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Cipralisant  

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包装规格：5mg 25mg in glass bottle
产品简介：一种有效的，选择性的组胺 H3 受体 (histamine H3 receptor) 调节剂，在体外，为组胺 H3 受体的激动剂，在体内为拮抗剂，pKi 值为 9.9，对大鼠组胺 H3 受体的 Ki 值为 0.47nM；Cipralisant 有潜力用于注意力不集中的过度反应症的研究。
溶解性：DMSO ：200 mg/mL(924.56 mM;超声助溶)
储备液保存：-80°C, 6 months -20°C, 1 month
靶点：H3 receptor:9.9 (pKi);rat H3 receptor:0.47 nM (Ki)
体外研究：Cipralisant behaves as a full agonist on adenylyl cyclase inhibition. Cipralisant (HEK cells) potently inhibits forskolin-induced cAMP accumulation, showing that Cipralisant works as a potent full histamine H3 receptor agonist. Cipralisant increases the basal [35S]GTPγS binding activities in membranes from HEK cells expressing the rat histamine H3 receptor (EC50, 5.6 nM).
体内研究：Cipralisant (0.3~30 mg/kg; s.c.) enhances acquisition over five trials, reaching significance at 1 mg/kg. Cipralisant (10 mg/kg; p.o.) completely blocks R-α-methylhistamine-induced drinking. Cipralisant promotes wakefulness in the rat. Cipralisant potently and significantly improves performance in the repeated acquisition model, in line with its high affinity for the rat H3 receptor and good CNS penetration. Cipralisant does not appear to be as efficacious as 3 mg/kg ciproxifan at its maximally effective dose . Cipralisant behaves as a partial agonist in a rat brain synaptosome model.
保存条件：-20℃
注意事项：1、为了您的安全和健康，请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。

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