ABT-239

H₃ receptor

用 ABT-239 (10 μM) 灌注 TMN 会增加 TMN、NBM 和皮质的组胺释放，但不会增加纹状体或 NAcc 的组胺释放。 TMN 灌注 ABT-239 可选择性激活 NBM 和皮质中的 c-Fos[4]。

ABT-239（3 mg/kg，腹腔注射）可显着延迟小鼠癫痫发作，减少 KA 引起的行为性癫痫发作，并减少小鼠头部摆动和前肢阵挛的发生率。 ABT-239（1 mg/kg，腹腔注射）与亚治疗剂量的 SVP（150 mg/kg，腹腔注射）联合使用，可显着减少不动、头部摆动和前肢阵挛的次数，而较高剂量的 ABT 组合-239（3 mg/kg，腹腔注射）导致所有阶段的还原增强。 ABT-239 (3 mg/kg, ip) 和 TDZD-8 (10 mg/kg, ip) 对小鼠海马中固缩神经元的数量有更强大的减少作用。 ABT-239 和 TDZD-8 的高剂量组合可显着增加 Bcl-2 表达以及降低 Bax 水平[1]。在 WT 中，ABT-239（3 mg/kg，腹腔注射）给药可将短期学习事件转化为长期记忆的经历，但在组胺耗尽的小鼠中则不然[2]。同时给予 ABT-239（1 和 3 mg/kg，腹腔注射）和尼古丁（0.035 mg/kg，腹腔注射），或 ABT-239（0.1 mg/kg，腹腔注射）和尼古丁（0.0175 mg/kg，腹腔注射）进一步增强尼古丁诱导的记忆获取和巩固的改善[3]。

ABT-239, SVP, and KA solutions are made in pyrogen-free normal saline for injection; TDZD-8, on the other hand, is dissolved in 10% DMSO and injected intraperitoneally in a volume not to exceed 10 mL/kg. There are ten groupings of animals. In a range finding study, animals in the second group (VEH) receive KA at a dose of 10 mg/kg, i.p. (pH 7.2±1), while the first group (CTRL) receives only vehicle (0.9% sodium chloride). This dose causes low-grade seizures (stages 0-4) in all animals without causing any mortality. In most studies, the KA dose used to elicit SE in mice ranged from 6–20 mg/kg to 25–45 mg/kg and higher. Two groups of animals receive increasing doses of ABT-239 (30 min before KA challenge): 1 mg/kg (AL) and 3 mg/kg (AH). In mice with Alzheimer's disease, these doses of ABT-239, which range from 0.1 to 3 mg/kg, show improved cognitive functions as well as disease-modifying properties. Prior to the KA injection, 30 minutes are spent giving the fifth and sixth groups graduated doses of SVP at 150 (SL) and 300 mg/kg (SH). The subeffective dose (the highest dose at which no protection is possible) of SVP at 150 mg/kg combined with ABT-239 at 1 (SLAL) and 3 mg/kg (SLAH), respectively, is given to the seventh and eighth groups. Thirty minutes later, KA administers the combination. Before being exposed to KA, the remaining two groups receive low doses of ABT-239 and TDZD-8, respectively, at 1 and 5 mg/kg (ALTL) and high doses, at 3 and 10 mg/kg (AHTH). The TDZD-8 dosages selected are based on earlier research in which doses between 1 and 10 mg/kg improved psychiatric conditions and decreased inflammation and tissue damage.

[1]. Histamine H3 receptor antagonism by ABT-239 attenuates kainic acid induced excitotoxicity in mice. Brain Res. 2014 Sep 18;1581:129-40.

[2]. 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]. 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]. 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.

C22H22N2O

330.42288

330.17

C, 79.97; H, 6.71; N, 8.48; O, 4.84

460746-46-7

Solid powder

C[C@@H]1CCCN1CCC2=CC3=C(O2)C=CC(=C3)C4=CC=C(C=C4)C#N

KFHYZKCRXNRKRC-MRXNPFEDSA-N

InChI=1S/C22H22N2O/c1-16-3-2-11-24(16)12-10-21-14-20-13-19(8-9-22(20)25-21)18-6-4-17(15-23)5-7-18/h4-9,13-14,16H,2-3,10-12H2,1H3/t16-/m1/s1

4-[2-[2-[(2R)-2-methylpyrrolidin-1-yl]ethyl]-1-benzofuran-5-yl]benzonitrile

ABT-239; ABT 239; ABT239

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO: ≥ 100 mg/mL (~302.7 mM)
H2O: < 0.1 mg/mL

Solubility in Formulation 1: ≥ 2.5 mg/mL (7.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: 2.5 mg/mL (7.57 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (7.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。