trpm8

Elismetrep (MT-8554) is an orally available TRPM8 inhibitor with potential analgesic activity for the study of vasomotor symptoms in postmenopausal women.

RQ-00203078 is a highly selective, potent, and orally available TRPM8 antagonist.

TC-I2000 is an TRPM8 channel blocker. Inhibits icilin-induced TRPM8 channel activation in rTRPM8-expressing CHO cells with IC50 of 53 nM.

TRPM8 antagonist WS-3 (Cyclohexanecarboxamide) is an agonist of TRPM8( EC50 : 3.7 μM).

TRPM8 antagonist 3 is a blocker of TRPM8 (IC50 = 11 nM).

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.

D-3263 hydrochloride (D3263 HCl salt) is enteric-coated, orally bioavailable transient receptor potential melatonin member 8 (TRPM8) agonist.

WS-12 is a potent TRPM8 agonist that acts as a cooling agent (EC50 : 193 nM)

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.

1. Pulegone ((+)-Pulegone) has cytotoxicity followed by regenerative cell proliferation is the MOA for Pulegone-induced urothelial tumors in female rats. 2. Pulegone induces a verapamil-sensitive psychostimulant effect that appears to independ on the opening of L-type calcium channels. 3. Pulegone has negative reinforcing properties and seems to possess anxiolytic-like actions unrelated to the benzodiazepine site of the γ-aminobutyric acid type A (GABAA) receptor.

(-)-Menthol (Levomenthol) is a levo isomer of menthol, an organic compound made synthetically or obtained from peppermint or mint oils with flavoring and local anesthetic properties. When added to pharmaceuticals and foods, menthol functions as a fortifier for peppermint flavors. It also has a counterirritant effect on skin and mucous membranes, thereby producing a local analgesic or anesthetic effect.

1,4-Cineole (Isocineole) is a natural, oxygenated monoterpene. 1,4-Cineole can activate both human TRPM8 and human TRPA1.

ICILIN (AG-3-5) is a synthetic TRPM8 ion channel super-agonist.

FEMA-4809, a highly potent TRPM8 receptor activator, TRPM8 is the ion channel responsible for the cool perception, which is triggered either by temperatures below 25 °C or by ligands such as (-)-menthol. FEMA-4809 is used as a cooling agent.

RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 agonist (EC50: hTRPV4 of 0.77 μM, mTRPV4 of 4.0 μM, and rTRPV4 of 4.1 μM) and also acts as an antagonist for TRPM8 (IC50: 4 μM).

TC-I 2014 shows antiallodynic properties in pain models. TC-I 2014 is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 antagonist (IC50: 0.8 nM, 3.0 nM, and 4.4 nM for canine, human and rat channels respectively).

beta-Eudesmol (Beta-Selinenol) is a noncompetitive antagonist of nicotinic acetylcholine receptors (nAChRs). It is a sesquiterpene that has been found in a variety of plants, including Cannabis, and has diverse biological activities.

BCTC is a potent TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 (IC50 of 35 and 6 nM, respectively)

AMG2850 is a potent, orally bioavailable, and selective antagonist of transient receptor potential melastatin 8 [TRPM8].

M8-B Hydrochloride is a selective transient receptor potential melastatin-8 (TRPM8) channel antagonist.

Cryosim-1 is a TRPM8 agonist.

DFL23448 is a TRPM8-selective ion channel antagonist, modifying bladder function and reduces bladder overactivity in awake rats.

AMG8788 is a selective, potent and orally active TRPM8 antagonist (IC50: 63.2 nM).

AMG9678 is a selective, potent, orally active TRPM8 antagonist with an IC50 of 31.2 nM.