Synonyms: 3α,5α-tetrahydroprogesterone | 3α,5α-THP | allopregnanolone | SAGE-547 | SAGE547 | Zulresso®
5α-pregnan-3α-ol-20-one is an approved drug (FDA (2019))
Compound class:
Metabolite or derivative
Comment: This steroidal compound behaves as a neuroactive agent with anti-depressant activity in mood disorders [2-3]. Pharmacologically it is a positive allosteric modulator of GABAA receptors.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Meltzer-Brody S, Colquhoun H, Riesenberg R, Epperson CN, Deligiannidis KM, Rubinow DR, Li H, Sankoh AJ, Clemson C, Schacterle A et al.. (2018)
Brexanolone injection in post-partum depression: two multicentre, double-blind, randomised, placebo-controlled, phase 3 trials. Lancet, 392 (10152): 1058-1070. [PMID:30177236] |
2. Melón L, Hammond R, Lewis M, Maguire J. (2018)
A Novel, Synthetic, Neuroactive Steroid Is Effective at Decreasing Depression-Like Behaviors and Improving Maternal Care in Preclinical Models of Postpartum Depression. Front Endocrinol (Lausanne), 9: 703. [PMID:30532739] |
3. Wilkinson ST, Sanacora G. (2019)
A new generation of antidepressants: an update on the pharmaceutical pipeline for novel and rapid-acting therapeutics in mood disorders based on glutamate/GABA neurotransmitter systems. Drug Discov Today, 24 (2): 606-615. [PMID:30447328] |