首页> 中文期刊> 《国际药学研究杂志》 >囊泡谷氨酸转运体抑制剂芝加哥天蓝6B的镇痛作用

囊泡谷氨酸转运体抑制剂芝加哥天蓝6B的镇痛作用

         

摘要

目的:研究抑制囊泡谷氨酸转运体(vesicular glutamate transporters,VGLUT)功能对动物疼痛行为的影响。方法分别观察选择性VGLUT抑制剂芝加哥天蓝6B(Chicago sky blue 6B,CSB6B)对小鼠热板潜伏期、醋酸扭体次数和福尔马林所致舔足时间的影响。结果腹腔注射CSB6B不影响小鼠热板潜伏期。小鼠醋酸扭体实验中,与溶剂对照组相比,CSB6B 2.5mg/kg腹腔注射30 min后可使小鼠扭体次数从26.50±2.97显著下降到8.22±1.90(P<0.01),腹腔注射60 min后可使小鼠扭体次数显著下降到9.60±1.84(P<0.01)。在福尔马林实验中,与溶剂对照组相比,CSB6B不影响小鼠的Ⅰ相舔足时间, CSB6B 0.5 mg/kg腹腔注射30 min后可使小鼠的Ⅱ相舔足时间从(139.40±21.02)s显著下降到(75.10±19.45)s(P<0.05),而注射2 h后对小鼠舔足时间没有显著影响。结论抑制VGLUT功能可显著抑制炎性疼痛,提示VGLUT参与了炎性疼痛的调控,可能成为疼痛治疗的新靶点。%Objective To investigate the effects of inhibiting vesicular glutamate transporters (VGLUT) on pain behaviors in animals. Methods The latency in hot plate test, number of writhes in acetic acid and licking time in formeldehyde solution (formalin) tests were recorded to determine the analgesic effect of Chicago sky blue 6B (CSB6B), a selective VGLUT inhibitor. Results Intraperitoneal administration of CSB6B did not affect the acute thermal pain responses in hot plate test. In acetic acid writhing, compared with control group (26.50 ±2.97), CSB6B (2.5 mg/kg, ip) significantly attenuated the acetic acid-induced writhing (8.22±1.90) 30 min after administration (P<0.01);CSB6B (2.5 mg/kg, ip) significantly reduced the acetic acid-induced writhing(9.60±1.84) 60 min after administration(P<0.01). In Formalin test, compared with control group(139.40±21.02), CSB6B (0.5 mg/kg, ip) significantly reduced the licking time(75.10±19.45) 30 min after administration(P<0.05) during the second phase, but not during the first phases. CSB6B(ip) did not affect the licking time 2 h after administration during the first and second phases. Conclusion Inhibition of VGLUTs activity is sufficient to attenuate the inflammatory pain and this finding suggests that VGLUT participate in regulation of inflammatory pain and be a novel therapeutic strategy for treatment of pain.

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