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Allopregnanolone

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https://www.readbyqxmd.com/read/29790373/non-clinical-studies-of-progesterone
#1
R Sitruk-Ware
Progesterone is a steroid hormone that is essential for the regulation of reproductive function. Progesterone has been approved for several indications including the treatment of anovulatory menstrual cycles, assisted reproductive technology, contraception during lactation and, when combined with estrogen, for the prevention of endometrial hyperplasia in postmenopausal hormonal therapy. In addition to its role in reproduction, progesterone regulates a number of biologically distinct processes in other tissues, particularly in the nervous system...
May 23, 2018: Climacteric: the Journal of the International Menopause Society
https://www.readbyqxmd.com/read/29773855/the-anxiolytic-like-effects-of-ginsenoside-rg3-on-chronic-unpredictable-stress-in-rats
#2
Jia-Ning Xu, Li-Fang Chen, Jun Su, Zhi-Li Liu, Jie Chen, Qing-Fen Lin, Wei-Dong Mao, Dong Shen
The present study is to evaluate the anxiolytic-like activities underlying ginsenoside Rg3 (GRg3). The anxiolytic-like activities were induced by GRg3 (20 and 40 mg/kg, i.g), evidenced by blocking the decreased time and entries in the open arms in elevated plus maze test and by reversing the increased latency to feed in novelty-suppressed feeding test. In addition, the decreased levels on progesterone, allopregnanolone, serotonin (5-HT) in the prefrontal cortex and hippocampus of chronic unpredictable stress (CUS) were blocked by GRg3 (20 and 40 mg/kg, i...
May 17, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29773519/the-neurosteroid-allopregnanolone-sulfate-inhibits-na-v-1-3-%C3%AE-subunit-containing-voltage-gated-sodium-channels-expressed-in-xenopus-oocytes
#3
Takafumi Horishita, Nobuyuki Yanagihara, Susumu Ueno, Dan Okura, Reiko Horishita, Tomoko Minami, Yuichi Ogata, Yuka Sudo, Yasuhito Uezono, Takashi Kawasaki
The neurosteroid allopregnanolone has potent analgesic effects, and its potential use for neuropathic pain is supported by recent reports. However, the analgesic mechanisms are obscure. The voltage-gated sodium channels (Nav ) α subunit Nav 1.3 is thought to play an essential role in neuropathic pain. Here, we report the effects of allopregnanolone sulfate (APAS) on sodium currents (INa ) in Xenopus oocytes expressing Nav 1.3 with β1 or β3 subunits. APAS suppressed INa of Nav 1.3 with β1 and β3 in a concentration-dependent manner (IC50 values; 75 and 26 μmol/L)...
March 30, 2018: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29761343/role-of-exogenous-progesterone-in-the-treatment-of-men-and-women-with-substance-use-disorders-a-narrative-review
#4
REVIEW
MacKenzie R Peltier, Mehmet Sofuoglu
Substance use disorders (SUDs) remain problematic as many individuals are untreated or do not benefit from the currently available interventions. Thus, there is an urgent need to develop novel pharmacological interventions to treat SUDs. Evidence suggests that the female sex hormone, progesterone, attenuates the craving for and the euphoric effects of drugs of abuse. Research to date has demonstrated that progesterone may modulate responses to drugs of abuse and may have utility as a novel treatment for SUDs...
May 14, 2018: CNS Drugs
https://www.readbyqxmd.com/read/29729249/neurosteroid-allopregnanolone-reduces-ipsilateral-visual-cortex-potentiation-following-unilateral-optic-nerve-injury
#5
Elena G Sergeeva, Claudia Espinosa-Garcia, Fahim Atif, Machelle T Pardue, Donald G Stein
In adult mice with unilateral optic nerve crush injury (ONC), we studied visual response plasticity in the visual cortex following stimulation with sinusoidal grating. We examined visually evoked potentials (VEP) in the primary visual cortex ipsilateral and contralateral to the crushed nerve. We found that unilateral ONC induces enhancement of visual response on the side ipsilateral to the injury that is evoked by visual stimulation to the intact eye. This enhancement was associated with supranormal spatial frequency thresholds in the intact eye when tested using optomotor response...
May 2, 2018: Experimental Neurology
https://www.readbyqxmd.com/read/29727810/ptsd-in-women-is-associated-with-a-block-in-conversion-of-progesterone-to-the-gabaergic-neurosteroids-allopregnanolone-and-pregnanolone-measured-in-plasma
#6
S L Pineles, Y I Nillni, G Pinna, J Irvine, A Webb, K A Arditte Hall, R Hauger, M W Miller, P A Resick, S P Orr, A M Rasmusson
There is a need to identify new and more effective treatments for posttraumatic stress disorder (PTSD). Allopregnanolone and its stereoisomer pregnanolone (together termed ALLO) are metabolites of progesterone that positively and allosterically modulate GABA effects at GABAA receptors, thereby reducing anxiety and depression. Previous research revealed that women with PTSD had low cerebrospinal fluid (CSF) ALLO levels and a low ratio of ALLO to the allopregnanolone precursor 5α-DHP, consistent with deficient activity of the ALLO synthetic enzyme 3α-hydroxysteroid dehydrogenase (3α-HSD)...
