Golexanolone
Chemical compound
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Other names | GR-3027; 3α-Ethynyl-3β-hydroxyandrostan-17 E -one oxime |
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Formula | C 21 H 31 N O 2 |
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 GABA A receptor . [1] [2] The medication selectively antagonizes the stimulatory actions of inhibitory neurosteroids like allopregnanolone and tetrahydrodeoxycorticosterone (THDOC) at the GABA A receptor, while not affecting the activation of the GABA A receptor by γ-aminobutyric acid (GABA). [2]
See also
References
- 1 2 "Golexanolone - Umecrine Cognition" . AdisInsight . Springer Nature Switzerland AG.
- 1 2 3 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 .
External links
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