Neuroaktivni steroidi , takođe poznati kao neurosteroidi , su endogeni steroidi koji brzo menjaju neuronsku ekscitabilnost putem interakcija sa ligandom kontrolisanih jonskih kanala i drugih receptora na ćelijskoj površini .[1] [2] neurosteroid koji je formirao francuski fiziolog Étienne-Émile Baulieu obuhvata steroide koji su sintetisani u mozgu.[3] neuroaktivni steroid se odnose na steroide koje sintetišu endokrine žlezde i koji dospevaju do mozga putem krvotoka.[4] izražvanje gena putem nuklearnih steroidnih hormonskih receptora . Neurosteroidi imaju širok opseg potencijalnih kliničkih primena od sedacije do tretmana epilepsije [5] traumatičnih moždanih povreda .[6] [7] Ganaksolon , sintetički analog endogenog neurosteroida alopregnanolona , se ispituje za moguću primenu u tretmanu epilepsije.[8]
↑ Paul SM, Purdy RH (1992). "Neuroactive steroids" (abstract). FASEB J. 6 (6): 2311–22. PMID 1347506 . http://www.fasebj.org/cgi/content/abstract/6/6/2311 . ↑ Lan NC, Gee KW (1994). "Neuroactive steroid actions at the GABA-A receptor". Horm Behav 28 (4): 537–44. DOI :10.1006/hbeh.1994.1052 . PMID 7729823 . ↑ Reddy DS (2010). "Neurosteroids: endogenous role in the human brain and therapeutic potentials" . Prog. Brain Res. 186 : 113–37. DOI :10.1016/B978-0-444-53630-3.00008-7 . PMC 3139029 . PMID 21094889 . //www.ncbi.nlm.nih.gov/pmc/articles/PMC3139029/ . ↑ Srivastava DP, Waters EM, Mermelstein PG, Kramár EA, Shors TJ, Liu F (November 2011). "Rapid estrogen signaling in the brain: implications for the fine-tuning of neuronal circuitry" . J. Neurosci. 31 (45): 16056–63. DOI :10.1523/JNEUROSCI.4097-11.2011 . PMC 3245715 . PMID 22072656 . //www.ncbi.nlm.nih.gov/pmc/articles/PMC3245715/ . ↑ Reddy DS, Rogawski MA (April 2009). "Neurosteroid replacement therapy for catamenial epilepsy" . Neurotherapeutics 6 (2): 392–401. DOI :10.1016/j.nurt.2009.01.006 . PMC 2682439 . PMID 19332335 . //www.ncbi.nlm.nih.gov/pmc/articles/PMC2682439/ . ↑ Morrow AL (2007). "Recent Developments in the Significance and Therapeutic Relevance of Neuroactive Steroids – Introduction to the Special Issue" . Pharmacol. Ther. 116 (1): 1–6. DOI :10.1016/j.pharmthera.2007.04.003 . PMC 2047816 . PMID 17531324 . //www.ncbi.nlm.nih.gov/pmc/articles/PMC2047816/ . ↑ Dubrovsky BO (2005). "Steroids, neuroactive steroids and neurosteroids in psychopathology". Prog. Neuropsychopharmacol. Biol. Psychiatry 29 (2): 169–92. DOI :10.1016/j.pnpbp.2004.11.001 . PMID 15694225 . ↑ Bialer M, Johannessen SI, Levy RH, Perucca E, Tomson T, White HS (2013). ""Ganaxolone" in Bialer M, Johannessen SI, Levy RH, Perucca E, Tomson T, White HS: Progress report on new antiepileptic drugs: a summary of the Eleventh Eilat Conference (EILAT XI)". Epilepsy Res. 103 (1): 2–30. DOI :10.1016/j.eplepsyres.2012.10.001 . PMID 23219031 .
