Golexanolone

Golexanolone
Clinical data
Other names	GR-3027; 3α-Ethynyl-3β-hydroxyandrostan-17E-one oxime
Identifiers
	IUPAC name (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	2089238-18-4;
PubChem CID	132190533;
UNII	9C48F08TP2;
Chemical and physical data
Formula	C21H31NO2
Molar mass	329.484 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES 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 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; Key:FFIBGVYTWNPLPN-BZLGYYABSA-N;

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]

References

^ ^a ^b https://adisinsight.springer.com/drugs/800049924
^ ^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.
^ 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.
^ 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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