917837-54-8|N-(4-Chlorophenyl)-3-((4-chlorophenyl)amino)-2-(3-methylisoxazol-5-yl)acrylamide|CsnPharm

CAS No.: 917837-54-8

CCMI Catalog No. CSN24754

Synonyms: AVL-3288;UCI-4083;N-(4-Chlorophenyl)-3-((4-chlorophenyl)amino)-2-(3-methylisoxazol-5-yl)acrylamide

CCMI is a positive allosteric modulator of α7 nAChRs.

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实验方案

技术信息

生物活性

描述The activation of brain α7 nicotinic acetylcholine receptors (α7 nAChRs) is involved in central nervous system disease related to cognitive dysfunction. CCMI is a positive allosteric modulator of α7 nAChRs. It dose-dependently evoked positive modulation of EC₅ currents induced by acetylcholine, choline, and nicotine with EC₅₀ values of 0.7 ± 0.2 μM, 0.6 ± 0.1 μM, and 0.5 ± 0.1 μM, respectively, and with n_H values of 1.4 ± 0.9, 1.2 ± 0.3, and 1.2 ± 0.3, respectively. CCMI at 1 μM induced a leftward shift in the concentration-response curve for acetylcholine, leading to a 2.7-fold reduction in the EC₅₀ value for acetylcholine compared to the group without CCMI. In oocytes, CCMI evoked positive modulation of submaximal GABA-evoked currents at human GABA_A α1β2γ2L receptors with an EC₅₀ value of 6.3 ± 0.2 μM. It also evoked positive modulation of choline-evoked currents in SH-SY5Y cells transfected with α7 nAChRs (a 1.8-fold increase compared to control). In the DBA/2 mouse model of sensory-gating deficit, intravenous administration of CCMI at the dosages of 0.3 and 1 mg/kg significantly reduced the ratio of test amplitude to conditioning amplitude up to 90 min after administration. In NSA mice, oral administration of CCMI at 0.3 - 3 mg/kg significantly reversed MK-801-induced hyperlocomotion^[1].
动物研究
剂量
Mice: 0.1 mg/kg - 1 mg/kg^[1] (i.p.) Rat: 0.3 mg/kg - 3 mg/kg^[2] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 0.1 mg/kg - 1 mg/kg^[1] (i.p.) Rat: 0.3 mg/kg - 3 mg/kg^[2] (i.p.)
给药途径	i.p.

[1] Ng HJ, Whittemore ER, Tran MB, et al. Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators. Proc Natl Acad Sci U S A.2007;104(19):8059-8064.

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
- 2.5757 mL
- 12.8784 mL
- 25.7568 mL
- 5 mM
- 0.5151 mL
- 2.5757 mL
- 5.1514 mL
- 10 mM
- 0.2576 mL
- 1.2878 mL
- 2.5757 mL

技术信息

CAS号

917837-54-8

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H15Cl2N3O2

运输

蓝冰

分子量

388.25

别名

AVL-3288;UCI-4083;N-(4-Chlorophenyl)-3-((4-chlorophenyl)amino)-2-(3-methylisoxazol-5-yl)acrylamide;XY-4083;Anvylic-3288

溶解度

DMSO	57.5 mg/mL (148.1 mM)
Water	insoluble

动物实验配方

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