Truong L, Allbutt H N, Coster M J, Kassiou M, Henderson J M
Department of Pharmacology, Bosch Building, Bosch Institute & School of Medical Sciences, University of Sydney, NSW 2006, Australia.
Brain Res Bull. 2009 Feb 16;78(2-3):91-6. doi: 10.1016/j.brainresbull.2008.10.004. Epub 2008 Nov 11.
Experimental lesions involving the parafascicular (Pf) nucleus and medial forebrain bundle (MFB) may model to some extent the pathological loss of glutamatergic neurons from the centromedian-parafascicular (CM-Pf) complex and nigral dopaminergic cell loss observed clinically at post-mortem in Parkinson's disease (PD) cases. Our study investigated whether there were alterations in symptomatology in such rats with unilateral 6-OHDA+Pf lesions after treatment with either a selective NR1A/NR2B NMDA antagonist and/or l-dopa. Rats were given dual surgery to the MFB with 6-hydroxydopamine (6-OHDA) and Pf with N-methyl-d-aspartate (NMDA). (i) An NR1A/NR2B selective NMDA antagonist (BZAD-01; 10mg/kg), (ii) l-dopa (25mg/kg), (iii) BZAD-01+l-dopa (10mg/kg; 25mg/kg) or (iv) vehicle solution were administered for 6 weeks, during which behavioural testing was performed. BZAD-01 improved postural asymmetry in the first month as well as apomorphine-induced rotation. The latter was also improved by l-dopa in this model. These data support the use of selective NR1/NR2B NMDA antagonists in the therapeutics of PD.
涉及束旁核(Pf)和内侧前脑束(MFB)的实验性损伤在一定程度上可能模拟帕金森病(PD)患者尸检时临床上观察到的中央中核-束旁核(CM-Pf)复合体谷氨酸能神经元的病理性丧失以及黑质多巴胺能细胞的丧失。我们的研究调查了在用选择性NR1A/NR2B NMDA拮抗剂和/或左旋多巴治疗后,单侧6-OHDA + Pf损伤的大鼠的症状是否有改变。给大鼠进行双侧手术,一侧MFB注射6-羟基多巴胺(6-OHDA),另一侧Pf注射N-甲基-D-天冬氨酸(NMDA)。(i)给予NR1A/NR2B选择性NMDA拮抗剂(BZAD-01;10mg/kg),(ii)左旋多巴(25mg/kg),(iii)BZAD-01 + 左旋多巴(10mg/kg;25mg/kg)或(iv)赋形剂溶液,持续给药6周,在此期间进行行为测试。BZAD-01在第一个月改善了姿势不对称以及阿扑吗啡诱导的旋转。在该模型中,左旋多巴也改善了后者。这些数据支持在PD治疗中使用选择性NR1/NR2B NMDA拮抗剂。