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Chemical Compound Review

Allopregnanolone     1- [(3S,5S,8S,9S,10S,13S,14S,17S) -3-hydroxy...

Synonyms: SureCN598848, AG-F-75099, CHEMBL2057301, CHEBI:11909, HMDB01455, ...
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Disease relevance of Allopregnanolone


Psychiatry related information on Allopregnanolone


High impact information on Allopregnanolone


Chemical compound and disease context of Allopregnanolone


Biological context of Allopregnanolone

  • Neonatal administration of allopregnanolone delays the onset of neurological symptoms, increases Purkinje and granule cell survival, reduces cortical GM2 and GM3 ganglioside accumulation and doubles the lifespan of NP-C mice [11].
  • We found that magnocellular oxytocin neurons in adult female rats exhibit an endogenous GABA(A) receptor subunit switch around parturition: a decrease in alpha1:alpha2 subunit mRNA ratio correlated with a decrease in allopregnanolone potentiation and increase in decay time constant of the GABA(A) receptor-mediated IPSCs in these cells [12].
  • Recently, allopregnanolone and allotetrahydroDOC have also been measured in brain and plasma where their levels have been shown to fluctuate in response to stress and during the estrous and menstrual cycles of rats and humans, respectively [21].
  • Interfering with PROG's metabolism to, or the biosynthesis of, 3alpha-hydroxy-5alpha-pregnan-20-one (3alpha,5alpha-TH PROG or allopregnanolone), the most effective endogenous GBR agonist, in the VTA attenuates female sexual behavior in rodents [22].
  • Finally, PMDD women with greater levels of premenstrual anxiety and irritability had significantly reduced allopregnanolone levels in the luteal phase relative to less symptomatic PMDD women [23].

