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 |
---|