TRPV1 Agonist

Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat.

N-Oleoyldopamine (OLDA) is an orally active TRPV1 activator and 5-LOX inhibitor with blood-brain barrier permeability. N-Oleoyldopamine excites histaminergic neurons in the tuberomammillary nucleus via a dopamine receptor mechanism, a process independent of TRPV1 and cannabinoid receptors. On one hand, N-Oleoyldopamine promotes the release of insulin and glucose-dependent insulinotropic polypeptide through a GPR119-dependent pathway to improve glucose tolerance; on the other hand, N-Oleoyldopamine improves left ventricular function and reduces myocardial infarction size by triggering the release of substance P and calcitonin gene-related peptide. N-Oleoyldopamine is used in studies related to glycemic abnormalities and myocardial ischemia-reperfusion injury.

Olvanil (NE-19550) is an analgesic and an agonist of transient receptor potential vanilloid type 1 (TRPV1) channels with an EC₅₀ of 0.7 nM.

Moringin is a potent and selective TRPA1 ion channel natural agonist with an EC₅₀ of 3.14 μM. Moringin does not activate or activates very weakly the vanilloids somatosensory channels TRPV1, TRPV2, TRPV3 and TRPV4, and the melastatin cooling receptor TRPM8. Moringin has hypoglycemic, antimicrobial, anti-inflammatory, anticancer and neuroprotection activities.

MDR-652 is a highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The K_is are 11.4 and 23.8 nM for hTRPV1 and rTRPV1, respectively. The EC₅₀s are 5.05 and 93 nM for hTRPV1 and rTRPV1, respectively. Potent topical analgesic activity.

Protokylol hydrochloride (Caytine hydrochloride; JB-251 hydrochloride) is the hydrochloride salt form of Protokylol (HY-114630). Protokylol hydrochloride is an agonist for β2-adrenergic receptor and TRPV1. Protokylol hydrochloride exhibits activity as a bronchodilator.

Capsiate, as a capsaicin analogue extracted from a non-pungent cultivar of CH-19 sweet red pepper, is an orally active agonist of TRPV1.

(R)-Methanandamide (AM-356), an analog of the endocannabinoid ligand Anandamide, is a potent CB1 agonist with a K_i of 20 nM. (R)-Methanandamide also activates vanilloid (TRPV1) receptors.

Arvanil (N-Vanillylarachidonamide) is a mixed agonist of CB1 and TRPV1 receptors. Arvanil downregulates CD25, HLA-DR, CD134/OX40, blocks G1/S phase transition, and induces phosphorylation of Akt. Arvanil does not induce apoptosis in cells. Arvanil inhibits lymphocyte activation and ameliorates autoimmune encephalomyelitis. Arvanil can be used in research related to Huntington's disease, vomiting, and multiple sclerosis.

MSP-3 is a potent TRPV1 agonist, with an EC₅₀ of 0.87 μM. MSP-3 exhibits neuroprotective and antinociceptive effects.

Dihydrocapsiate, as a compound of capsinoid family, is an orally active TRPV1 agonist. Dihydrocapsiate can be used for the research of metabolism disease.

Vanillyl butyl ether is a major contributor to the characteristic flavor and fragrance of vanilla. Vanillyl butyl ether is one of the eco-friendly and nontoxic substances. Vanillyl butyl ether exhibits mutually inhibitory effects on mammalian TRPV1 and TRPM8 channels. Vanillyl butyl ether shows repellency activity against Tribolium castaneum, T. confusum and L. bostrychophila. Vanillyl butyl ether acts as a mild warming agent, providing a warming sensation and enhancing blood circulation.

Polygodial pyridazine (compound 7) is a polygodial analogue and a TRPV1 agonist with a GI₅₀ of 72 μM against MCF-7. Polygodial pyridazine can be utilized in cancer research.

SA-13353 is a TRPV1 agonist with cardioprotective effect. SA-13353 can be used for the research of cardiovascular disease .

TRPV1/CB2 agonist 1 (compound 41) is a TRPV1/CB2 agonist, with an EC₅₀ of 26.8 μM for hTRPV1. TRPV1/CB2 agonist 1 can be used in nervous system related research.