TRPV1 Activator

Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoid receptors (CB1 and CB2). Anandamide can activate numerous other receptors like PPARS, TRPV1, and GPR18/GPR55. Anandamide also has potential anti-fungal and anti-inflammatory activities. Anandamide can be used for the research of Alzheimer’s disease (AD) and ulcerative colitis.

LE135 is a potent RAR antagonist that binds selectively to RARα (K_i of 1.4 μM) and RARβ (K_i of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC₅₀s of 2.5 μM and 20 μM, respectively.

N-Arachidonyldopamine acts as an Anandamide (HY-10863) membrane transport inhibitor, a selective CB₁ cannabinoid receptor agonist, and a VR1 receptor activator. It exhibits an EC₅₀ value of 48 nM for rat VR1 and a K_i value of 0.25 μM for CB1. N-Arachidonyldopamine exists in mammalian neural tissues. It stimulates intracellular Ca²⁺ mobilization, mediates cannabinoid-like effects, and induces hypothermia, hypomotility, catalepsy, analgesia, and hyperalgesia to heat. N-Arachidonyldopamine possesses anticancer activity against breast cancer. It can be used in research related to breast cancer and heat hyperalgesia.

N-Arachidonoyl Taurine is an activator of the transient receptor potential vanilloid TRPV1 and TRPV4, with EC₅₀s value of 28 μM and 21 μM, respectively.

JTE-907 is a selective and orally active cannabinoid CB2 receptor inverse agonist and exerts anti-inflammatory effects. JTE-907 upregulates IL-6, MCP-1, IL-1β, VEGF, ANGPTL4, and TRPV1 in mature adipocytes. JTE-907 downregulates CB1, MCP-1, and IL-1β in preadipocytes. JTE-907 inhibits ear swelling in mice. JTE-907 reverses the protective effects of CB2 agonists and Anandamide (HY-10863) against cytokine-evoked colonic mucosal damage. JTE-907 can be used for the research of allergic dermatitis, obesity, and colitis.

AM9053 is a selective, effective and slowly reversible inhibitor of N-acyl ethanolamine acid amidease (NAAA) (IC₅₀ = 30 nM). The effect of AM9053 on FAAH activity is limited (IC₅₀ > 100 nM). AM9053 inhibits the proliferation of colorectal cancer cells by activating the PPAR-α and TRPV1 dependent mechanisms and induces S-phase cell cycle arrest. AM9053 alleviates intestinal fibrosis by regulating macrophage activity and inhibiting the IL-23 signaling pathway. AM9053 leads to an increase in NAE levels, especially PEA and OEA. AM9053 can be used for the study of colorectal cancer and intestinal fibrosis.

20-Hydroxy-N-arachidonoyl taurine (Compound C20:4 NAT) acts as an activator of TRPV1 and TRPV4, with EC₅₀ values of 28 µM and 21 µM, respectively. 20-Hydroxy-N-arachidonoyl taurine serves as a substrate for fatty acid amide hydrolase (FAAH).

4,5-Di-O-caffeoylquinic acid, an active compound, is isolated from sweetpotato (Ipomoea batatas L.). 4,5-Di-O-caffeoylquinic acid suppresses inflammatory responses through TRPV1 activation.