replication of Enterocytozoon bieneusi and Vittaforma corneae. Ovalicin alleviates intestinal injury and prolongs survival in infected mouse models, without showing obvious hepatorenal toxicity. Ovalicin attenuates LPS-induced calcium influx, reduces the infiltration of macrophages and mast cells in the skin, and regulates the expression of inflammation-related genes such as IL-31, effectively relieving allergic symptoms in mouse models. Ovalicin can be used for the research of microsporidiosis and atopic dermatitis.

A 80426 is an orally active serotonin (5-HT uptake) inhibitor (IC₅₀ = 13 nM; K_i = 3.8 nM) and α₂-Adrenoceptor receptor antagonist (K_i = 2 nM). A 80426 shows weak antagonistic effect to dopamine D₁ receptor (K_i = 744 nM) and D₂ receptor (K_i = 52 nM). A 80426 upregulates the expression and activity of TRPV1, activates the NF-κB and PI3K pathways, and reduces the levels of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. A 80426 can be used in research related to inflammatory pain and depression.

DD-161515 is a TRPV1/VR1 inhibitor with an IC₅₀ of 0.7 μM in rats. DD-161515 binds to an allosteric site of TRPV1 distinct from that of capsaicin, blocks channel opening, inhibits receptor-mediated calcium ion influx, reduces the excitability of peripheral sensory nerve fibers, and thereby inhibits nociception induced by heat and transmission of chemically induced pain signals. DD-161515 can be used in studies related to inflammatory pain.