TRPV3 74a

TRPV3 antagonist 74a is a potent and selective TRPV3 antagonist. TRPV3 antagonist 74a displays no significant activity against a panel of other ion channels. TRPV3 antagonist 74a can be used for the research of neuropathic pain[1][2].

Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel

Research Areas >> Neurological Disease

TRPV3

TRPV3 antagonist 74a (100 μΜ; 2300 seconds; keratinocytes) largely attenuates SLIGRL or SLIGKV-induced Ca2+ responses[2].

TRPV3 antagonist 74a (150 μg; intradermal injection; 30 minutes) decreases the number of scratches significantly[2]. .TRPV3 antagonist 74a (10~100 mg/kg; p.o.) dose-dependently attenuates mechanical allodynia induced by von Frey hair stimulation to the ipsilateral (injured) hind paw. TRPV3 antagonist 74a exhibits anti-nociceptive activity in the reserpine model of central pain by increasing muscle pressure threshold[1]. Animal Model: WT mice Dosage: 150 μg Administration: Intradermal injection; 30 minutes Result: The number of scratches decreased significantly.

[1]. Gomtsyan A, et al. Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists. J Med Chem. 2016;59(10):4926-4947.

[2]. Zhao J, et al. PAR2 Mediates Itch via TRPV3 Signaling in Keratinocytes. J Invest Dermatol. 2020;140(8):1524-1532.