Ifenprodil(NP-120,别名Dilvax、RC61-91)是作用于多重靶点的化合物,兼具脑血管扩张作用与多种生物活性,适用于特定疾病研究且有神经系统疾病治疗潜力。它是选择性NMDA受体拮抗剂(优先抑制含NR2B亚基受体,NR1A/NR2B的IC50=0.34μM,是NR1A/NR2A的400多倍),同时也是α1肾上腺素受体拮抗剂、GIRK(Kir3)抑制剂,还能抑制甲型H1N1流感病毒(EC50=6.6µM),具有神经保护、抗惊厥、抗伤害作用,可用于脑血管疾病和外周动脉闭塞性疾病研究。
[1] Williams K. Ifenprodil discriminates subtypes of the N-methyl-D-aspartate receptor: selectivity and mechanisms at recombinant heteromeric receptors. Mol Pharmacol. 1993 Oct;44(4):851-9. PMID: 7901753.[2]Kobayashi T, Washiyama K, Ikeda K. Inhibition of G protein-activated inwardly rectifying K+ channels by ifenprodil. Neuropsychopharmacology. 2006 Mar;31(3):516-24. doi: 10.1038/sj.npp.1300844. PMID: 16123769.[3]Chen YW, Chiu CC, Wang JN, Hung CH, Wang JJ. Ifenprodil for prolonged spinal blockades of motor function and nociception in rats. Pharmacol Rep. 2016 Apr;68(2):357-62. doi: 10.1016/j.pharep.2015.09.011. Epub 2016 Jan 14. PMID: 26922539.





