List of neurosteroids
This is a list of neurosteroids, or natural and synthetic steroids that are active on the mammalian nervous system through receptors other than steroid hormone receptors. It includes inhibitory, excitatory, and neurotrophic neurosteroids as well as pheromones and vomeropherines. In contrast to steroid hormones, neurosteroids have rapid, non-genomic effects through interactions with membrane steroid receptors and can quickly influence central nervous system function.
Inhibitory
Natural
Cholestanes
- 25-Hydroxycholesterol: cholest-5-en-3β,25-diol – NMDA receptor negative allosteric modulator
Androstanes
- 3α,5α-Androstanediol : 5α-androstane-3α,17β-diol – GABAA receptor positive allosteric modulator
- 3α,5β-Androstanediol : 5β-androstane-3α,17β-diol – GABAA receptor positive allosteric modulator
- 3α-Androstenol: 5α-androst-16-en-3α-ol – GABAA receptor positive allosteric modulator
- Androsterone: 5α-androstan-3α-ol-17-one – GABAA receptor positive allosteric modulator
- Etiocholanolone: 5β-androstan-3α-ol-17-one – GABAA receptor positive allosteric modulator
- Dihydrotestosterone : 5α-androst-17β-ol-3-one – of the above-listed inhibitory androstane neurosteroids
- Testosterone: androst-4-en-17β-ol-3-one – of the above-listed inhibitory androstane neurosteroids
Pregnanes
- 3α-Dihydroprogesterone : pregn-4-en-3α-ol-20-one – GABAA receptor positive allosteric modulator
- 5α-Dihydroprogesterone : 5α-pregnane-3,20-dione – GABAA receptor positive allosteric modulator
- 5β-Dihydroprogesterone : 5β-pregnane-3,20-dione – GABAA receptor positive allosteric modulator
- Allopregnanediol: 5α-pregnane-3α,20α-diol – GABAA receptor positive allosteric modulator
- Allopregnanolone : 5α-pregnan-3α-ol-20-one – GABAA receptor positive allosteric modulator
- Dihydrodeoxycorticosterone : 21-hydroxy-5α-pregnan-20-one – GABAA receptor positive allosteric modulator
- Pregnanediol: 5β-pregnan-3α,20α-diol – GABAA receptor positive allosteric modulator
- Pregnanolone : 5β-pregnan-3α-ol-20-one – GABAA receptor positive allosteric modulator
- Tetrahydrodeoxycorticosterone : 3α,21-dihydroxy-5α-pregnan-20-one – GABAA receptor positive allosteric modulator
- Deoxycorticosterone : 21-hydroxypregn-4-ene-3,20-dione – of DHDOC and THDOC
- Pregnenolone : pregn-5-en-3β-ol-20-one – of pregnanolones and pregnanediols
- Progesterone : pregn-4-ene-3,20-dione – of pregnanediones, pregnanolones, and pregnanediols
Synthetic
Cholestanes
- Acebrochol : 5α,6β-dibromocholestan-3β-ol 3β-acetate – GABAA receptor positive allosteric modulator
Pregnanes
- Alfadolone: 3α,21-dihydroxy-5α-pregnane-11,20-dione – GABAA receptor positive allosteric modulator
- Alfadolone acetate: 3α,21-dihydroxy-5α-pregnane-11,20-dione 21-acetate – GABAA receptor positive allosteric modulator
- Alfaxalone: 3α-hydroxy-5α-pregnane-11,20-dione – GABAA receptor positive allosteric modulator
- EIDD-036 : 20-pregn-4-en-3-one – progesterone-like inhibitory neurosteroid
- Ganaxolone: 3β-methyl-5α-pregnan-3α-ol-20-one – GABAA receptor positive allosteric modulator
- Hydroxydione: 21-hydroxy-5β-pregnane-3,20-dione – GABAA receptor positive allosteric modulator
- Minaxolone: 11α--2β-ethoxy-5α-pregnan-3α-ol-20-one – GABAA receptor positive allosteric modulator
- ORG-20599: 21-chloro-2β-morpholin-4-yl-5β-pregnan-3α-ol-20-one – GABAA receptor positive allosteric modulator
- ORG-21465: 2β--3α-hydroxy-11,20-dioxo-5α-pregnan-21-yl methanesulfonate – GABAA receptor positive allosteric modulator
- Renanolone: 5β-pregnan-3α-ol-11,20-dione – GABAA receptor positive allosteric modulator
- SGE-516 – GABAA receptor positive allosteric modulator
- SGE-872 – GABAA receptor positive allosteric modulator
- SAGE-217, Zuranolone: 3α-hydroxy-3β-methyl-21--19-nor-5β-pregnan-20-one – GABAA receptor positive allosteric modulator
- EIDD-1723 – of EIDD-036
- P1-185 – of progesterone and by extension pregnanediones, pregnanolones, and pregnanediols
- Progesterone carboxymethyloxime – of progesterone and by extension pregnanediones, pregnanolones, and pregnanediols
Excitatory
Natural
Cholestanes
- Cerebrosterol : cholest-5-en-3β,24S-diol – NMDA receptor positive allosteric modulator
Pregnanes
- 3β-Dihydroprogesterone : pregn-4-en-3β-ol-20-one – GABAA receptor negative allosteric modulator
