trpm8

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.

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

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

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.

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

(-)-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.

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

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

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).

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

Pico145 (HC-608) is a remarkable inhibitor of TRPC1 4 5 channels, specifically inhibiting ( )-englerin A-activated TRPC4 TRPC5 channels with IC50s of 0.349 and 1.3 nM in cells, while showing no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, or TRPM8.

PF-05105679 is a selective TRPM8 antagonist (IC50 = 103 nM). PF-05105679 can be used in research on cold-related pain.

AMG 333 is TRPM8 antagonist with an IC50 of 13 nM,a Clinical Candidate for the Treatment of Migraine.

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.

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

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

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).

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

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

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

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

AMTB hydrochloride (AMTB HCl) is a novel TRPM8 channel blocker and is effective for pain and urinary diseases. AMTB can act on the bladder afferent pathway to attenuate the bladder micturition reflex and nociceptive reflex responses in the rat.

Cryosim-3 is a water-soluble, potent, and selective TRPM8 receptor agonist.

Cryosim-1 is a TRPM8 agonist.

RN-9893 is an antagonist of transient receptor potential vanilloid 4 (TRPV4; IC50s = 0.42 and 0.66 μM, respectively, for the human and rat receptors).1 It is selective for TRPV4 over TRPV1, TRPV3, and TRPM8 (IC50s = 10, >30, and 30 μM, respectively). RN-9893 reduces rat TRPV4 activity induced by 4α-phorbol 12,13-didecanoate or hypotonicity (IC50s = 0.57 and 2.1 μM, respectively, in cell free assays). |1. Wei, Z.L., Nguyen, M.T., O'Mahony, D.J., et al. Identification of orally-bioavailable antagonists of the TRPV4 ion-channel. Bioorg. Med. Chem. Lett. 25(18), 4011-4015 (2015).

Selective TRPC5 activator (EC50 = 1.4 μM in a calcium influx assay, 1.3 μM in whole cell patch clamp assay). Displays >14.5-fold selectivity for TRPC5 over other TRP channels (EC50 = 20.6 μM for TRPM8). Also activates TRPC1:5 and TRPC4:5 heteromers. Beckmann et al (2017) A benzothiadiazine derivative and methylprednisolone are novel and selective activators of transient receptor potential canonical 5 (TRPC5) channels. Cell Calcium. 66 10 PMID:28807145

D-3263 is an agonist of transient receptor potential melatonin member 8 (TRPM8) with potential antitumor activity.