两种新型突触囊泡蛋白2A（SV2A）配体——布立西坦和司来西坦，可改善dt sz突变仓鼠的阵发性肌张力障碍。
Brivaracetam and seletracetam, two new SV2A ligands, improve paroxysmal dystonia in the dt sz mutant hamster.
作者信息
Hamann Melanie, Sander Svenja E, Richter Angelika
机构信息
Institute of Pharmacology and Toxicology, Faculty of Veterinary Medicine, Freie Universität Berlin, 14195 Berlin, Germany.
出版信息
Eur J Pharmacol. 2008 Dec 28;601(1-3):99-102. doi: 10.1016/j.ejphar.2008.10.048. Epub 2008 Nov 6.
Previous examinations demonstrated antidystonic effects of the synaptic vesicle protein 2A (SV2A) ligand levetiracetam in the dt(sz) mutant hamster, an animal model of paroxysmal non-kinesiogenic dyskinesia in which dystonic episodes can be induced by stress. In the present study, we examined the effects of the two new, high affinity SV2A ligands, brivaracetam and seletracetam, in comparison to levetiracetam on the severity of dystonia in mutant hamsters. Seletracetam (50 and 75 mg/kg i.p.) and brivaracetam (75 mg/kg i.p.) reduced the severity of dystonia to a comparable extent as levetiracetam (50 and 75 mg/kg i.p.). These data confirm the therapeutic potential of these pyrrolidone derivatives for the treatment of paroxysmal dystonia.
先前的研究表明，在dt(sz)突变仓鼠（一种阵发性非运动诱发性运动障碍的动物模型，其中应激可诱发肌张力障碍发作）中，突触囊泡蛋白2A（SV2A）配体左乙拉西坦具有抗肌张力障碍作用。在本研究中，我们比较了两种新型高亲和力SV2A配体布瓦西坦和西来西坦与左乙拉西坦对突变仓鼠肌张力障碍严重程度的影响。西来西坦（腹腔注射50和75mg/kg）和布瓦西坦（腹腔注射75mg/kg）降低肌张力障碍严重程度的程度与左乙拉西坦（腹腔注射50和75mg/kg）相当。这些数据证实了这些吡咯烷酮衍生物治疗阵发性肌张力障碍的潜在疗效。
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