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Other names | GR-3027; 3α-Ethynyl-3β-hydroxyandrostan-17E-one oxime |
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Formula | C21H31NO2 |
Molar mass | 329.484 g·mol−1 |
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Golexanolone, also known by the developmental code name GR-3027, is a neurosteroid medication which is under development for the treatment of hypersomnia and hepatic encephalopathy.[1][2][3][4] It acts as a negative allosteric modulator of the GABAA receptor.[1][2] The medication selectively antagonizes the stimulatory actions of inhibitory neurosteroids like allopregnanolone and tetrahydrodeoxycorticosterone (THDOC) at the GABAA receptor, while not affecting the activation of the GABAA receptor by γ-aminobutyric acid (GABA).[2]
See also
[edit]References
[edit]- ^ a b "Golexanolone - Umecrine Cognition". AdisInsight. Springer Nature Switzerland AG.
- ^ a b c Agusti A, Llansola M, Hernández-Rabaza V, Cabrera-Pastor A, Montoliu C, Felipo V (June 2016). "Modulation of GABAA receptors by neurosteroids. A new concept to improve cognitive and motor alterations in hepatic encephalopathy". The Journal of Steroid Biochemistry and Molecular Biology. 160: 88–93. doi:10.1016/j.jsbmb.2015.08.020. PMID 26307490. S2CID 42040436.
- ^ Johansson M, Månsson M, Lins LE, Scharschmidt B, Doverskog M, Bäckström T (May 2018). "GR3027 reversal of neurosteroid-induced, GABA-A receptor-mediated inhibition of human brain function: an allopregnanolone challenge study". Psychopharmacology. 235 (5): 1533–1543. doi:10.1007/s00213-018-4864-1. PMC 5919995. PMID 29492615.
- ^ Johansson M, Agusti A, Llansola M, Montoliu C, Strömberg J, Malinina E, et al. (September 2015). "GR3027 antagonizes GABAA receptor-potentiating neurosteroids and restores spatial learning and motor coordination in rats with chronic hyperammonemia and hepatic encephalopathy". American Journal of Physiology. Gastrointestinal and Liver Physiology. 309 (5): G400-9. doi:10.1152/ajpgi.00073.2015. PMC 4556948. PMID 26138462.