MarketList of neurosteroids
Company Profile

List of neurosteroids

Neurosteroids are 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 Cholestanes25-Hydroxycholesterol: cholest-5-en-3β,25-diol – NMDA receptor negative allosteric modulator Androstanes3α,5α-Androstanediol (3α-androstanediol): 5α-androstane-3α,17β-diol – GABAA receptor positive allosteric modulator3α,5β-Androstanediol (etiocholanediol): 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 • Allopregnanolone (brexanolone; SAGE-547): 5α-pregnan-3α-ol-20-one – GABAA receptor positive allosteric modulator • Dihydrodeoxycorticosterone (DHDOC): 21-hydroxy-5α-pregnan-20-one – GABAA receptor positive allosteric modulator • Pregnanediol: 5β-pregnan-3α,20α-diol – GABAA receptor positive allosteric modulator • 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-(dimethylamino)-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-(2,2-dimethyl-4-morpholinyl)-3α-hydroxy-11,20-dioxo-5α-pregnan-21-yl methanesulfonate – GABAA receptor positive allosteric modulator • Posovolone (Co 134444): 3β-Hydroxy-21-(1H-imidazol-1-yl)-3α-(methoxymethyl)-5α-pregnan-20-one – 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 The following are proneurosteroids: • EIDD-1723 – of EIDD-036 (see above) • Progesterone carboxymethyloxime (P4-3-CMO) – of progesterone and by extension pregnanediones, pregnanolones, and pregnanediols (see above) ==Excitatory==
Excitatory
Natural CholestanesCerebrosterol (24(S)-Hydroxycholesterol): cholest-5-en-3β,24S-diol – NMDA receptor positive allosteric modulator Pregnanes3β-Dihydroprogesterone (3β-DHP): 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 (sepranolone): 5α-pregnan-3β-ol-20-one – GABAA receptor negative allosteric modulator • Pregnenolone sulfate (PS): 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 The following are proneurosteroids: • Pregnenolone (P5): pregn-5-en-3β-ol-20-one – of pregnenolone sulfate AndrostanesDehydroepiandrosterone (DHEA; prasterone): 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 (DHEA-S; prasterone sulfate): androst-5-en-3β-ol-17-one 3β-sulfate – GABAA receptor negative allosteric modulator, NMDA receptor positive allosteric modulator, other actions Synthetic Androstanes17-Phenylandrostenol (17-PA): 17-phenyl-5α-androst-16-en-3α-ol – GABAA receptor negative allosteric modulator • Golexanolone (GR-3027): 3α-ethynyl-3β-hydroxyandrostan-17E-one oxime – GABAA receptor negative allosteric modulator Others • SAGE-201 - oxysterol/cholesterol analogue – NMDA receptor positive allosteric modulator • SAGE-301 - oxysterol/cholesterol analogue – NMDA receptor positive allosteric modulator • SAGE-718: oxysterol/cholesterol analogue; exact chemical structure undisclosed – NMDA receptor positive allosteric modulator ==Mixed==
Mixed
Natural CholestanesCholesterol: cholest-5-en-3β-ol – NMDA receptor positive allosteric modulator, possible GABAA receptor positive allosteric modulator, many other actions PregnanesEpipregnanolone sulfate: 5β-pregnan-3β-ol-20-one 3β-sulfate – GABAA and NMDA receptor negative allosteric modulator, TRPM3 agonist ==Neurotrophic==
Neurotrophic
Natural AndrostanesDehydroepiandrosterone (DHEA; prasterone): androst-5-en-3β-ol-17-one – TrkA, TrkC, and p75NTR agonist, TrkB ligandDehydroepiandrosterone sulfate (DHEA-S; prasterone sulfate): androst-5-en-3β-ol-17-one 3β-sulfate – TrkA and p75NTR agonist ErgostanesAnicequol (NGA0187, NGD-187): 16β-acetoxy-3β,7β,11β-trihydroxy-5α-ergost-22(E)-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 AndrostanesBNN-20: 17β-spiro-(androst-5-en-17,2'-oxiran)-3β-ol – TrkA, TrkB, and p75NTR agonist PregnanesBNN-27: 17α,20R-epoxypregn-5-ene-3β,21-diol – TrkA and p75NTR agonist ==Antineurotrophic==
Antineurotrophic
Natural AndrostanesTestosterone: androst-4-en-17β-ol-3-one – TrkA and p75NTR antagonist Synthetic PregnanesDexamethasone: 9α-fluoro-11β,17α,21-trihydroxy-16α-methylpregna-1,4-diene-3,20-dione – TrkA and p75NTR antagonist ==Pheromones and pherines==
Pheromones and pherines
Natural Androstanes3α-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 EstranesEstratetraenol: estra-1,3,5(10),16-tetraen-3-ol Synthetic AndrostanesFasedienol (Aloradine; PH94B; 4-androstadienol): androsta-4,16-dien-3β-ol EstranesEstratetraenyl acetate (ETA): estra-1,3,5(10),16-tetraen-3-yl acetate PregnanesPregnadienedione (PDD): pregna-4,20-dien-3,6-dione OthersPH10, PH15, PH30, PH56, PH78, PH84, Salubrin (PH80) – pherines with undefined structures developed by a company called Pherin Pharmaceuticals ==Others==
Others
Natural PregnanesPregnenolone (P5): pregn-5-en-3β-ol-20-one – MAP2 ligand • Progesterone (P4): pregn-4-ene-3,20-dione – sigma-1 receptor antagonist, nicotinic acetylcholine receptor negative allosteric modulator, MAP2 ligand, other actions SpirostanesCaprospinol (SP-233; diosgenin 3-caproate): (22R,25R)-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 EstranesEstradiol (E2): Estra-1,3,5(10)-triene-3,17β-diol; found to increase the expression of the oxytocin receptor. Synthetic Pregnanes3β-Methoxypregnenolone (MAP-4343): 3β-methoxypregn-5-en-20-one – MAP2 ligand • Cyclopregnol (neurosterone): 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 AndrostanesCetadiol: androst-5-ene-3β,16α-diol – undefined mechanism of action; developed as a "tranquilizer" and for the treatment of alcoholism in the 1950s ==See also==
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