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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[1]. | [in vivo]
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[2]. | Animal Model: | Male γ2I77 mice[2] | | Dosage: | 20 mg/kg and 60 mg/kg | | Administration: | Injected i.p. | | Result: | Produced modest anxiolytic-like effects. |
| [storage]
Desiccate at RT | [References]
[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. DOI:10.1021/jm040863t
[2] Lepp? 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. DOI:10.1016/j.neuropharm.2004.11.007 |
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