Allopregnanolone
Mostrando 1-12 de 16 artigos, teses e dissertações.
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1. Estrous cycle and stress: influence of progesterone on the female brain
The female brain operates in a constantly changing chemical milieu caused by cyclical changes in gonadal hormones during the estrous cycle (menstrual cycle in women). Such hormones are highly lipophilic and pass readily from the plasma to the brain where they can influence neuronal function. It is becoming clear that the rapid reduction in peripheral circula
Brazilian Journal of Medical and Biological Research. Publicado em: 2012-04
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2. Evaluation of the tolerability, hormonal profile and endometrial effects of allopregnanolone, administered in the form of a gel by the vaginal route to postmenopausal women on oral estrogen therapy: phase II study. / Avaliação da Tolerabilidade, do Perfil Hormonal e dos Efeitos Endometrais Secundário à Administração Vaginal do Gel e de Allopregnanolona à Mulheres na Pós-Menopausa, em Uso de Estrogenioterapia: Estudo Fase 2.
Objectives: To evaluate the tolerability and to obtain preliminary data regarding the endometrial effects of allopregnanolone, administered in the form of a gel by the vaginal route to postmenopausal women on oral estrogen therapy, along two cycles of treatment, and to obtain preliminary data about the effect of the drug under study on serum gonadotropin, es
Publicado em: 2000
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3. Selective serotonin reuptake inhibitors directly alter activity of neurosteroidogenic enzymes
The neurosteroid 3α-hydroxysteroid-5α-pregnan-20-one (allopregnanolone) acts as a positive allosteric modulator of γ-aminobutyric acid at γ-aminobutyric acid type A receptors and hence is a powerful anxiolytic, anticonvulsant, and anesthetic agent. Allopregnanolone is synthesized from progesterone by reduction to 5α-dihydroprogesterone, mediated by 5α-
The National Academy of Sciences.
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4. Stress-induced elevations of gamma-aminobutyric acid type A receptor-active steroids in the rat brain.
A 3 alpha-hydroxy A-ring-reduced metabolite of progesterone, 3 alpha-hydroxy-5 alpha-pregnan-20-one (allopregnanolone), and one of deoxycorticosterone (DOC), 3 alpha,21-dihydroxy-5 alpha-pregnan-20- one (allotetrahydroDOC), are among the most potent known ligands of gamma-aminobutyric acid (GABA) receptors designated GABAA in the central nervous system. With
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5. Modulation of GABAA receptor-mediated IPSCs by neuroactive steroids in a rat hypothalamo-hypophyseal coculture model.
1. We have used the whole-cell configuration of the patch-clamp technique to investigate the effects of neuroactive steroids on GABAA receptor-mediated synaptic transmission between rat hypothalamic neurones and pituitary intermediate lobe (IL) cells grown in coculture. In order to discriminate between possible pre- and postsynaptic sites of action, the effe
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6. In socially isolated mice, the reversal of brain allopregnanolone down-regulation mediates the anti-aggressive action of fluoxetine
Social isolation (SI) of male mice lasting >4 weeks is associated with aggression toward intruders and a down-regulation of brain allopregnanolone (Allo) content. SI of female mice fails to down-regulate brain Allo content or to induce aggressiveness. Fluoxetine (Prozac in clinical use) is an S- and R-fluoxetine (FLX) mixture, which in mammals is metabolized
The National Academy of Sciences.
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7. Changes in brain testosterone and allopregnanolone biosynthesis elicit aggressive behavior
In addition to an action on metabolism, anabolic/androgenic steroids also increase sex drive and mental acuity. If abused, such steroids can cause irritability, impulsive aggression, and signs of major depression [Pearson, H. (2004) Nature 431, 500-501], but the mechanisms that produce these symptoms are unknown. The present study investigates behavioral and
National Academy of Sciences.
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8. Genetic essential tremor in γ-aminobutyric acidA receptor α1 subunit knockout mice
Essential tremor is the most common movement disorder and has an unknown etiology. Here we report that γ-aminobutyric acidA (GABAA) receptor α1–/– mice exhibit postural and kinetic tremor and motor incoordination that is characteristic of essential tremor disease. We tested mice with essential-like tremor using current drug therapies that alleviate sym
American Society for Clinical Investigation.
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9. Role of brain allopregnanolone in the plasticity of γ-aminobutyric acid type A receptor in rat brain during pregnancy and after delivery
The relation between changes in brain and plasma concentrations of neurosteroids and the function and structure of γ-aminobutyric acid type A (GABAA) receptors in the brain during pregnancy and after delivery was investigated in rats. In contrast with plasma, where all steroids increased in parallel, the kinetics of changes in the cerebrocortical concentrat
The National Academy of Sciences.
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10. Dehydroepiandrosterone and allopregnanolone protect sympathoadrenal medulla cells against apoptosis via antiapoptotic Bcl-2 proteins
The neuroactive steroids dehydroepiandrosterone (DHEA), its sulfate ester DHEA sulfate (DHEAS), and allopregnanolone (Allo), produced by the CNS and the adrenals, appear to exert a protective effect in hippocampal and cortical neuron ischemia- and excitotoxicity-induced injury. We hypothesized that they may also play a protective role on the adrenal medulla,
National Academy of Sciences.
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11. Brain 5α-dihydroprogesterone and allopregnanolone synthesis in a mouse model of protracted social isolation
Allopregnanolone (ALLO), is a brain endogenous neurosteroid that binds with high affinity to γ-aminobutyric acid type A (GABAA) receptors and positively modulates the action of GABA at these receptors. Unlike ALLO, 5α-dihydroprogesterone (5α-DHP) binds with high affinity to intracellular progesterone receptors that regulate DNA transcription. To inv
The National Academy of Sciences.
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12. Fluoxetine and norfluoxetine stereospecifically facilitate pentobarbital sedation by increasing neurosteroids
Mice housed in social isolation exhibit a decreased response to γ-aminobutyric acid-mimetic drugs [i.e., pentobarbital (PTB)] associated with a down-regulation of telencephalic allopregnanolone (Allo) levels. In these mice, the PTB-induced loss of righting reflex is greatly reduced. Fluoxetine (FLX) and norfluoxetine (NFLX) stereospecifically reverse the ef
National Academy of Sciences.