Synthetic neurosteroids on brain protection
Neurosteroids, like allopregnanolone and pregnanolone, are endogenous regulators of neuronal excitability. Inside the brain, they are highly selective and potent modulators of GABAA receptor activity. Their anticonvulsant, anesthetics and anxiolytic properties are useful for the treatments of severa...
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Published in | Neural regeneration research Vol. 10; no. 1; pp. 17 - 21 |
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Main Authors | , |
Format | Journal Article |
Language | English |
Published |
India
Medknow Publications and Media Pvt. Ltd
2015
Medknow Publications & Media Pvt. Ltd Laboratorio de Neurobiología, Instituto de Biología y Medicina Experimental IBYME-C0NICET, Vuelta de 0bligado 2490, C1428ADN Ciudad Autónoma de Buenos Aires, Argentina Medknow Publications & Media Pvt Ltd Wolters Kluwer Medknow Publications |
Subjects | |
Online Access | Get full text |
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Summary: | Neurosteroids, like allopregnanolone and pregnanolone, are endogenous regulators of neuronal excitability. Inside the brain, they are highly selective and potent modulators of GABAA receptor activity. Their anticonvulsant, anesthetics and anxiolytic properties are useful for the treatments of several neurological and psychiatric disorders via reducing the risks of side effects obtained with the commercial drugs. The principal disadvantages of endogenous neurosteroids adminis- tration are their rapid metabolism and their low oral bioavailability. Synthetic steroids analogues with major stability or endogenous neurosteroids stimulation synthesis might constitute prom- ising novel strategies for the treatment of several disorders. Numerous studies indicate that the 3ct-hydroxyl configuration is the key for binding and activity, but modifications in the steroid nucleus may emphasize different pharmacophores. So far, several synthetic steroids have been developed with successful neurosteroid-like effects. In this work, we summarize the properties of various synthetic steroids probed in trials throughout the analysis of several neurosteroids-like actions. |
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Bibliography: | Neurosteroids, like allopregnanolone and pregnanolone, are endogenous regulators of neuronal excitability. Inside the brain, they are highly selective and potent modulators of GABAA receptor activity. Their anticonvulsant, anesthetics and anxiolytic properties are useful for the treatments of several neurological and psychiatric disorders via reducing the risks of side effects obtained with the commercial drugs. The principal disadvantages of endogenous neurosteroids adminis- tration are their rapid metabolism and their low oral bioavailability. Synthetic steroids analogues with major stability or endogenous neurosteroids stimulation synthesis might constitute prom- ising novel strategies for the treatment of several disorders. Numerous studies indicate that the 3ct-hydroxyl configuration is the key for binding and activity, but modifications in the steroid nucleus may emphasize different pharmacophores. So far, several synthetic steroids have been developed with successful neurosteroid-like effects. In this work, we summarize the properties of various synthetic steroids probed in trials throughout the analysis of several neurosteroids-like actions. allopregnanolone; synthetic steroids; GABAA receptor; neuroprotection; cerebral cortex;hippocampus 11-5422/R ObjectType-Article-2 SourceType-Scholarly Journals-1 ObjectType-Feature-3 content type line 23 ObjectType-Review-1 Author contributions: MR was responsible for writing the first draft of the manuscript and contributed to its editing and revision. HC was responsible for the review conception, and contributed to the design of the manuscript, writing and editing. Both authors approved the final version of this review. |
ISSN: | 1673-5374 1876-7958 |
DOI: | 10.4103/1673-5374.150640 |