April 24, 2018: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/29665216/peak-visual-gamma-frequency-is-modified-across-the-healthy-menstrual-cycle
#7
Rachael L Sumner, Rebecca L McMilllan, Alexander D Shaw, Krish D Singh, Fred Sundram, Suresh D Muthukumaraswamy
Fluctuations in gonadal hormones over the course of the menstrual cycle are known to cause functional brain changes and are thought to modulate changes in the balance of cortical excitation and inhibition. Animal research has shown this occurs primarily via the major metabolite of progesterone, allopregnanolone, and its action as a positive allosteric modulator of the GABAA receptor. Our study used EEG to record gamma oscillations induced in the visual cortex using stationary and moving gratings. Recordings took place during twenty females' mid-luteal phase when progesterone and estradiol are highest, and early follicular phase when progesterone and estradiol are lowest...
April 17, 2018: Human Brain Mapping
https://www.readbyqxmd.com/read/29648595/progesterone-as-a-postnatal-prophylactic-agent-for-encephalopathy-caused-by-prenatal-hypoxic-ischemic-insult
#8
Yoshimasa Kawarai, Hirokazu Tanaka, Tatsuya Kobayashi, Makio Shozu
Brain damage caused by hypoxic ischemic insult during the perinatal period causes hypoxic ischemic encephalopathies (HIEs). Therapeutic hypothermia is indicated for HIE, but since the therapeutic burden is large for its limited therapeutic effectiveness, another strategy is needed. Progesterone (P4) plays a neuroprotective role through the actions of its metabolite, allopregnanolone (Allo), on P4 receptor, GABA (γ-aminobutyric acid)A receptors or both. We examined the therapeutic potential of P4 using a newborn rat model of HIE...
April 10, 2018: Endocrinology
https://www.readbyqxmd.com/read/29604384/allopregnanolone-effects-on-transmission-in-the-brain-stem-solitary-tract-nucleus-nts
#9
Sojin Kim, Sung-Moon Kim, Bermseok Oh, Jihoon Tak, Eunhee Yang, Young-Ho Jin
During pregnancy, the progesterone metabolite, allopregnanolone (ALLO), becomes elevated and has been associated with altered levels within the CNS and resulting changes in GABAA receptor function. Pregnant animals poorly compensate reflexes for decrease in blood pressure during hemorrhage. Previous works suggested that ALLO decreases baroreflex responses by central actions, however, the underlying mechanisms are poorly understood. In this study, we tested ALLO actions on visceral afferent synaptic transmission at second order neurons within medial portions of the nucleus tractus solitarius (NTS) using hindbrain slices from non-pregnant female rats...
March 28, 2018: Neuroscience
https://www.readbyqxmd.com/read/29602830/3-%C3%AE-methyl-neurosteroid-analogs-are-preferential-positive-allosteric-modulators-and-direct-activators-of-extrasynaptic-%C3%AE-subunit-%C3%AE-aminobutyric-acid-type-a-receptors-in-the-hippocampus-dentate-gyrus-subfield
#10
Shu-Hui Chuang, Doodipala Samba Reddy
Neurosteroids are powerful modulators of γ -aminobutyric acid (GABA)-A receptors. Ganaxolone (3 α -hydroxy-3 β -methyl-5 α -pregnan-20-one, GX) and synthetic analogs of the neurosteroid allopregnanolone (AP) are designed to treat epilepsy and related conditions. However, their precise mechanism of action in native neurons remains unclear. Here, we sought to determine the mode of action of GX and its analogs at GABA-A receptors in native hippocampal neurons by analyzing extrasynaptic receptor-mediated tonic currents and synaptic receptor-mediated phasic currents...
June 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29593126/effect-of-the-allopregnanolone-and-allotetrahydrodeoxycorticosteron-on-spike-wave-discharges-in-the-eeg-of-absence-epilepsy-rat-models
#11
Sebahattin Karabulut, Ruslan Bayramov, Keziban Korkmaz Bayramov, Ahmet K Filiz, Ahmet S Taskiran, Ercan Ozdemir
Absence epilepsy is a generalized nonconvulsive type of epilepsy that is characterized by spike-wave discharges (SWD) with a frequency of 2.5-4 Hz in the EEG. The activation of the GABAergic system in central nervous system suppresses convulsive seizures but exacerbates absence seizures. Endogenous neuroactive steroids such as 3α-hydroxy-5α-pregnan-20-one (3α,5α-THPROG; allopregnanolone) and 3α,21-dihydroxy-5α-pregnan-20-one (3α,5α-THDOC, allotetrahydrodeoxycorticosteron) are GABA-A receptor-positive allosteric modulators...
