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DMCM HCl {[allProObj[0].p_purity_real_show]}

货号:A224725 同义名: DMCM hydrochloride

DMCM HCl is benzodiazepine inverse agonist that displays anxiogenic and potent convulsant activity.

DMCM HCl 化学结构 CAS号:1215833-62-7
DMCM HCl 化学结构
CAS号:1215833-62-7
DMCM HCl 3D分子结构
CAS号:1215833-62-7
DMCM HCl 化学结构 CAS号:1215833-62-7
DMCM HCl 3D分子结构 CAS号:1215833-62-7
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DMCM HCl 纯度/质量文件 产品仅供科研

货号:A224725 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 GABA receptor GABAA receptor 其他靶点 纯度
Niflumic Acid 98%
Ginkgolide A ++

GABA receptor, Ki: 14.5 μM

98%
Valproic acid sodium Autophagy,HDAC 97%
Flumazenil 95%
Bemegride 98%
Bicuculline +++

GABAA receptor, IC50: 2 μM

99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

DMCM HCl 生物活性

描述 DMCM HCl is a nonselective full inverse agonist of benzodiazepine. DMCM shows binding affinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5  receptors, respectively[3]. DMCM most probably induces the seizures by selective impairment of the functions mediated by the GABA/BZ receptor-chloride channel complex (inverse agonism) and therefore differs from GABA receptor blockers[4]. Dunnett's analysis showed that DMCM significantly decreased immobility time at the dose of 0.1mg/kg, exerted acute antidepressant-like effects[5]. DMCM has potent convulsant, proconvulsant and anxiogenic properties in vivo. In vivo DMCM (20-60 mg/kg i.p.) produced modest anxiolytic-like effects in gamma2I77 mice as assessed by elevated plus maze and staircase tests, but no motor impairment was found in the rotarod test[6]. DMCM inhibits both a spinal nociceptive reflex (tail-flick to heat) and a supraspinal measure of pain (vocalization to shock). DMCM induces hypoalgesia on a wide range of assays[7].

DMCM HCl 参考文献

[1]Conto MB, de Carvalho JG, et al. Behavioral differences between subgroups of rats with high and low threshold to clonic convulsions induced by DMCM, a benzodiazepine inverse agonist. Pharmacol Biochem Behav. 2005 Nov;82(3):417-26.

[2]Petersen EN. DMCM: a potent convulsive benzodiazepine receptor ligand. Eur J Pharmacol. 1983 Oct 14;94(1-2):117-24.

[3]Chambers MS, Atack JR, Carling RW, Collinson N, Cook SM, Dawson GR, Ferris P, Hobbs SC, O'connor D, Marshall G, Rycroft W, Macleod AM. An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. J Med Chem. 2004 Nov 18;47(24):5829-32

[4]Petersen EN. DMCM: a potent convulsive benzodiazepine receptor ligand. Eur J Pharmacol. 1983 Oct 14;94(1-2):117-24

[5]Samardžić J, Strac DŠ, Obradović M, Oprić D, Obradović DI. DMCM, a benzodiazepine site inverse agonist, improves active avoidance and motivation in the rat. Behav Brain Res. 2012 Dec 1;235(2):195-9

[6]Leppä E, Vekovischeva OY, Lindén AM, Wulff P, Oberto A, Wisden W, Korpi ER. Agonistic effects of the beta-carboline DMCM revealed in GABA(A) receptor gamma 2 subunit F77I point-mutated mice. Neuropharmacology. 2005 Mar;48(4):469-78

[7]Sieve AN, King TE, Ferguson AR, Grau JW, Meagher MW. Pain and negative affect: evidence the inverse benzodiazepine agonist DMCM inhibits pain and learning in rats. Psychopharmacology (Berl). 2001 Jan 1;153(2):180-90

DMCM HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.85mL

0.57mL

0.29mL

14.25mL

2.85mL

1.43mL

28.51mL

5.70mL

2.85mL

DMCM HCl 技术信息

CAS号1215833-62-7
分子式C17H19ClN2O4
分子量 350.8
SMILES Code O=C(C1=C(CC)C2=C(C=N1)NC3=C2C=C(OC)C(OC)=C3)OC.[H]Cl
MDL No. MFCD10687107
别名 DMCM hydrochloride
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

DMSO: 9 mg/mL(25.66 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 25 mg/mL(71.27 mM),配合低频超声助溶

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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