货号	规格	价格	上海	北京	珠海	重庆	武汉
S85456-5mg促销	≥98%	￥900.00 ￥710.00 S85456-5mg ￥710.00 现货	7 7	-	-	-	-
S85456-10mg促销	≥98%	￥1700.00 ￥1350.00 S85456-10mg ￥1350.00 现货	6 6	-	-	-	-
S85456-25mg促销	≥98%	￥3600.00 ￥2870.00 S85456-25mg ￥2870.00 现货	4 4	-	-	-	-
S85456-50mg促销	≥98%	￥5300.00 ￥4230.00 S85456-50mg ￥4230.00 现货	2 2	-	-	-	-

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产品描述：

ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist.

靶点：

H3 receptor;TRP/TRPVChannel

体外研究：

Perfusion of the TMN with ABT-239 (10 μM) increases histamine release from the TMN, NBM, and cortex, but not from the striatum or NAcc. TMN perfusion with ABT-239 activates c-Fos selectively in the NBM and cortex

体内研究：

ABT-239 (3 mg/kg, i.p.) significantly delays onset of seizure, reduces behavioral seizures elicited by KA, and reduces in the incidence of head bobbing and forelimb clonus in mice. ABT-239 (1 mg/kg, i.p.) in conbination with sub-therapeutic dose of SVP (150 mg/kg, i.p.), significantly decreases the number of immobility, head bobbing and forelimb clonus, where as a higher dose combination of ABT-239 (3 mg/kg, i.p.) causes enhanced reduction in all the stages. ABT-239 (3 mg/kg, i.p.) and TDZD-8 (10 mg/kg, i.p.) have more powerful reduction in the number of pyknotic neurons in mice hippocampi. The high dose combination of ABT-239 and TDZD-8 produces the most pronounced increase in Bcl-2 expression as well as decrease in the level of Bax. ABT-239 (3 mg/kg, i.p.) administration transforms a short-term learning event into a long-term remembered experience in WT but not in histamine-depleted mice. Concomitant administration of either ABT-239 (1 and 3 mg/kg, i.p.) and nicotine (0.035 mg/kg, i.p.), or ABT-239 (0.1 mg/kg, i.p.) and nicotine (0.0175 mg/kg, i.p.) further increases nicotine-induced improvement in both memory acquisition and consolidation

参考文献：

1. Bhowmik M, et al. Histamine H3 receptor antagonism by ABT-239 attenuates kainic acid induced excitotoxicity in mice. Brain Res. 2014 Sep 18;1581:129-40. 2. Provensi G, et al. Donepezil, an acetylcholine esterase inhibitor, and ABT-239, a histamine H3 receptor antagonist/inverse agonist, require the integrity of brain histamine system to exert biochemical and procognitive effects in the mouse. Neuropharmacology. 2016 Oct;109:139-147. 3. Kruk M, e tal. Effects of the histamine H2 receptor antagonist ABT-239 on cognition and nicotine-induced memory enhancement in mice. Pharmacol Rep. 2012;64(6):1316-25. 4. Munari L, et al. Selective brain region activation by histamine H2 receptor antagonist/inverse agonist ABT-239 enhances acetylcholine and histamine release and increases c-Fos expression. Neuropharmacology. 2013 Jul;70:131-40.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.026 ml	15.132 ml	30.264 ml
5 mM	0.605 ml	3.026 ml	6.053 ml
10 mM	0.303 ml	1.513 ml	3.026 ml
50 mM	0.061 ml	0.303 ml	0.605 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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