For research use only. Not for therapeutic Use.
Priralfinamide, also known as Ralfinamide, FCE-26742A; NW-1029; PNU-0154339E, is a Na-channel blocker for the treatment of neuropathic pain and other pain conditions such as post-operative dental pain. It has a relatively complex pharmacology, acting as a mixed voltage-gated sodium channel blocker (including Nav1.7), N-type calcium channel blocker, noncompetitive NMDA receptor antagonist, and monoamine oxidase B inhibitor.
Catalog Number | M117811 |
CAS Number | 133865-88-0 |
Molecular Formula | C17H19FN2O2 |
Purity | ≥95% |
Target | Sodium Channel |
Storage | -20°C |
IUPAC Name | (2S)-2-[[4-[(2-fluorophenyl)methoxy]phenyl]methylamino]propanamide |
InChI | InChI=1S/C17H19FN2O2/c1-12(17(19)21)20-10-13-6-8-15(9-7-13)22-11-14-4-2-3-5-16(14)18/h2-9,12,20H,10-11H2,1H3,(H2,19,21)/t12-/m0/s1 |
InChIKey | BHJIBOFHEFDSAU-LBPRGKRZSA-N |
SMILES | CC(C(=O)N)NCC1=CC=C(C=C1)OCC2=CC=CC=C2F |
Reference | </br> 1: Di Stefano AF, Radicioni MM, Rusca A. Pressor response to oral tyramine and monoamine oxidase inhibition during treatment with ralfinamide (NW-1029). Neurotox Res. 2013 May;23(4):315-26. doi: 10.1007/s12640-012-9344-5. Epub 2012 Aug 8. PubMed PMID: 22872464.</br>2: Bauer M, Bliesath H, Leuratti C, Lackner E, Dieterle W, Müller M, Brunner M. Disposition and metabolism of ralfinamide, a novel Na-channel blocker, in healthy male volunteers. Pharmacology. 2010;86(5-6):297-305. doi: 10.1159/000321322. Epub 2010 Nov 11. PubMed PMID: 21071997.</br>3: Browne LE, Clare JJ, Wray D. Functional and pharmacological properties of human and rat NaV1.8 channels. Neuropharmacology. 2009 Apr;56(5):905-14. doi: 10.1016/j.neuropharm.2009.01.018. Epub 2009 Jan 31. PubMed PMID: 19371587.</br>4: Zhang SH, Blech-Hermoni Y, Faravelli L, Seltzer Z. Ralfinamide administered orally before hindpaw neurectomy or postoperatively provided long-lasting suppression of spontaneous neuropathic pain-related behavior in the rat. Pain. 2008 Oct 15;139(2):293-305. doi: 10.1016/j.pain.2008.04.020. Epub 2008 Jun 25. PubMed PMID: 18583049.</br>5: Yamane H, de Groat WC, Sculptoreanu A. Effects of ralfinamide, a Na+ channel blocker, on firing properties of nociceptive dorsal root ganglion neurons of adult rats. Exp Neurol. 2007 Nov;208(1):63-72. Epub 2007 Jul 19. PubMed PMID: 17707373; PubMed Central PMCID: PMC2117901.</br>6: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2005 Jul-Aug;27(6):411-61. PubMed PMID: 16179960.</br>7: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2005 Mar;27(2):145-59. PubMed PMID: 15834466.</br>8: Stummann TC, Salvati P, Fariello RG, Faravelli L. The anti-nociceptive agent ralfinamide inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive Na+ currents in dorsal root ganglion neurons. Eur J Pharmacol. 2005 Mar 14;510(3):197-208. PubMed PMID: 15763243.</br>9: Cattabeni F. Ralfinamide. Newron Pharmaceuticals. IDrugs. 2004 Oct;7(10):935-9. PubMed PMID: 15478019.</br></br></br> |