For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I037564 |
| CAS Number | 1432051-63-2 |
| Synonyms | 3-[(S)-hydroxy(pyridin-2-yl)methyl]-1-methyl-3-[4-(trifluoromethyl)pyridin-2-yl]cyclobutan-1-ol |
| Molecular Formula | C17H17F3N2O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C17H17F3N2O2/c1-15(24)9-16(10-15,14(23)12-4-2-3-6-21-12)13-8-11(5-7-22-13)17(18,19)20/h2-8,14,23-24H,9-10H2,1H3/t14-,15?,16?/m1/s1 |
| InChIKey | MTJXDHFAWXGXIN-QQFBHYJXSA-N |
| SMILES | CC1(CC(C1)(C2=NC=CC(=C2)C(F)(F)F)C(C3=CC=CC=N3)O)O |
| 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. |
