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Chemical Structure : GR3027
Catalog No.: PC-35454Not For Human Use, Lab Use Only.
GR3027 (Golexanolone) is a GABA-A receptor modulating steroid antagonist that selectively antagonizes the enhanced activation of GABAA receptors by neurosteroids such as allopregnanolone and THDOC.
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GR3027 (Golexanolone) is a GABA-A receptor modulating steroid antagonist that selectively antagonizes the enhanced activation of GABAA receptors by neurosteroids such as allopregnanolone and THDOC; inhibits α1β2γ2L receptor 29 ± 5% of THDOC enhancement of the GABA response, does not antagonize the effect of GABA at the GABAA receptor; during the specific conditions used for the different receptors, IC50=250 nM for the α1β2γ2L GABAA receptor and 350 nM for the α5β3γ2L GABAA receptor; restores spatial learning and motor coordination in rats with chronic hyperammonemia and hepatic encephalopathy.
Sleep Disorder
Phase 2 Clinical
| M.Wt | ||
| Formula | C21H31NO2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Johansson M, et al. Am J Physiol Gastrointest Liver Physiol. 2015 Sep 1;309(5):G400-9.
2. Johansson M, et al. J Steroid Biochem Mol Biol. 2016 Jun;160:98-105.
3. Johansson M, et al. Psychopharmacology (Berl). 2018 May;235(5):1533-1543.
4. Patent WO 2008/063128.
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