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Clinical data
Other namesGR-3027; 3α-Ethynyl-3β-hydroxyandrostan-17E-one oxime
CAS Number
PubChem CID
Chemical and physical data
Molar mass329.484 g·mol−1
3D model (JSmol)

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]

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  1. ^ a b https://adisinsight.springer.com/drugs/800049924
  2. ^ a b c Agusti, Ana; Llansola, Marta; Hernández-Rabaza, Vicente; Cabrera-Pastor, Andrea; Montoliu, Carmina; Felipo, Vicente (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. ISSN 0960-0760.
  3. ^ Johansson, Maja; Månsson, Maria; Lins, Lars-Eric; Scharschmidt, Bruce; Doverskog, Magnus; Bäckström, Torbjörn (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. ISSN 0033-3158. PMC 5919995.
  4. ^ Johansson, Maja; Agusti, Ana; Llansola, Marta; Montoliu, Carmina; Strömberg, Jessica; Malinina, Evgenya; Ragagnin, Gianna; Doverskog, Magnus; Bäckström, Torbjörn; Felipo, Vicente (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–G409. doi:10.1152/ajpgi.00073.2015. ISSN 0193-1857. PMC 4556948.

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