Anatomical context of Allopregnanolone


Associations of Allopregnanolone with other chemical compounds


Gene context of Allopregnanolone


Analytical, diagnostic and therapeutic context of Allopregnanolone


  1. Rise in intracellular calcium via a nongenomic effect of allopregnanolone in fetal rat hypothalamic neurons. Dayanithi, G., Tapia-Arancibia, L. J. Neurosci. (1996) [Pubmed]
  2. Pharmacology of endogenous neuroactive steroids. Reddy, D.S. Critical reviews in neurobiology. (2003) [Pubmed]
  3. High serum allopregnanolone levels in girls with precocious puberty. Iughetti, L., Predieri, B., Cobellis, L., Luisi, S., Luisi, M., Forese, S., Petraglia, F., Bernasconi, S. J. Clin. Endocrinol. Metab. (2002) [Pubmed]
  4. Serum allopregnanolone levels in pregnant women: changes during pregnancy, at delivery, and in hypertensive patients. Luisi, S., Petraglia, F., Benedetto, C., Nappi, R.E., Bernardi, F., Fadalti, M., Reis, F.M., Luisi, M., Genazzani, A.R. J. Clin. Endocrinol. Metab. (2000) [Pubmed]
  5. Diminished allopregnanolone enhancement of GABA(A) receptor currents in a rat model of chronic temporal lobe epilepsy. Mtchedlishvili, Z., Bertram, E.H., Kapur, J. J. Physiol. (Lond.) (2001) [Pubmed]
  6. The neurosteroid allopregnanolone is reduced in prefrontal cortex in Alzheimer's disease. Marx, C.E., Trost, W.T., Shampine, L.J., Stevens, R.D., Hulette, C.M., Steffens, D.C., Ervin, J.F., Butterfield, M.I., Blazer, D.G., Massing, M.W., Lieberman, J.A. Biol. Psychiatry (2006) [Pubmed]
  7. Decreased cerebrospinal fluid allopregnanolone levels in women with posttraumatic stress disorder. Rasmusson, A.M., Pinna, G., Paliwal, P., Weisman, D., Gottschalk, C., Charney, D., Krystal, J., Guidotti, A. Biol. Psychiatry (2006) [Pubmed]
  8. Effects of triazolam at three phases of the menstrual cycle. Rukstalis, M., de Wit, H. Journal of clinical psychopharmacology. (1999) [Pubmed]
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  10. Distress vocalizations in maternally separated mouse pups: modulation via 5-HT(1A), 5-HT(1B) and GABA(A) receptors. Fish, E.W., Sekinda, M., Ferrari, P.F., Dirks, A., Miczek, K.A. Psychopharmacology (Berl.) (2000) [Pubmed]
  11. Niemann-Pick type C disease involves disrupted neurosteroidogenesis and responds to allopregnanolone. Griffin, L.D., Gong, W., Verot, L., Mellon, S.H. Nat. Med. (2004) [Pubmed]
  12. Plasticity in fast synaptic inhibition of adult oxytocin neurons caused by switch in GABA(A) receptor subunit expression. Brussaard, A.B., Kits, K.S., Baker, R.E., Willems, W.P., Leyting-Vermeulen, J.W., Voorn, P., Smit, A.B., Bicknell, R.J., Herbison, A.E. Neuron (1997) [Pubmed]
  13. Pregnane X receptor (PXR) activation: A mechanism for neuroprotection in a mouse model of Niemann-Pick C disease. Langmade, S.J., Gale, S.E., Frolov, A., Mohri, I., Suzuki, K., Mellon, S.H., Walkley, S.U., Covey, D.F., Schaffer, J.E., Ory, D.S. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
  14. In socially isolated mice, the reversal of brain allopregnanolone down-regulation mediates the anti-aggressive action of fluoxetine. Pinna, G., Dong, E., Matsumoto, K., Costa, E., Guidotti, A. Proc. Natl. Acad. Sci. U.S.A. (2003) [Pubmed]
  15. Stress-induced elevations of gamma-aminobutyric acid type A receptor-active steroids in the rat brain. Purdy, R.H., Morrow, A.L., Moore, P.H., Paul, S.M. Proc. Natl. Acad. Sci. U.S.A. (1991) [Pubmed]
  16. Enhanced anticonvulsant activity of neuroactive steroids in a rat model of catamenial epilepsy. Reddy, D.S., Rogawski, M.A. Epilepsia (2001) [Pubmed]
  17. Initial sensitivity, tolerance and cross-tolerance to allopregnanolone- and ethanol-induced hypothermia in selected mouse lines. Palmer, A.A., Moyer, M.R., Crabbe, J.C., Phillips, T.J. Psychopharmacology (Berl.) (2002) [Pubmed]
  18. Ethnic differences in allopregnanolone concentrations in women during rest and following mental stress. Girdler, S.S., Beth Mechlin, M., Light, K.C., Leslie Morrow, A. Psychophysiology. (2006) [Pubmed]
  19. Low pregnenolone sulphate plasma concentrations in patients with generalized social phobia. Heydari, B., Le Mellédo, J.M. Psychological medicine. (2002) [Pubmed]
  20. Infusion of neurosteroids into the rat nucleus basalis affects paradoxical sleep in accordance with their memory modulating properties. Darnaudéry, M., Pallarés, M., Bouyer, J.J., Le Moal, M., Mayo, W. Neuroscience (1999) [Pubmed]
  21. Neuroactive steroids. Paul, S.M., Purdy, R.H. FASEB J. (1992) [Pubmed]
  22. The role of neurosteroids and non-genomic effects of progestins and androgens in mediating sexual receptivity of rodents. Frye, C.A. Brain Res. Brain Res. Rev. (2001) [Pubmed]
  23. Allopregnanolone levels and reactivity to mental stress in premenstrual dysphoric disorder. Girdler, S.S., Straneva, P.A., Light, K.C., Pedersen, C.A., Morrow, A.L. Biol. Psychiatry (2001) [Pubmed]
  24. Gas chromatographic-mass fragmentographic quantitation of 3 alpha-hydroxy-5 alpha-pregnan-20-one (allopregnanolone) and its precursors in blood and brain of adrenalectomized and castrated rats. Cheney, D.L., Uzunov, D., Costa, E., Guidotti, A. J. Neurosci. (1995) [Pubmed]
  25. Identification of fatty acid esters of pregnenolone and allopregnanolone from bovine corpora lutea. Albert, D.H., Ponticorvo, L., Lieberman, S. J. Biol. Chem. (1980) [Pubmed]
  26. Neuroactive steroid effects on cognitive functions with a focus on the serotonin and GABA systems. Birzniece, V., Bäckström, T., Johansson, I.M., Lindblad, C., Lundgren, P., Löfgren, M., Olsson, T., Ragagnin, G., Taube, M., Turkmen, S., Wahlström, G., Wang, M.D., Wihlbäck, A.C., Zhu, D. Brain Res. Brain Res. Rev. (2006) [Pubmed]
  27. Hormonal regulation of atypical absence seizures. Persad, V., Ting Wong, C.G., Cortez, M.A., Wang, Y.T., Snead, O.C. Ann. Neurol. (2004) [Pubmed]
  28. Impairments in spatial learning and memory: ethanol, allopregnanolone, and the hippocampus. Silvers, J.M., Tokunaga, S., Berry, R.B., White, A.M., Matthews, D.B. Brain Res. Brain Res. Rev. (2003) [Pubmed]
  29. Neuroactive pregnanolone isomers during pregnancy. Parízek, A., Hill, M., Kancheva, R., Havlíková, H., Kancheva, L., Cindr, J., Pasková, A., Pouzar, V., Cerny, I., Drbohlav, P., Hájek, Z., Stárka, L. J. Clin. Endocrinol. Metab. (2005) [Pubmed]
  30. Kinetics of allopregnanolone formation catalyzed by human 3 alpha-hydroxysteroid dehydrogenase type III (AKR1C2). Trauger, J.W., Jiang, A., Stearns, B.A., LoGrasso, P.V. Biochemistry (2002) [Pubmed]
  31. Hypothalamic amenorrhea with normal body weight: ACTH, allopregnanolone and cortisol responses to corticotropin-releasing hormone test. Meczekalski, B., Tonetti, A., Monteleone, P., Bernardi, F., Luisi, S., Stomati, M., Luisi, M., Petraglia, F., Genazzani, A.R. Eur. J. Endocrinol. (2000) [Pubmed]
  32. PXR (NR1I2): splice variants in human tissues, including brain, and identification of neurosteroids and nicotine as PXR activators. Lamba, V., Yasuda, K., Lamba, J.K., Assem, M., Davila, J., Strom, S., Schuetz, E.G. Toxicol. Appl. Pharmacol. (2004) [Pubmed]
  33. CYP2D in the brain. Funae, Y., Kishimoto, W., Cho, T., Niwa, T., Hiroi, T. Drug Metab. Pharmacokinet. (2003) [Pubmed]
  34. The influence of subchronic administration of the neurosteroid allopregnanolone on sleep in the rat. Damianisch, K., Rupprecht, R., Lancel, M. Neuropsychopharmacology (2001) [Pubmed]
  35. Functional changes in rat nigral GABA(A) receptors induced by degeneration of the striatonigral GABAergic pathway: an electrophysiological study of receptors incorporated into Xenopus oocytes. Sanna, E., Motzo, C., Usala, M., Pau, D., Cagetti, E., Biggio, G. J. Neurochem. (1998) [Pubmed]
  36. Neurosteroid withdrawal model of perimenstrual catamenial epilepsy. Reddy, D.S., Kim, H.Y., Rogawski, M.A. Epilepsia (2001) [Pubmed]
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