生物活性 | |||
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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 | |||
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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 |
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