Bioactivity | 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]. |
Invitro | TRPV3 antagonist 74a (100 μΜ; 2300 seconds; keratinocytes) largely attenuates SLIGRL or SLIGKV-induced Ca2+ responses[2]. |
In Vivo | 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: |
Name | TRPV3 antagonist 74a |
CAS | 1432051-63-2 |
Formula | C17H17F3N2O2 |
Molar Mass | 338.32 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |