ABT-239

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Chemical Structure| 460746-46-7 同义名 : -
CAS号 : 460746-46-7
货号 : A663348
分子式 : C22H22N2O
纯度 : 95%
分子量 : 330.42
MDL号 : MFCD13248643
存储条件:

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(317.77 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Histaminergic H3 receptors (H3R) antagonists enhance cognition in preclinical models and modulate neurotransmission, in particular acetylcholine (ACh) release in the cortex and hippocampus, two brain areas involved in memory processing. ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist[3]. ABT-239 (10 μM) increased histamine release from the TMN (tuberomamillary nucleus), NBM (nucleus basalis magnocellularis), and cortex[4]. ABT-239 (3 mg/kg, i.p.) ameliorated the cognitive performance in the ORT (object recognition test). ABT-239 systemic treatments increased GSK-3β phosphorylation in cortical and hippocampal homogenates of normal mice[3]. ABT-239 (1 and 3 mg/kg; i.p.) significantly attenuated KA (Kainic acid)-mediated behavioural and excitotoxic anomalies and restored altered expression of Bax, cleaved caspase-3, phospho-Akt (Ser473) and cAMP response element binding protein (CREB)[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.03mL

0.61mL

0.30mL

15.13mL

3.03mL

1.51mL

30.26mL

6.05mL

3.03mL

参考文献

[1]Provensi G, Costa A, 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.

[2]Bhowmik M, Saini N, et al. Histamine H3 receptor antagonism by ABT-239 attenuates kainic acid induced excitotoxicity in mice. Brain Res. 2014 Sep 18;1581:129-40.

[3]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.

[4]Munari L, et al. Selective brain region activation by histamine H₃ receptor antagonist/inverse agonist ABT-239 enhances acetylcholine and histamine release and increases c-Fos expression. Neuropharmacology. 2013 Jul;70:131-40。

[5]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.