Kralic Jason E, Criswell Hugh E, Osterman Jessica L, O'Buckley Todd K, Wilkie Mary E, Matthews Douglas B, Hamre Kristin, Breese George R, Homanics Gregg E, Morrow A Leslie
Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina 27599-7178, USA.
J Clin Invest. 2005 Mar;115(3):774-9. doi: 10.1172/JCI23625.
Essential tremor is the most common movement disorder and has an unknown etiology. Here we report that gamma-aminobutyric acidA (GABA(A)) receptor alpha1-/- mice exhibit postural and kinetic tremor and motor incoordination that is characteristic of essential tremor disease. We tested mice with essential-like tremor using current drug therapies that alleviate symptoms in essential tremor patients (primidone, propranolol, and gabapentin) and several candidates hypothesized to reduce tremor, including ethanol; the noncompetitive N-methyl-D-aspartate receptor antagonist MK-801; the adenosine A1 receptor agonist 2-chloro-N6-cyclopentyladenosine (CCPA); the GABA(A) receptor modulators diazepam, allopregnanolone, and Ro15-4513; and the L-type Ca2+ channel antagonist nitrendipine. Primidone, propranolol, and gabapentin reduced the amplitude (power) of the pathologic tremor. Nonsedative doses of ethanol eliminated tremor in mice. Diazepam, allopregnanolone, Ro15-4513, and nitrendipine had no effect or enhanced tremor, whereas MK-801 and CCPA reduced tremor. To understand the etiology of tremor in these mice, we studied the electrophysiological properties of cerebellar Purkinje cells. Cerebellar Purkinje cells in GABA(A) receptor alpha1-/- mice exhibited a profound loss of all responses to synaptic or exogenous GABA, but no differences in abundance, gross morphology, or spontaneous synaptic activity were observed. This genetic animal model elucidates a mechanism of GABAergic dysfunction in the major motor pathway and potential targets for pharmacotherapy of essential tremor.
特发性震颤是最常见的运动障碍性疾病,其病因不明。在此我们报告,γ-氨基丁酸A(GABA(A))受体α1基因敲除小鼠表现出姿势性和运动性震颤以及运动不协调,这些都是特发性震颤疾病的特征。我们使用当前可缓解特发性震颤患者症状的药物疗法(扑米酮、普萘洛尔和加巴喷丁)以及几种被推测可减轻震颤的候选药物对具有类似特发性震颤的小鼠进行了测试,这些候选药物包括乙醇;非竞争性N-甲基-D-天冬氨酸受体拮抗剂MK-801;腺苷A1受体激动剂2-氯-N6-环戊基腺苷(CCPA);GABA(A)受体调节剂地西泮、别孕烯醇酮和Ro15-4513;以及L型钙通道拮抗剂尼群地平。扑米酮、普萘洛尔和加巴喷丁降低了病理性震颤的幅度(功率)。非镇静剂量的乙醇消除了小鼠的震颤。地西泮、别孕烯醇酮、Ro15-4513和尼群地平没有效果或加重了震颤,而MK-801和CCPA减轻了震颤。为了了解这些小鼠震颤的病因,我们研究了小脑浦肯野细胞的电生理特性。GABA(A)受体α1基因敲除小鼠的小脑浦肯野细胞对突触或外源性GABA的所有反应均显著丧失,但在数量、大体形态或自发突触活动方面未观察到差异。这种基因动物模型阐明了主要运动通路中GABA能功能障碍的机制以及特发性震颤药物治疗的潜在靶点。