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AMG 9810
- Soluble in DMSO and EtOH
- MF: C21H23NO3
- MW: 337.41
Description
AMG 9810 is a potent and selective vanilloid receptor-1 (TRPV1) antagonist with antihyperalgesic properties (IC50 value for human TRPV1, 24.5 +/- 15.7 nM; rat TRPV1, 85.6 +/- 39.4 nM). Also, AMG 9810 blocks all known modes of TRPV1 activation, including protons (IC50 value for rat TRPV1, 294 +/- 192 nM; human TRPV1, 92.7 +/- 72.8 nM), heat (IC50 value for rat TRPV1, 21 +/- 17 nM; human TRPV1, 15.8 +/- 10.8 nM), and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine.
More Information
| Parent CAS No. | 545395-94-6 |
|---|---|
| Chemical Name | (E)-3-(4-tert-Butylphenyl)-N-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)acrylamide |
| SMILES | C1OC2C=CC(NC(=O)/C=C/C3C=CC(C(C)(C)C)=CC=3)=CC=2OC1 |
| MFCD | MFCD00955103 |
| InChi | InChI=1S/C21H23NO3/c1-21(2,3)16-7-4-15(5-8-16)6-11-20(23)22-17-9-10-18-19(14-17)25-13-12-24-18/h4-11,14H,12-13H2,1-3H3,(H,22,23)/b11-6+ |
| InChiKey | GZTFUVZVLYUPRG-IZZDOVSWSA-N |
| CID | 680502 |
| Short Description | TRPV1 antagonist |
References
- EM Doherty et al. Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides. J Med Chem. 2005 Jan 13;48(1):71-90.
- NR Gavva et al. AMG 9810 [(E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic properties. J Pharmacol Exp Ther. 2005 Apr;313(1):474-84.


