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Encenicline

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Chemical Structure| 550999-75-2 同义名 : EVP-6124
CAS号 : 550999-75-2
货号 : A628540
分子式 : C16H17ClN2OS
纯度 : 99%
分子量 : 320.837
MDL号 : MFCD23381267
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Encenicline (EVP-6124) effectively competes with [3H]-MLA (Methyllycaconitine) and [125I]-α-bungarotoxin for binding, showing Ki values of 9.98 nM and 4.33 nM, respectively. This highlights its roughly 300-fold greater potency than the natural agonist ACh (acetylcholine), which has a Ki of 3 μM in assays involving [3H]-MLA. At a minimal concentration of 10 nM, Encenicline achieves a 51% inhibition of the 5-HT3 receptor. Further, it displaces [3H]-mesulergine from the human 5-HT2B receptor expressed in CHO cells with a Ki of 14 nM and displays only antagonist activity in the rat gastric fundus assay, indicating an IC50 of 16 μM. Notably, Encenicline exhibits a preference for α7 nicotinic acetylcholine receptors (nAChRs) without affecting the heteromeric α4β2 nAChRs in both binding and functional tests[1].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02327182 Alzheimer's Disease Phase 3 Terminated(This study was term... 展开 >>inated due to the benefit-risk balance of MT-4666.) 收起 << - Japan ... 展开 >> Investigational site Osaka, Kansai, Japan 收起 <<
NCT01073228 Alzheimer's Disease ... 展开 >> Central Nervous System Diseases Cognition 收起 << Phase 2 Completed - -
NCT00766363 Alzheimer's Disease ... 展开 >> Central Nervous System Diseases 收起 << Phase 1 Completed - United States, California ... 展开 >> Pacific Research Network, Inc. San Diego, California, United States, 92103 United States, Florida MD Clinical Hallandale Beach, Florida, United States, 33009 United States, New Jersey Comprehensive Clinical Research Berlin, New Jersey, United States, 08009 Global Medical Institutes, LLC Princeton, New Jersey, United States, 08540 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.12mL

0.62mL

0.31mL

15.58mL

3.12mL

1.56mL

31.17mL

6.23mL

3.12mL
参考文献

[1]Prickaerts J, et al. EVP-6124, a novel and selective α7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of α7 nicotinic acetylcholine receptors. Neuropharmacology. 2012 Feb;62(2):109

[2]Thomas Papouin, et al. Septal Cholinergic Neuromodulation Tunes the Astrocyte-Dependent Gating of Hippocampal NMDA Receptors to Wakefulness. Neuron. 2017 May 17;94:1-15.