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ABT-239

Catalog No. T14087 CAS 460746-46-7

ABT-239 is a novel, highly efficacious antagonist belonging to the non-imidazole class of histamine H3 receptor (H3R) antagonists. It also acts as a transient receptor potential vanilloid type 1 (TRPV1) antagonist.

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ABT-239, CAS 460746-46-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 40.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 172.00
25 mg	In stock	$ 372.00
50 mg	In stock	$ 556.00
100 mg	In stock	$ 783.00
500 mg	In stock	$ 1,650.00
1 mL * 10 mM (in DMSO)	In stock	$ 97.00

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Purity: 100%

ee: 100%

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Description	ABT-239 is a novel, highly efficacious antagonist belonging to the non-imidazole class of histamine H3 receptor (H3R) antagonists. It also acts as a transient receptor potential vanilloid type 1 (TRPV1) antagonist.
In vitro	Perfusing the tuberomammillary nucleus (TMN) with ABT-239 selectively activates c-Fos in the nucleus basalis of Meynert (NBM) and cortex. Moreover, when the TMN is perfused with ABT-239 at a concentration of 10 μM, there is an increase in histamine release from the TMN, NBM, and cortex; however, this effect is not observed in either the striatum or the nucleus accumbens (NAcc).
In vivo	ABT-239, administered intraperitoneally (i.p.) at a dosage of 3 mg/kg, markedly delays seizure onset, diminishes behavioral seizures triggered by KA, and lowers the occurrence of head bobbing and forelimb clonus in mice. Additionally, at this dosage, ABT-239 enhances memory by converting a short-term learning event into a long-lasting memory in wild type (WT) mice, albeit not in those lacking histamine. The compound is also found to significantly reduce all stages of neuronal damage. In conjunction, ABT-239 and TDZD-8 (10 mg/kg, i.p.) notably decrease the quantity of pyknotic neurons in the hippocampi of mice. When ABT-239 (1 mg/kg, i.p.) is combined with a sub-therapeutic dose of SVP (150 mg/kg, i.p.), there is a marked decrease in behaviors associated with distress such as immobility, head bobbing, and forelimb clonus. A higher dose combination of ABT-239 and TDZD-8 exhibits the most significant enhancement of Bcl-2 expression and reduction in Bax levels, indicating improved neuronal survival. Additionally, combined administration of ABT-239 (at doses of 1 and 3 mg/kg, i.p.) with nicotine enhances nicotine's beneficial effects on memory acquisition and consolidation, with further improvements observed at lower concentrations of ABT-239 (0.1 mg/kg, i.p.) and nicotine.

Molecular Weight	330.42
Formula	C22H22N2O
CAS No.	460746-46-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (272.4 mM)

H2O: insoluble

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Bioactive Compound Library Neuronal Signaling Compound Library Bioactive Compounds Library Max

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Keywords

ABT-239 460746-46-7 Membrane transporter/Ion channel TRP/TRPV Channel ABT 239 ABT239 inhibitor inhibit

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