ABT-239
目录号 : GC35222
ABT-239 是一种新颖的，高效的，非咪唑类的 H3R 拮抗剂，也是 TRPV1 的拮抗剂。
Cas No.:460746-46-7
Sample solution is provided at 25 µL, 10mM.
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ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist.
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[4].
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[1]. 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[2]. 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[3].
[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. Neuropharmacolo [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.
Animal experiment: | Solutions of?KA,?ABT-239 and?SVP are prepared in pyrogen-free normal saline for injection except for TDZD-8, which is dissolved in 10% DMSO and are administered?intraperitoneally in a volume not exceeding 10?mL/kg. The animals are divided into ten groups. The first group (CTRL) receive vehicle (0.9% sodium chloride) only whereas animals in the second group (VEH) are given vehicle followed by KA at a dose of 10mg/kg, i.p. (pH 7.2±1), this being the dose that induces low-grade?seizures?(stage 0-4) in all the animals without any mortality in a range finding study. The KA dose employs to evoke SE in mice in various studies mostly varied from as low as 6-20mg/kg to as high as 25-45mg/kg. Animals in the next two groups are administered ABT-239 in increasing doses of 1 (AL) and 3mg/kg (AH) 30?min before KA challenge. These doses ranging from 0.1 to 3mg/kg of ABT-239 display disease modifying attributes in a mice model of?Alzheimer?s disease as well as improved cognitive functions. The fifth and sixth group receive graduated doses of 150 (SL) and 300mg/kg (SH) of SVP 30?min prior to KA injection. The seventh and eight group receive combinations of subeffective dose (maximum possible dose at which there is no protection) of SVP at 150mg/kg with ABT-239 at 1 (SLAL) and 3mg/kg (SLAH) respectively followed 30?min later by KA. The remaining two groups receive low dose combination at 1 and 5mg/kg (ALTL) and a high dose combination at 3 and 10mg/kg (AHTH) of ABT-239 and TDZD-8, respectively before KA exposure. The doses of TDZD-8 chosen are based on previous studies where doses ranging from 1 to 10mg/kg reduced inflammation and tissue injury as well as improve psychiatric conditions. |
References: [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. | |
| Cas No. | 460746-46-7 | SDF | |
| Canonical SMILES | C[C@H]1N(CCC2=CC3=C(C=CC(C4=CC=C(C#N)C=C4)=C3)O2)CCC1 | ||
| 分子式 | C22H22N2O | 分子量 | 330.42 |
| 溶解度 | DMSO: ≥ 100 mg/mL (302.65 mM); Water: < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0265 mL | 15.1323 mL | 30.2645 mL |
| 5 mM | 0.6053 mL | 3.0265 mL | 6.0529 mL |
| 10 mM | 0.3026 mL | 1.5132 mL | 3.0265 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet