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Chemical Structure : KRM-II-81
Catalog No.: PC-35483Not For Human Use, Lab Use Only.
KRM-II-81 is a selective α2/α3 subtype GABAA receptor ligand (positive allosteric modulator) with EC50 of 937 nM for α3β3γ2 GABAAR.
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KRM-II-81 is a selective α2/α3 subtype GABAA receptor ligand (positive allosteric modulator) with EC50 of 937 nM for α3β3γ2 GABAAR.
KRM-II-81 demonstrated similar efficacy at α1/α2/α3 GABAA receptors and negligible efficacy at α4/α5/α6 GABAA receptors, with α2 and α3-subtypes being 17- and 28-fold more potent than α1 subtypes in HEK-293T cells expressing GABAA receptors with different α subunits.
KRM-II-81 exhibited improved anxiolytic-like effects in a mouse marble burying assay and a rat Vogel conflict test.
KRM-II-81 dose-dependently decreased 0.6% acetic acid- and 0.32% lactic acid-induced writhing.
KRM-II-81 exhibited significant antinociceptive effects in chemical stimulation-induced pain in mice.
| M.Wt | 351.369 | |
| Formula | C21H13N5O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Poe MM, et al. J Med Chem. 2016 Dec 8;59(23):10800-10806.
2. Lewter LA, et al. ACS Chem Neurosci. 2017 Jun 21;8(6):1305-1312.
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