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Chemical Compound Review

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

Synonyms: Pregnanolone, Allopregnanolone, 3-Hydroxypregnan-20-one, Pregnan-3alpha-ol-20-one, Allopregnan-3 beta-ol-20-one, ...
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Disease relevance of ELTANOLONE


High impact information on ELTANOLONE


Chemical compound and disease context of ELTANOLONE


Biological context of ELTANOLONE


Anatomical context of ELTANOLONE

  • Furthermore, the effect of pulsatile infusion (six pulses; 10 min on, 30 min off) of low doses of the following three progestins [5 beta-pregnan-3 beta-ol-20-one (pregnanolone), 5 alpha-pregnan-3 alpha-ol-20-one (3 alpha-5 alpha-P), and 20 alpha-OH-P] into the hypothalamus of does using push-pull cannulae were examined in Exp III [16].
  • The reduced uptake of pregnanolone in cerebellum, cortex and hippocampus (after 2.0 g kg(-1)) was not due to a corresponding change in serum concentration [17].
  • In membranes from cerebellum, there was little overall change in pregnanolone potency although the effects of threshold concentrations were increased [18].
  • A similar reduction of pregnanolone tissue concentrations was only found in brain stem and striatum [17].
  • CONCLUSIONS: Eltanolone induced no significant inotropic effect on rat myocardium [19].

Associations of ELTANOLONE with other chemical compounds


Gene context of ELTANOLONE

  • Finally, the neuroactive steroid pregnanolone [(3alpha,5beta)-3-hydroxypregnan-20-one] produced anesthesia (loss of righting reflex) in VDAC-1- and VDAC-3-deficient mice, and there was no difference in the recovery time between the VDAC-deficient mice and wild-type controls [26].
  • In this connection, cellular radiolabeling with [3H] pregnanolone (3 alpha-hydroxy-5 alpha-pregnane-20-one) revealed bFGF to be a potent inhibitor of the steroidogenic enzyme 17 alpha-hydroxylase/17-20-lyase [27].
  • Sub-hypnotic doses (7.5 and 12.5 mg/kg, i.p.) of pregnanolone, administered 10 min before GHB, dose-dependently facilitated the expression of GHB-induced LORR in GHB-R male rats [28].
  • Following application of the steroids 5alpha-pregnan-3alpha,21-diol-20-one (5alpha-THDOC), alphaxalone and 5beta-pregnan-3alpha-ol-20-one (pregnanolone) hyperpolarizing PSPs developed into biphasic responses consisting of an early hyperpolarizing and a late depolarizing PSP sequence [29].
  • Myocardial effects of eltanolone in hamsters with hypertrophic cardiomyopathy [30].

