| Description | Ensaculin (Anseculin), a novel benzopyrone partially substituted with piperazine, showed memory-enhancing effects in passive and conditioned avoidance paradigms in normal and artificially amnesic rodents. It showed neuroprotective activity in a model of NMDA toxicity and neurotrophic effects in primary cultured rat brain cells.Ensaculin can be used for the treatment of dementia. |
| In vivo | Ensaculin (0.1、1及10 mg/kg；i.p.；Wistar大鼠；谷氨酸灌注开始20分钟后)显著抑制了2,3-DHBA的形成，将其水平分别降至对照水平的60.5%和56.7%。Ensaculin可能对于治疗与高水平羟基自由基和兴奋毒性相关的神经退行性疾病有用。[1] |
| Target activity | 5-HT2:＞100 nM, 5-HT1A:8 nM, α:＞100 nM, α1B:9.3 nM, α1A:4.7 nM, D4:277 nM, D3:27.7 nM, D2:16.6 nM |
| Synonyms | Anseculin |
| molecular weight | 452.54 |
| Molecular formula | C26H32N2O5 |
| CAS | 155773-59-4 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 42.6 mg/mL (94.03 mM ), Sonication is recommended. |
| References | 1. Teismann P, et al. Comparison of the novel drug Ensaculin with MK-801 on the reduction of hydroxyl radical production in rat striatum after local application of glutamate. Brain Res. 2000;857(1-2):165-17 2. Teismann P, et al. Effects of ensaculin on dopamine metabolite levels and K(+)-induced glutamate release. Eur J Pharmacol. 2000;398(2):247-250. 3. Hoerr R, et al. Ensaculin (KA-672 HCl): a multitransmitter approach to dementia treatment. CNS Drug Rev. 2002;8(2):143-158. |