产品描述: | DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity 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 |
靶点: |
Ki: 10 nM (GABAA α1 receptor), 13 nM (GABAA α2 receptor), 7.5 nM (GABAA α3 receptor), 2.2 nM (GABAA α5 receptor);GABAReceptor |
体内研究: |
DMCM has potent convulsant, proconvulsant and anxiogenic properties in vivo. DMCM (20-60 mg/kg; i.p.) produces modest anxiolytic-like effects in γ2I77 mice. Animal Model: Male γ2I77 mice Dosage: 20 mg/kg and 60 mg/kg Administration: Injected i.p. Result: Produced modest anxiolytic-like effects. |
参考文献: |
1. Chambers MS, et al. 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. 2. Leppä E, et al. 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. |
溶解性: |
Soluble in DMSO、H2O |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.851 ml |
14.253 ml |
28.507 ml |
5 mM |
0.57 ml |
2.851 ml |
5.701 ml |
10 mM |
0.285 ml |
1.425 ml |
2.851 ml |
50 mM |
0.057 ml |
0.285 ml |
0.57 ml |
|
注意: |
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