Lermontova N N, Redkozubov A E, Shevtsova E F, Serkova T P, Kireeva E G, Bachurin S O
Department of Biological Research, Institute of Physiologically Active Substances, Russian Academy of Sciences, Chernogolovka, Moscow Region.
Bull Exp Biol Med. 2001 Nov;132(5):1079-83. doi: 10.1023/a:1017972709652.
Dimebon, a Russian-made drug, inhibited toxic effects of beta -amyloid on cultured neurons. Excessive accumulation of beta-amyloid in the brain is characteristic of Alzheimer dementias. Antialzheimer preparations tacrine and dimebon improve survival of cerebellar granule cells during long-term incubation with Abeta25-35, the neurotoxic fragment of beta-amyloid. Both preparations can block potential-dependent Ca(2+) entry into neurons by about 20%, which is explained by their selective action on L-type Ca(2+) channels. It was assumed that the neuroprotective effect of dimebon and tacrine against Abeta25-35 partially depends on inhibition of potential-dependent Ca(2+) entry.
二苯美伦是一种俄罗斯制造的药物，可抑制β-淀粉样蛋白对培养神经元的毒性作用。大脑中β-淀粉样蛋白的过度积累是阿尔茨海默病痴呆症的特征。抗阿尔茨海默病制剂他克林和二苯美伦可提高小脑颗粒细胞在与β-淀粉样蛋白的神经毒性片段Abeta25-35长期孵育期间的存活率。两种制剂均可使依赖电位的Ca(2+)进入神经元的量减少约20%，这是由于它们对L型Ca(2+)通道具有选择性作用。据推测，二苯美伦和他克林对Abeta25-35的神经保护作用部分取决于对依赖电位的Ca(2+)进入的抑制。
