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CAS No.: 550999-74-1

Encenicline HCl Catalog No. CSN16494

Synonyms: EVP-6124 hydrochloride;Encenicline HCl;EVP-6124 (hydrochloride)

EVP-6124 HCl is a partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).

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描述EVP-6124 HCl is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs). In binding and functional experiments, EVP-6124 showed selectivity for α7 nAChRs and did not activate or inhibit heteromeric α4β2 nAChRs. EVP-6124 had good brain penetration and an adequate exposure time. EVP-6124 (0.3 mg/kg, p.o.) significantly restored memory function in scopolamine-treated rats (0.1 mg/kg, i.p.) in an object recognition task (ORT). In co-application experiments of EVP-6124 with acetylcholine, sustained exposure to EVP-6124 in functional investigations in oocytes caused desensitization at concentrations greater than 3 nM, while lower concentrations (0.3 - 1 nM) caused an increase in the acetylcholine-evoked response^[3]. Effective dose combinations were donepezil/EVP-6124(5/2 mg) and donepezil/EVP-6124 (5/0.3 mg) and showed improvements of the delayed recall of the Visual Verbal Learning Test (1.2; CI = 0.1 - 2.3) and reaction time during the two-back condition of the N-back (-42; CI = -77, -8), respectively^[4]. Treatment with EVP-6124 in Phase I and II trials involving patients with mild-to-moderate AD was well tolerated and showed statistically significant improvements compared with placebo on cognitive and functional measures^[5].
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
NCT02246075	Alzheimer's Disease ... more >> Dementia Cognition Collapse <<	Phase 2	Withdrawn(Forum has decided no... more >>t to proceed with this study at this time.) Collapse <<	-	United States, Florida ... more >> Delray Beach, Florida, United States United States, New Mexico Albuquerque, New Mexico, United States Collapse <<
NCT02246075	Alzheimer's Disease ... more >> Dementia Cognition Collapse <<	Phase 2	Withdrawn(Forum has decided no... more >>t to proceed with this study at this time.) Collapse <<	-	United States, Florida ... more >> Delray Beach, Florida, United States United States, New Mexico Albuquerque, New Mexico, United States Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7988 mL
- 13.9939 mL
- 27.9878 mL
- 5 mM
- 0.5598 mL
- 2.7988 mL
- 5.5976 mL
- 10 mM
- 0.2799 mL
- 1.3994 mL
- 2.7988 mL

技术信息

CAS号

550999-74-1

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H18Cl2N2OS

运输

蓝冰

分子量

357.30

别名

EVP-6124 hydrochloride;Encenicline HCl;EVP-6124 (hydrochloride);EVP-6124;MT-4666

溶解度

DMSO	350.0 mg/mL (979.6 mM)
Water	insoluble

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