Golexanolone (Golexanolona) is a novel GABA-A receptor-modulating steroid antagonist that reduces peripheral inflammation and neuroinflammation and improves cognitive and motor function in rats with chronic hyperammonemia, and may be used to study hepatic encephalopathy.

In the absence of agonist (i.e., GABA, 0), the THDOC-mediated outward current excursion was significantly reduced when Golexanolone(GR3027) concentration was incrementally increased (0.03-3 µM, Fig. 2A), with an IC50 = 344 nM and Imax -33%. In addition, analysis of the AUC and peak current amplitude of the GABA-mediated response showed a concentration-dependent decrease in both parameters (IC50 = 341 nM, Imax -35% for AUC; IC50 = 563 nM, Imax -37% for peak current amplitude; n = 4-14, 95% confidence intervals;) The data suggest that the effects of Golexanolone(GR3027) on the THDOC-mediated α5β3γ2L GABAA channel activation.[2]

In a toxicity study using doses of 50 and 100 mg/kg/day to evaluate oral administration of Golexanolone(GR3027) in rats, no toxicity was observed at 100 mg/kg/day.[1]