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Clinical data
Other namesGR-3027; 3α-Ethynyl-3β-hydroxyandrostan-17E-one oxime
  • (3S,5S,8R,9S,10S,13S,14S,17E)-3-Ethynyl-17-hydroxyimino-10,13-dimethyl-2,4,5,6,7,8,9,11,12,14,15,16-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol
CAS Number
PubChem CID
Chemical and physical data
Molar mass329.484 g·mol−1
3D model (JSmol)
  • C[C@]12CC[C@](C[C@@H]1CC[C@@H]3[C@@H]2CC[C@]\4([C@H]3CC/C4=N\O)C)(C#C)O
  • InChI=1S/C21H31NO2/c1-4-21(23)12-11-19(2)14(13-21)5-6-15-16-7-8-18(22-24)20(16,3)10-9-17(15)19/h1,14-17,23-24H,5-13H2,2-3H3/b22-18+/t14-,15-,16-,17-,19-,20-,21-/m0/s1

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 "Golexanolone - Umecrine Cognition". AdisInsight. Springer Nature Switzerland AG.
  2. ^ 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.
  3. ^ 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.
  4. ^ 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.

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