Molecular Biology Unit, Mossakowski Medical Research Centre, Polish Academy of Sciences, 5 Pawinskiego Str, 02-106 Warsaw, Poland.
Neurochem Res. 2011 Nov;36(11):2091-5. doi: 10.1007/s11064-011-0568-1. Epub 2011 Aug 13.
Biphalin is a dimeric opioid peptide that exhibits affinity for three types of opioid receptors (MOP, DOP and KOP). Biphalin is undergoing intensive preclinical study. It was recognized that activation of δ-opioid receptor elicits neuroprotection against brain hypoxia and ischemia. We compare the effect of biphalin and morphine and the inhibition of opioid receptors by naltrexone on survival of neurons in rat organotypic hippocampal cultures challenged with NMDA.
(1) 0.025-0.1 μM biphalin reduces NMDA-induced neuronal damage; (2) biphalin neuroprotection is abolished by naltrexone; (3) reduced number of dead cells is shown even if biphalin is applied with delay after NMDA challenge.
双啡肽是一种二聚体阿片肽,对三种类型的阿片受体(MOP、DOP 和 KOP)具有亲和力。双啡肽正在进行深入的临床前研究。人们认识到,δ-阿片受体的激活可以引发对脑缺氧和缺血的神经保护作用。我们比较了双啡肽和吗啡以及纳曲酮对 NMDA 挑战的大鼠器官型海马培养物中神经元存活的影响。
(1)0.025-0.1μM 双啡肽可减少 NMDA 诱导的神经元损伤;(2)纳曲酮可消除双啡肽的神经保护作用;(3)即使在 NMDA 挑战后延迟给予双啡肽,也显示出死亡细胞数量减少。