| Name | ABT-239 |
| Description | ABT-239 is a novel, highly efficacious non-imidazole class histamine H3 receptor (H3R) antagonist and 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 90 mg/mL (272.38 mM), Sonication is recommended.
H2O : insoluble
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (9.99 mM), Sonication is recommended.
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| Keywords | TRPVChannel | TRPV1 | TRPV Channel | TRPChannel | TRP Channel | ABT-239 | ABT239 | ABT 239 |
| Inhibitors Related | Undecane | Rosiglitazone | Caffeic Acid | Meclizine dihydrochloride | Famotidine | Probenecid | 1,4-Cineole | Sodium butanoate | trans-Cinnamaldehyde | Alginic acid | Mianserin hydrochloride | Trazodone hydrochloride |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Ion Channel Targeted Library |
United States
