DMCM HCl

产品说明书

Print
Chemical Structure| 1215833-62-7 同义名 : DMCM hydrochloride
CAS号 : 1215833-62-7
货号 : A224725
分子式 : C17H19ClN2O4
纯度 : 98%
分子量 : 350.8
MDL号 : MFCD10687107
存储条件:

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

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

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].
实验方案
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

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