新型二苯哌嗪类化合物的合成及 T 型钙通道阻断活性，以及体内镇痛活性评价。
Synthesis and T-type calcium channel blocking activity of novel diphenylpiperazine compounds, and evaluation of in vivo analgesic activity.
机构信息
School of Pharmacy, Ewha Womans University, Seoul 120-750, Republic of Korea.
出版信息
Bioorg Med Chem. 2010 Aug 15;18(16):5938-44. doi: 10.1016/j.bmc.2010.06.082. Epub 2010 Jun 30.
PMID:20659804
Abstract
Novel diphenylpiperazine derivatives were synthesized and evaluated for their inhibitory activity against T-type calcium channel by whole-cell patch clamp recordings on HEK293 cells. Among the test compounds, 2 and 3d were effective in decreasing the response to formalin in both the first and second phases and demonstrated antiallodynic effects in a rat model of neuropathic pain.
摘要
新型二苯哌嗪衍生物被合成，并通过全细胞膜片钳记录在 HEK293 细胞上评估其对 T 型钙通道的抑制活性。在测试的化合物中，2 和 3d 有效地减少了福尔马林在第一和第二阶段的反应，并在神经病理性疼痛的大鼠模型中显示出抗痛觉过敏作用。
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