Lifarizine

• CAT Number: M017544
• CAS Number: 119514-66-8
• Molecular Formula: C29H32N4
• Molecular Weight: 436.603
• Purity: ≥95%
• Target: calcium and sodium channel antagonist
• Storage: Store at -20°C
• IUPAC Name: 1-benzhydryl-4-[[5-methyl-2-(4-methylphenyl)-1H-imidazol-4-yl]methyl]piperazine
• InChI: InChI=1S/C29H32N4/c1-22-13-15-26(16-14-22)29-30-23(2)27(31-29)21-32-17-19-33(20-18-32)28(24-9-5-3-6-10-24)25-11-7-4-8-12-25/h3-16,28H,17-21H2,1-2H3,(H,30,31)
• InChIKey: HTDFEXRUDGWNHA-UHFFFAOYSA-N
• SMILES: CC1=CC=C(C=C1)C2=NC(=C(N2)C)CN3CCN(CC3)C(C4=CC=CC=C4)C5=CC=CC=C5

Lifarizine, also known as RS-87476, is a calcium and sodium channel antagonist potentially for the treatment of stroke. Lifarizine (RS-87476) showed neuroprotective efficacy in a simplified rat survival model of 2 vessel occlusion. The effects of lifarizine on intracellular Ca2+ and glutamate exocytosis may contribute to its neuroprotective action.

Reference

1:Inhibition by lifarizine of intracellular Ca2+ rises and glutamate exocytosis in depolarized rat cerebrocortical synaptosomes and cultured neurones. Budd DC, May GR, Nicholls DG, McCormack JG.Br J Pharmacol. 1996 May;118(1):162-6. PMID: 8733590 Free PMC Article2:Neuroprotective efficacy of lifarizine (RS-87476) in a simplified rat survival model of 2 vessel occlusion. McBean DE, Winters V, Wilson AD, Oswald CB, Alps BJ, Armstrong JM.Br J Pharmacol. 1995 Dec;116(8):3093-8. PMID: 8719782 Free PMC Article3:Efficacy and tolerability of lifarizine in acute ischemic stroke. A pilot study. Lifarizine Study Group. Squire IB, Lees KR, Pryse-Phillips W, Kertesz A, Bamford J.Ann N Y Acad Sci. 1995 Sep 15;765:317-8. No abstract available. PMID: 7486628 4:Selectivity of the neuroprotective agent lifarizine. Sheridan RD.Trends Pharmacol Sci. 1995 Sep;16(9):292. No abstract available. PMID: 7482992 5:Reduction by lifarizine of the neuronal damage induced by cerebral ischaemia in rodents. Alps BJ, Calder C, Wilson AD, McBean DE, Armstrong JM.Br J Pharmacol. 1995 Aug;115(8):1439-46. PMID: 8564203 Free PMC Article6:Neuroprotective properties of lifarizine compared with those of other agents in a mouse model of focal cerebral ischaemia. Brown CM, Calder C, Linton C, Small C, Kenny BA, Spedding M, Patmore L.Br J Pharmacol. 1995 Aug;115(8):1425-32. PMID: 8564201 Free PMC Article7:[3H]-lifarizine, a high affinity probe for inactivated sodium channels. MacKinnon AC, Wyatt KM, McGivern JG, Sheridan RD, Brown CM.Br J Pharmacol. 1995 Jul;115(6):1103-9. PMID: 7582509 Free PMC Article8:Neuroprotective profile of lifarizine (RS-87476) in rat cerebrocortical neurones in culture. May GR, Rowand WS, McCormack JG, Sheridan RD.Br J Pharmacol. 1995 Apr;114(7):1365-70. PMID: 7606340 Free PMC Article9:Actions of the novel neuroprotective agent, lifarizine (RS-87476), on voltage-dependent sodium currents in the neuroblastoma cell line, N1E-115. McGivern JG, Patmore L, Sheridan RD.Br J Pharmacol. 1995 Apr;114(8):1738-44. PMID: 7599943 Free PMC Article10:Block of human voltage-sensitive Na+ currents in differentiated SH-SY5Y cells by lifarizine. Brown NA, Kemp JA, Seabrook GR.Br J Pharmacol. 1994 Oct;113(2):600-6. PMID: 7834213 Free PMC Article