Neuroaktivni steroid
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] Termin neurosteroid koji je formirao francuski fiziolog Étienne-Émile Baulieu obuhvata steroide koji su sintetisani u mozgu.[3] U kontrastu s njima neuroaktivni steroid se odnose na steroide koje sintetišu endokrine žlezde i koji dospevaju do mozga putem krvotoka.[4] Osim njihovih dejstava na neuronske membranske receptore, neki od ovih steroida modu da utiču na izražvanje gena putem nuklearnih steroidnih hormonskih receptora. Neurosteroidi imaju širok opseg potencijalnih kliničkih primena od sedacije do tretmana epilepsije[5] i traumatičnih moždanih povreda.[6][7] Ganaksolon, sintetički analog endogenog neurosteroida alopregnanolona, se ispituje za moguću primenu u tretmanu epilepsije.[8]
Reference
- ↑ Paul SM, Purdy RH (1992). „Neuroactive steroids” (abstract). FASEB J. 6 (6): 2311–22. PMID 1347506.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
Literatura
- 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.
- 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.
- 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.
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Dialkil-fenoli | |||||||||
CL-218,872 • Eszopiklon • Indiplon • Nekopidem • Pazinaklon • ROD-188 • Saripidem • Suproklon • Suriklon • SX-3228 • U-89843A • U-90042 • Zaleplon • Zolpidem • Zopiklon | |||||||||
Neuroaktivni steroidi |
receptor
Acetilholinski receptor
α1- adrenergički
Selektivni 5-HT2A & α1-adrenergički antagonisti |
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GHB receptor
GHB Tip |
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Oreksinski antagonisti |
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negrupisani
Drugi | 2-Metil-2-butanol • Acekarbromal • Acetofenon • Apronal • Bromidi • Bromizoval • Karbromal • Hloralosa • Klometiazol • Embutramid • Etomidat • Evoksin • Fenadiazol • Gaboksadol • Loreklezol • Mefenoksalon • Sulfonmetan • Trihloroetanol • Triklofos • Valerian • Valnoktamid |
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