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西尼地平,一种 L/N 型钙通道阻滞剂,可预防小鼠获得和表达乙醇诱导的运动敏化。

Cilnidipine, an L/N-type calcium channel blocker prevents acquisition and expression of ethanol-induced locomotor sensitization in mice.

机构信息

Sinhgad College of Pharmacy, Post-Graduate Research Department, Off Sinhgad Road, Vadgaon (Bk), Pune 411 0 41, Maharashtra, India.

出版信息

Neurosci Lett. 2012 Apr 11;514(1):91-5. doi: 10.1016/j.neulet.2012.02.064. Epub 2012 Mar 3.

DOI:10.1016/j.neulet.2012.02.064
PMID:22402189
Abstract

Several evidences indicated the involvement of L- and N-type calcium channels in behavioral effects of drugs of abuse, including ethanol. Calcium channels are implicated in ethanol-induced behaviors and neurochemical responses. Calcium channel antagonists block the psychostimulants induced behavioral sensitization. Recently, it is demonstrated that L-, N- and T-type calcium channel blockers attenuate the acute locomotor stimulant effects of ethanol. However, no evidence indicated the role of calcium channels in ethanol-induced psychomotor sensitization. Therefore, present study evaluated the influence of cilnidipine, an L/N-type calcium channel blocker on acquisition and expression of ethanol-induced locomotor sensitization. The results revealed that cilnidipine (0.1 and 1.0μg/mouse, i.c.v.) attenuates the expression of sensitization to locomotor stimulant effect of ethanol (2.0g/kg, i.p.), whereas pre- treatment of cilnidipine (0.1 and 1.0μg/mouse, i.c.v.) during development of sensitization blocks acquisition and attenuates expression of sensitization to locomotor stimulant effect of ethanol. Cilnidipine per se did not influence locomotor activity in tested doses. Further, cilnidipine had no influence on effect of ethanol on rotarod performance. These results support the hypothesis that neuroadaptive changes in calcium channels participate in the acquisition and the expression of ethanol-induced locomotor sensitization.

摘要

有几项证据表明 L 型和 N 型钙通道参与了包括乙醇在内的成瘾药物的行为效应。钙通道与乙醇诱导的行为和神经化学反应有关。钙通道拮抗剂可阻断精神兴奋剂引起的行为敏化。最近的研究表明,L 型、N 型和 T 型钙通道阻滞剂可减弱乙醇引起的急性运动兴奋作用。然而,目前尚无证据表明钙通道在乙醇诱导的运动敏化中的作用。因此,本研究评估了 L/N 型钙通道阻滞剂西尼地平对乙醇诱导的运动敏化的获得和表达的影响。结果表明,西尼地平(0.1 和 1.0μg/只,侧脑室注射)可减弱乙醇(2.0g/kg,腹腔注射)对运动兴奋作用的敏化表达,而在敏化的发展过程中,西尼地平(0.1 和 1.0μg/只,侧脑室注射)预处理可阻断敏化的获得,并减弱乙醇对运动兴奋作用的敏化表达。在测试剂量下,西尼地平本身不会影响运动活性。此外,西尼地平对乙醇对旋转棒性能的影响没有影响。这些结果支持了这样一种假设,即钙通道的神经适应性变化参与了乙醇诱导的运动敏化的获得和表达。

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The role of L-type calcium channels in the development and expression of behavioral sensitization to ethanol.L 型钙通道在乙醇行为敏化发展和表达中的作用。
Neurosci Lett. 2013 Oct 11;553:196-200. doi: 10.1016/j.neulet.2013.08.008. Epub 2013 Aug 28.