Brexanolone, also known as 3a5a-Allopregnanolone; Allotetrahydroprogesterone and Allopregnanolone, is a GABA(A) receptor modulator potentially for the treatment of epilepsy and depression. Brexanolone was approved in 3/19/201 9to treat postpartum depression (PPD) in adult women.
MacNevin, Christopher J.; Atif, Fahim; Sayeed, Iqbal; Stein, Donald G.; Liotta, Dennis C. Development and Screening of Water-Soluble Analogues of Progesterone and Allopregnanolone in Models of Brain Injury. Journal of Medicinal Chemistry. Volume 52. Issue 19. Pages 6012-6023. Journal. (2009).
Kapras, Vojtech; Stastna, Eva; Chodounska, Hana; Pouzar, Vladimir; Kristofikova, Zdena. Preparation of steroid sulfamates and their interaction with GABAA receptor. Collection of Czechoslovak Chemical Communications. Volume 74. Issue 4. Pages 643-650. Journal. (2009).
Gu, Xiangzhong; Jiang, Chengyu; Qiu, Wenwei; Gao, Wei. Process for configuration inversion of 3-hydroxy group in steroids. Assignee Jiangsu Jiaerke Pharmaceutical Group Co., Ltd., Peop. Rep. China. CN 108864237. (2018).
Wu, Peiying; Wang, Qinghao; Gao, Qi; Wang, Jun; Gu, Huifen. Method for preparing sterol compound by inverting the hydroxy configuration. Assignee Shanghai Xingling Pharmaceutical Co., Ltd., Peop. Rep. China. CN 103396467. (2013).
Mensah-Nyagan, Ayikoe Guy; Meyer, Laurence; Patte-Mensah, Christine; Taleb, Omar; Miesch, Michel; Geoffroy, Philippe; Ressault, Blandine. Derivatives of allopregnanolone and of epiallopregnanolone, their preparation and their uses for treating a neuropathological condition. Assignee Universite de Strasbourg, Fr.; Centre National de la Recherche Scientifique – CNRS. WO 2012127176. (2012).
MacNevin, Christopher; Stein, Donald G.; Liotta, Dennis C.; Sayeed, Iqbal; Guthrie, David B.; Lockwood, Mark A.; Natchus, Michael G. Preparation of steroid analogues for neuroprotection. Assignee Emory University, USA. WO 2009108804. (2009).
Karpenko, R. G.; Grinenko, G. S.; Davitishvili, M. G.; Malyutina, O. F. Nonenzymic synthesis of corticosteroids and related compounds. I. Tigogenin-based synthesis of 9,11-unsaturated steroids. Khimiko-Farmatsevticheskii Zhurnal. Volume 21. Issue 12. Pages 1466-9. Journal. (1987).
Kasal, Alexander; Pasztorova, Svetlana. On steroids. CCCLVII. Synthesis of RIA haptens: 3α,11α-dihydroxy-5α-pregnan-20-one 11-hemisuccinate. Collection of Czechoslovak Chemical Communications. Volume 58. Issue 3. Pages 619-28. Journal. (1993).
Souli, Charikleia; Avlonitis, Nicolaos; Calogeropoulou, Theodora; Tsotinis, Andrew; Maksay, Gabor; Biro, Timea; Politi, Aggeliki; Mavromoustakos, Thomas; Makriyannis, Alexandros; Reis, Heribert; Papadopoulos, Manthos. Novel 17β-Substituted Conformationally Constrained Neurosteroids that Modulate GABAA Receptors. Journal of Medicinal Chemistry. Volume 48. Issue 16. Pages 5203-5214. Journal. (2005).