- Epipregnanolone: 5β-pregnan-3β-ol-20-one – GABAA receptor negative allosteric modulator
- Isopregnanolone : 5α-pregnan-3β-ol-20-one – GABAA receptor negative allosteric modulator
- Pregnenolone sulfate : pregn-5-en-3β-ol-20-one 3β-sulfate – GABAA receptor negative allosteric modulator, NMDA receptor positive allosteric modulator, sigma-1 receptor agonist, TRPM3 agonist, other actions
- Pregnenolone : pregn-5-en-3β-ol-20-one – of pregnenolone sulfate
Androstanes
- Dehydroepiandrosterone : androst-5-en-3β-ol-17-one – GABAA receptor positive allosteric modulator, NMDA receptor positive allosteric modulator, sigma-1 receptor agonist, other actions
- Dehydroepiandrosterone sulfate : androst-5-en-3β-ol-17-one 3β-sulfate – GABAA receptor positive allosteric modulator, NMDA receptor positive allosteric modulator, other actions
Synthetic
Androstanes
- 17-Phenylandrostenol : 17-phenyl-5α-androst-16-en-3α-ol – GABAA receptor negative allosteric modulator
- Golexanolone : 3α-ethynyl-3β-hydroxyandrostan-17E-one oxime – GABAA receptor negative allosteric modulator
Others
- SGE-201 - oxysterol/cholesterol analogue – NMDA receptor positive allosteric modulator
- SGE-301 - oxysterol/cholesterol analogue – NMDA receptor positive allosteric modulator
- SAGE-718: oxysterol/cholesterol analogue; exact chemical structure undisclosed – NMDA receptor positive allosteric modulator
Mixed
Natural
Cholestanes
- Cholesterol: cholest-5-en-3β-ol – NMDA receptor positive allosteric modulator, possible GABAA receptor positive allosteric modulator, many other actions
Pregnanes
- Epipregnanolone sulfate: 5β-pregnan-3β-ol-20-one 3β-sulfate – GABAA and NMDA receptor negative allosteric modulator, TRPM3 agonist
Neurotrophic
Natural
Androstanes
- Dehydroepiandrosterone : androst-5-en-3β-ol-17-one – TrkA, TrkC, and p75NTR agonist, TrkB ligand
- Dehydroepiandrosterone sulfate : androst-5-en-3β-ol-17-one 3β-sulfate – TrkA and p75NTR agonist
Ergostanes
- Anicequol : 16β-acetoxy-3β,7β,11β-trihydroxy-5α-ergost-22-en-6-one – non-endogenous; fungi-derived; undefined mechanism of action; shows neurotrophic activity in vitro; was formerly under development for the treatment of cognitive disorders
Synthetic
Androstanes
- BNN-20: 17β-spiro--3β-ol – TrkA, TrkB, and p75NTR agonist
Pregnanes
- BNN-27: 17α,20R-epoxypregn-5-ene-3β,21-diol – TrkA and p75NTR agonist
Antineurotrophic
Natural
Androstanes
- Testosterone: androst-4-en-17β-ol-3-one – TrkA and p75NTR antagonist
Synthetic
Pregnanes
- Dexamethasone: 9α-fluoro-11β,17α,21-trihydroxy-16α-methylpregna-1,4-diene-3,20-dione – TrkA and p75NTR antagonist
Pheromones and pherines
Natural
Androstanes
- 3α-Androstenol: 5α-androst-16-en-3α-ol
- 3β-Androstenol: 5α-androst-16-en-3β-ol
- Androstadienol: androsta-5,16-dien-3β-ol
- Androstadienone: androsta-4,16-dien-3-one
- Androstenone: 5α-androst-16-en-3-one
- Androsterone: 5α-androstan-3α-ol-17-one
Estranes
- Estratetraenol: estra-1,3,5,16-tetraen-3-ol
Synthetic
Androstanes
- 4-Androstadienol : androsta-4,16-dien-3β-ol
Estranes
- Estratetraenyl acetate : estra-1,3,5,16-tetraen-3-yl acetate
Pregnanes
- Pregnadienedione : pregna-4,20-dien-3,6-dione
Others
- PH10, PH15, PH30, PH56, PH78, PH84, Salubrin – pherines with undefined structures developed by a company called Pherin Pharmaceuticals
Others
Natural
Pregnanes
- Pregnenolone : pregn-5-en-3β-ol-20-one – MAP2 ligand
- Progesterone : pregn-4-ene-3,20-dione – sigma-1 receptor antagonist, nicotinic acetylcholine receptor negative allosteric modulator, MAP2 ligand, other actions
Spirostanes
- Caprospinol : -20α-spirost-5-en-3β-yl hexanoate – β-amyloid ligand, sigma-1 receptor ligand, other actions; found naturally in Gynura japonica; under development as a neuroprotective against Alzheimer's disease
Synthetic
Pregnanes
- 3β-Methoxypregnenolone : 3β-methoxypregn-5-en-20-one – MAP2 ligand
- Cyclopregnol : 6β-hydroxy-3:5-cyclopregnan-20-one – undefined mechanism of action; developed as a "psychotropic agent" for the treatment of "mental disorders" such as schizophrenia in the 1950s
Androstanes
- Cetadiol: androst-5-ene-3β,16α-diol – undefined mechanism of action; developed as a "tranquilizer" and for the treatment of alcoholism in the 1950s