Analytical, diagnostic and therapeutic context of ELTANOLONE


  1. alpha4beta3delta GABA(A) receptors characterized by fluorescence resonance energy transfer-derived measurements of membrane potential. Adkins, C.E., Pillai, G.V., Kerby, J., Bonnert, T.P., Haldon, C., McKernan, R.M., Gonzalez, J.E., Oades, K., Whiting, P.J., Simpson, P.B. J. Biol. Chem. (2001) [Pubmed]
  2. Relative potency of eltanolone, propofol, and thiopental for induction of anesthesia. Van Hemelrijck, J., Muller, P., Van Aken, H., White, P.F. Anesthesiology (1994) [Pubmed]
  3. Effects of eltanolone on cerebral blood flow and metabolism in healthy volunteers. Wolff, J., Carl, P., Hansen, P.B., Høgskilde, S., Christensen, M.S., Sørensen, M.B. Anesthesiology (1994) [Pubmed]
  4. Pregnanolone: a new steroid intravenous anaesthetic. Dose-finding study. Powell, H., Morgan, M., Sear, J.W. Anaesthesia. (1992) [Pubmed]
  5. Pregnanolone (3 alpha-hydroxy-5 alpha-pregnane-20-one), a progesterone metabolite, facilitates inhibition of synaptic transmission in the Schäffer collateral pathway of the guinea pig hippocampus in vitro. Landgren, S.O. Epilepsy Res. (1991) [Pubmed]
  6. 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]
  7. Dipole potential and head-group spacing are determinants for the membrane partitioning of pregnanolone. Alakoskela, J.M., Söderlund, T., Holopainen, J.M., Kinnunen, P.K. Mol. Pharmacol. (2004) [Pubmed]
  8. Circulating levels of anxiolytic steroids in the luteal phase in women with premenstrual syndrome and in control subjects. Schmidt, P.J., Purdy, R.H., Moore, P.H., Paul, S.M., Rubinow, D.R. J. Clin. Endocrinol. Metab. (1994) [Pubmed]
  9. Citalopram increases pregnanolone sensitivity in patients with premenstrual syndrome: an open trial. Sundström, I., Bäckström, T. Psychoneuroendocrinology (1998) [Pubmed]
  10. Effects of neurosteroids on glucocorticoid receptor-mediated gene transcription in LMCAT cells-A possible interaction with psychotropic drugs. Basta-Kaim, A., Budziszewska, B., Jaworska-Feil, L., Le??kiewicz, M., Tetich, M., Otczyk, M., Kubera, M., Laso??, W. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology (2007) [Pubmed]
  11. The interaction of eltanolone and fentanyl with special reference to logistic regression analysis. Bowen, P.J., Windsor, A., Flaishon, R., Sebel, P.S. Anesth. Analg. (1998) [Pubmed]
  12. Pharmacokinetic-pharmacodynamic modeling of the new steroid hypnotic eltanolone in healthy volunteers. Hering, W.J., Ihmsen, H., Langer, H., Uhrlau, C., Dinkel, M., Geisslinger, G., Schüttler, J. Anesthesiology (1996) [Pubmed]
  13. Effects of eltanolone on myocardial performance and coronary flow in intact and catecholamine-depleted isolated rabbit hearts. Mouren, S., Abdenour, L., Souktani, R., Coriat, P. Anesthesiology (1996) [Pubmed]
  14. Estradiol and the addition of progesterone increase the sensitivity to a neurosteroid in postmenopausal women. Wihlbäck, A.C., Nyberg, S., Bäckström, T., Bixo, M., Sundström-Poromaa, I. Psychoneuroendocrinology (2005) [Pubmed]
  15. Steroid potentiation and inhibition of N-methyl-D-aspartate receptor-mediated intracellular Ca++ responses: structure-activity studies. Irwin, R.P., Lin, S.Z., Rogawski, M.A., Purdy, R.H., Paul, S.M. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  16. Infusion of progestins into the hypothalamus of female New Zealand white rabbits: effect on in vivo luteinizing hormone-releasing hormone release as determined with push-pull perfusion. Lin, W.W., Ramirez, V.D. Endocrinology (1990) [Pubmed]
  17. The interaction between ethanol and pregnanolone at induction of anaesthesia investigated with a threshold method in male rats. Wang, M.D., Zhu, D., Bäckström, T., Wahlström, G. Br. J. Pharmacol. (2001) [Pubmed]
  18. The influence of membrane cholesterol on the GABAA receptor. Bennett, P.J., Simmonds, M.A. Br. J. Pharmacol. (1996) [Pubmed]
  19. In vitro effects of eltanolone on rat myocardium. Riou, B., Ruel, P., Hanouz, J.L., Langeron, O., Lecarpentier, Y., Viars, P. Anesthesiology (1995) [Pubmed]
  20. 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]
  21. Pharmacological characterisation of multiple components in the enhancement by pregnanolone and propofol of [3H]flunitrazepam binding to GABAA receptors. Zhong, Y., Simmonds, M.A. Neuropharmacology (1996) [Pubmed]
  22. Concentration-effect relationships of eltanolone given as a bolus dose or constant rate intravenous infusion to healthy male volunteers. Wessén, A., Parivar, K., Widman, M., Nilsson, A., Hartvig, P. Anesthesiology (1996) [Pubmed]
  23. Differential antagonism by epipregnanolone of alphaxalone and pregnanolone potentiation of [3H]flunitrazepam binding suggests more than one class of binding site for steroids at GABAA receptors. Prince, R.J., Simmonds, M.A. Neuropharmacology (1993) [Pubmed]
  24. Negative GABA(A) modulators attenuate the discriminative stimulus effects of benzodiazepines and the neuroactive steroid pregnanolone in rhesus monkeys. McMahon, L.R., France, C.P. Psychopharmacology (Berl.) (2005) [Pubmed]
  25. Inhibition of evoked glutamate release by neurosteroid allopregnanolone via inhibition of L-type calcium channels in rat medial prefrontal cortex. Hu, A.Q., Wang, Z.M., Lan, D.M., Fu, Y.M., Zhu, Y.H., Dong, Y., Zheng, P. Neuropsychopharmacology (2007) [Pubmed]
  26. Neuroactive steroid interactions with voltage-dependent anion channels: lack of relationship to GABA(A) receptor modulation and anesthesia. Darbandi-Tonkabon, R., Manion, B.D., Hastings, W.R., Craigen, W.J., Akk, G., Bracamontes, J.R., He, Y., Sheiko, T.V., Steinbach, J.H., Mennerick, S.J., Covey, D.F., Evers, A.S. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
  27. Basic fibroblast growth factor inhibits gonadotropin-supported ovarian androgen biosynthesis: mechanism(s) and site(s) of action. Hurwitz, A., Hernandez, E.R., Resnick, C.E., Packman, J.N., Payne, D.W., Adashi, E.Y. Endocrinology (1990) [Pubmed]
  28. Endogenous gamma-aminobutyric acid (GABA)(A) receptor active neurosteroids and the sedative/hypnotic action of gamma-hydroxybutyric acid (GHB): a study in GHB-S (sensitive) and GHB-R (resistant) rat lines. Barbaccia, M.L., Carai, M.A., Colombo, G., Lobina, C., Purdy, R.H., Gessa, G.L. Neuropharmacology (2005) [Pubmed]
  29. Neuroactive steroids induce GABA(A) receptor-mediated depolarizing postsynaptic potentials in hippocampal CA1 pyramidal cells of the rat. Burg, M., Heinemann, U., Schmitz, D. Eur. J. Neurosci. (1998) [Pubmed]
  30. Myocardial effects of eltanolone in hamsters with hypertrophic cardiomyopathy. Ruel, P., Hanouz, J.L., Riou, B., Lecarpentier, Y., Coriat, P. British journal of anaesthesia. (1996) [Pubmed]
  31. Determination of C-21 ketosteroids in serum using trifluoromethanesulfonic acid catalyzed precolumn dansylation and 1,1'-oxalyldiimidazole postcolumn peroxyoxalate chemiluminescence detection. Appelblad, P., Jonsson, T., Bäckström, T., Irgum, K. Anal. Chem. (1998) [Pubmed]
  32. Lack of anticonvulsant tolerance to the neuroactive steroid pregnanolone in mice. Kokate, T.G., Yamaguchi, S., Pannell, L.K., Rajamani, U., Carroll, D.M., Grossman, A.B., Rogawski, M.A. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
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