Akk G, Shu HJ, Wang C, Steinbach JH, Zorumski CF, Covey DF, Mennerick S (2005). "Neurosteroid access to the GABAA receptor". J. Neurosci. 25 (50): 11605–13. DOI :10.1523/JNEUROSCI.4173-05.2005 . PMID 16354918 . Wang JM, Johnston PB, Ball BG, Brinton RD (2005). "The neurosteroid allopregnanolone promotes proliferation of rodent and human neural progenitor cells and regulates cell-cycle gene and protein expression". J. Neurosci. 25 (19): 4706–18. DOI :10.1523/JNEUROSCI.4520-04.2005 . PMID 15888646 . Dong E, Matsumoto K, Uzunova V, Sugaya I, Takahata H, Nomura H, Watanabe H, Costa E, Guidotti A (2001). "Brain 5α-dihydroprogesterone and allopregnanolone synthesis in a mouse model of protracted social isolation" . Proc. Natl. Acad. Sci. U.S.A. 98 (5): 2849–54. DOI :10.1073/pnas.051628598 . PMC 30228 . PMID 11226329 . //www.ncbi.nlm.nih.gov/pmc/articles/PMC30228/ . Melcangi RC, Celotti F, Martini L (1994). "Progesterone 5-alpha-reduction in neuronal and in different types of glial cell cultures: type 1 and 2 astrocytes and oligodendrocytes". Brain Res. 639 (2): 202–6. DOI :10.1016/0006-8993(94)91731-0 . PMID 8205473 . Corpéchot C, Robel P, Axelson M, Sjövall J, Baulieu EE (1981). "Characterization and measurement of dehydroepiandrosterone sulfate in rat brain" . Proc. Natl. Acad. Sci. U.S.A. 78 (8): 4704–7. DOI :10.1073/pnas.78.8.4704 . PMC 320231 . PMID 6458035 . //www.ncbi.nlm.nih.gov/pmc/articles/PMC320231/ . Reddy D, Rogawski MA (2012). "Neurosteroids — Endogenous regulators of seizure susceptibility and role in the treatment of epilepsy". In: Noebels JL, Avoli M, Rogawski MA, et al., editors. Jasper's Basic Mechanisms of the Epilepsies [Internet]. 4th edition. Bethesda (MD): National Center for Biotechnology Information (US); 2012. Available from: http://www.ncbi.nlm.nih.gov/books/NBK98218/ . PMID 22787590 .
Jonotropni
Agonisti: Konkurentni agonisti :
Aspartat • Glutamat • Homokinolinska kiselina • Ibotenska kiselina • NMDA • Kinolinska kiselina • Tetrazolilglicin ;
Agonisti glicinskog mesta: ACBD • ACPC • ACPD • Alanin • CCG • Cikloserin • DHPG • Fluoroalanin • Glicin • HA-966 • L-687,414 • Milacemid • Sarkozin • Serin • Tetrazolilglicin ;
Agonisti poliaminskog mesta: Akamprosat • Spermidin • Spermin Antagonisti :Konkurentni antagonisti: AP5 (APV) • AP7 • CGP-37849 • CGP-39551 • CGP-39653 • CGP-40116 • CGS-19755 • CPP • LY-233,053 • LY-235,959 • LY-274,614 • MDL-100,453 • Midafotel (d-CPPen) • NPC-12,626 • NPC-17,742 • PBPD • PEAQX • Perzinfotel • PPDA • SDZ-220581 • Selfotel ;
Nekonkurentni antagonisti: ARR-15,896 • Karoverin • Deksanabinol • FPL-12495 • FR-115,427 • Hodgkinsin • Magnezijum • MDL-27,266 • NPS-1506 • Psihotridin • Cink ;
Nekonkurentni blokatori pora: 2-MDP • 3-MeO-PCP • 8A-PDHQ • Amantadin • Aptiganel • ARL-12,495 • ARL-15,896-AR • ARL-16,247 • Budipin • Delucemin • Deksoksadrol • Dekstralorfan • Dieticiklidin • Dizocilpin • Endopsihozin • Esketamin • Etoksadrol • Eticiklidin • Gaciklidin • Ibogain • Indantadol • Ketamin • Ketobemidon • Loperamid • Memantin • Meperidin (Petidin) • Metadon • Metorfan (
Dekstrometorfan ,
Levometorfan )
• Metoksetamin • Milnacipran • Morfanol (
Dekstrorfan ,
Levorfanol )
• NEFA • Nerameksan • Azotsuboksid • Noribogain • Orfenadrin • PCPr • Fenciklamin • Fenciklidin • Propoksifen • Remacemid • Rinhofilin • Riluzol • Rimantadin • Roliciklidin • Sabeluzol • Tenociklidin • Tiletamin • Tramadol • Ksenon ;
Antagonisti glicinskog mesta: ACEA-1021 • ACEA-1328 • ACC • Karisoprodol • CGP-39653 • CKA • DCKA • Felbamat • Gavestinel • GV-196,771 • Kinurenska kiselina • L-689,560 • L-701,324 • Lakosamid • Likostinel • LU-73,068 • MDL-105,519 • Meprobamat • MRZ 2/576 • PNQX • ZD-9379 ;
Antagonisti NR2B podjedinice: Bezonprodil • CO-101,244 (PD-174,494) • CP-101,606 • Eliprodil • Haloperidol • Ifenprodil • Izoksuprin • Nilidrin • Ro8-4304 • Ro25-6981 • Traksoprodil ;
Neklasifikovani/nesortirani antagonisti: Hloroform • Dietil etar • Enfluran • Etanol (Alkohol) • Halotan • Izofluran • Metoksifluran • Toluen • Trihloroetan • Trihloroetanol • Trihloroetilen • Ksilen
Metabotropni
Inhibitori transporta
