ABT-239

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性组胺 H3 受体拮抗剂，Ki 为 0.1-5.8 nM（人、大鼠 H3）。

A potent and selective Histamine H3 receptor antagonist with Ki of 0.1-5.8 nM (human, rat H3); exhibits 1000-fold selectivity versus H1, H2 and H4; excellent pharmacokinetic and metabolic properties across species and good oral bioavailability.Pain Discontinued.

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.

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. 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. 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.

ABT239 | ABT 239

GPCR/G Protein

Histamine Receptor

Histamine Receptor

Neurological Disease

Pain

460746-46-7

330.4229

C22H22N2O

>98% (HPLC)

DMSO: ≥ 3.3 mg/mL

N#CC1=CC=C(C2=CC=C(OC(CCN3[C@H](C)CCC3)=C4)C4=C2)C=C1

Benzonitrile, 4-[2-[2-[(2R)-2-methyl-1-pyrrolidinyl]ethyl]-5-benzofuranyl]-

(-20℃)

With Ice Pack

≥ 2 years