Compounds that affect neuronal excitability through modulation of specific ionotropic receptors
Zuranolone, an example of a neurosteroid, used for the treatment of postpartum depression
Neurosteroids, also known as neuroactive steroids, are endogenous or exogenous steroids that rapidly alter neuronal excitability through interaction with ligand-gated ion channels and other cell surface receptors.[1][2] The term neurosteroid was coined by the French physiologist Étienne-Émile Baulieu and refers to steroids synthesized in the brain.[3][4] The term, neuroactive steroid refers to steroids that can be synthesized in the brain, or are synthesized by an endocrine gland, that then reach the brain through the bloodstream and have effects on brain function.[5] The term neuroactive steroids was first coined in 1992 by Steven Paul and Robert Purdy. In addition to their actions on neuronal membrane receptors, some of these steroids may also exert effects on gene expression via nuclear steroid hormone receptors. Neurosteroids have a wide range of potential clinical applications from sedation to treatment of epilepsy[6] and traumatic brain injury.[7][8] Ganaxolone, a synthetic analog of the endogenous neurosteroid allopregnanolone, is under investigation for the treatment of epilepsy.[9]
^Lan NC, Gee KW (December 1994). "Neuroactive steroid actions at the GABAA receptor". Hormones and Behavior. 28 (4): 537–44. doi:10.1006/hbeh.1994.1052. PMID 7729823. S2CID 40697424.
^Reddy DS (2010). "Neurosteroids". Sex Differences in the Human Brain, their Underpinnings and Implications. Progress in Brain Research. Vol. 186. pp. 113–37. doi:10.1016/B978-0-444-53630-3.00008-7. ISBN 9780444536303. PMC 3139029. PMID 21094889.
^Reddy DS, 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. (eds.). Jasper's Basic Mechanisms of the Epilepsies [Internet]. 4th edition. Bethesda (MD): National Center for Biotechnology Information (US). National Center for Biotechnology Information (US). PMID 22787590.
^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". The Journal of Neuroscience. 31 (45): 16056–63. doi:10.1523/JNEUROSCI.4097-11.2011. PMC 3245715. PMID 22072656.
^Cite error: The named reference pmid19332335 was invoked but never defined (see the help page).
^Morrow AL (October 2007). "Recent developments in the significance and therapeutic relevance of neuroactive steroids--Introduction to the special issue". Pharmacology & Therapeutics. 116 (1): 1–6. doi:10.1016/j.pharmthera.2007.04.003. PMC 2047816. PMID 17531324.
^Dubrovsky BO (February 2005). "Steroids, neuroactive steroids and neurosteroids in psychopathology". Progress in Neuro-Psychopharmacology & Biological Psychiatry. 29 (2): 169–92. doi:10.1016/j.pnpbp.2004.11.001. PMID 15694225. S2CID 36197603.
^Bialer M, Johannessen SI, Levy RH, Perucca E, Tomson T, White HS (January 2013). "Progress report on new antiepileptic drugs: a summary of the Eleventh Eilat Conference (EILAT XI)". Epilepsy Research. 103 (1): 2–30. doi:10.1016/j.eplepsyres.2012.10.001. PMID 23219031.
Neurosteroids, also known as neuroactive steroids, are endogenous or exogenous steroids that rapidly alter neuronal excitability through interaction with...
This is a list of neurosteroids, or natural and synthetic steroids that are active on the mammalian nervous system through receptors other than steroid...
binding to an array of nuclear and cell surface receptors, and acting as a neurosteroid and modulator of neurotrophic factor receptors. In the United States...
brain, complicating drug discovery. For example, the binding site of neurosteroids in the GABAA receptor is not known and barbiturates bind at a beta subunit...
Allopregnanolone is a naturally occurring neurosteroid which is made in the body from the hormone progesterone. As a medication, allopregnanolone is referred...
than DHEA. The steroid is hormonally inert and is instead an important neurosteroid and neurotrophin. Similarly to other conjugated steroids, DHEA-S is devoid...
corticosteroids (glucocorticoids and mineralocorticoids), as well as neurosteroids, from cholesterol. Steroidogenic enzymes are most highly expressed in...
addition, pregnenolone is biologically active in its own right, acting as a neurosteroid. In addition to its role as a natural hormone, pregnenolone has been...
(5α-androstane-3α,17β-diol) – an endogenous androgen, estrogen, and neurosteroid 3β-Androstanediol (5α-androstane-3β,17β-diol) – an endogenous estrogen...
or 3α-hydroxy-5α-androstan-17-one, is an endogenous steroid hormone, neurosteroid, and putative pheromone. It is a weak androgen with a potency that is...
methaqualone binding site is distinct from the benzodiazepine, barbiturate, and neurosteroid binding sites on the GABA-A receptor complex, and it may partially overlap...
Norethisterone, also known as norethindrone and sold under many brand names, is a progestin medication used in birth control pills, menopausal hormone...
Alexaki VI, Avlonitis N, Pediaditakis I, Efstathopoulos P, et al. (2011). "Neurosteroid dehydroepiandrosterone interacts with nerve growth factor (NGF) receptors...
or 3α-androstenol), is a 16-androstene class steroidal pheromone and neurosteroid in humans and other mammals, notably pigs. It possesses a characteristic...
nasopharyngitis, and urinary tract infection. An orally active inhibitory pregnane neurosteroid, zuranolone acts as a positive allosteric modulator of the GABAA receptor...
on GABAAR subtype-dependent extracellular domain sites. Alcohols and neurosteroids, among other general anesthetics, act at GABAAR subunit-interface transmembrane...
corticosteroids, and plays an important role in brain function as a neurosteroid. In addition to its role as a natural hormone, progesterone is also used...
Pregnenolone sulfate (PS, PREGS) is an endogenous excitatory neurosteroid that is synthesized from pregnenolone. It is known to have cognitive and memory-enhancing...
progesterone. Progesterone also has antimineralocorticoid and inhibitory neurosteroid activity, whereas it appears to have little or no glucocorticoid or antiandrogenic...
progesterone. Progesterone also has antimineralocorticoid and inhibitory neurosteroid activity, whereas it appears to have little or no glucocorticoid or antiandrogenic...
mineralocorticoids List of neurosteroids – excitatory, inhibitory, mixed, neurotrophic, antineurotrophic, and other neurosteroids, as well as pheromones and...
Medicine, could be neurosteroids that are essential and active while the foal is in utero. Foals receive stimulation of certain neurosteroids that keep them...
also referred to as allotetrahydrocorticosterone, is an endogenous neurosteroid. It is synthesized from the adrenal hormone deoxycorticosterone by the...
that inhibits the production of endogenous neurosteroids. Neurosteroids include the excitatory neurosteroids pregnenolone sulfate, dehydroepiandrosterone...
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