March 2018: General Physiology and Biophysics
https://www.readbyqxmd.com/read/29587349/evaluation-of-two-liver-treatment-strategies-in-a-mouse-model-of-niemann-pick-disease-type-c1
#12
Lynn Ebner, Anne Gläser, Anja Bräuer, Martin Witt, Andreas Wree, Arndt Rolfs, Marcus Frank, Brigitte Vollmar, Angela Kuhla
Niemann-Pick-disease type C1 (NPC1) is an autosomal-recessive cholesterol-storage disorder. Besides other symptoms, NPC1 patients develop liver dysfunction and hepatosplenomegaly. The mechanisms of hepatomegaly and alterations of lipid metabolism-related genes in NPC1 disease are still poorly understood. Here, we used an NPC1 mouse model to study an additive hepatoprotective effect of a combination of 2-hydroxypropyl-β-cyclodextrin (HPβCD), miglustat and allopregnanolone (combination therapy) with the previously established monotherapy using HPβCD...
March 24, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29574659/the-5%C3%AE-reductase-inhibitor-finasteride-exerts-neuroprotection-against-ischemic-brain-injury-in-aged-male-rats
#13
Motoki Tanaka, Takunori Ogaeri, Mikhail Samsonov, Masahiro Sokabe
Progesterone (P4) exerts potent neuroprotection both in young and aged animal models of stroke. The neuroprotection is likely to be mediated by allopregnanolone (ALLO) metabolized from P4 by 5α-reductase, since the neuroprotection is attenuated by the 5α-reductase inhibitor finasteride, which was done only with young animals though. Thus, we do not know the contribution of ALLO to the P4-induced neuroprotection in aged animals. We examined effects of finasteride on the P4-induced neuroprotection in aged (16-18-month-old) male rats subjected to transient focal cerebral ischemia...
March 25, 2018: Translational Stroke Research
https://www.readbyqxmd.com/read/29571173/seizure-freedom-in-patients-with-dravet-syndrome-with-contraceptives-a-case-report-with-two-patients
#14
Jan Lotte, Stefan Grothe, Gerhard Josef Kluger
Dravet syndrome is a rare and malignant epileptic syndrome that is typically resistant to antiepileptic drugs. There is a growing interest in the antiepileptic properties of neurosteroids. Especially progesterone is known to act as an anticonvulsive agent. However, contraceptives that act as orally given neurosteroids often lead to increased seizures in women with epilepsy.We report on two girls with Dravet syndrome, who gained seizure freedom under therapy with contraceptives. The first patient received an oral contraceptive, a combination of an estrogen, and a gestagen, due to hypermenorrhea...
March 23, 2018: Neuropediatrics
https://www.readbyqxmd.com/read/29544630/gaba-a-receptors-mediate-tonic-inhibition-and-neurosteroid-sensitivity-in-the-brain
#15
Doodipala Samba Reddy
Neurosteroids like allopregnanolone (AP) are positive allosteric modulators of synaptic and extrasynaptic GABA-A receptors. AP and related neurosteroids exhibit a greater potency for δ-containing extrasynaptic receptors. The δGABA-A receptors, which are expressed extrasynaptically in the dentate gyrus and other regions, contribute to tonic inhibition, promoting network shunting as well as reducing seizure susceptibility. Levels of endogenous neurosteroids fluctuate with ovarian cycle. Natural and synthetic neurosteroids maximally potentiate tonic inhibition in the hippocampus and provide robust protection against a variety of limbic seizures and status epilepticus...
2018: Vitamins and Hormones
https://www.readbyqxmd.com/read/29543748/allopregnanolone-alters-the-gene-expression-profile-of-human-glioblastoma-cells
#16
Carmen J Zamora-Sánchez, Aylin Del Moral-Morales, Ana M Hernández-Vega, Valeria Hansberg-Pastor, Ivan Salido-Guadarrama, Mauricio Rodríguez-Dorantes, Ignacio Camacho-Arroyo
Glioblastomas (GBM) are the most frequent and aggressive brain tumors. In these malignancies, progesterone (P4) promotes proliferation, migration, and invasion. The P4 metabolite allopregnanolone (3α-THP) similarly promotes cell proliferation in the U87 human GBM cell line. Here, we evaluated global changes in gene expression of U87 cells treated with 3α-THP, P4, and the 5α-reductase inhibitor, finasteride (F). 3α-THP modified the expression of 137 genes, while F changed 90. Besides, both steroids regulated the expression of 69 genes...
March 15, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29492615/gr3027-reversal-of-neurosteroid-induced-gaba-a-receptor-mediated-inhibition-of-human-brain-function-an-allopregnanolone-challenge-study
#17
Maja Johansson, Maria Månsson, Lars-Eric Lins, Bruce Scharschmidt, Magnus Doverskog, Torbjörn Bäckström
RATIONALE: GR3027 is a novel small molecule GABA-A receptor-modulating steroid antagonist, which in non-clinical studies has shown promise for treatment of human disorders due to allosteric over-activation of GABA-A receptors by neurosteroids, such as allopregnanolone. We here studied its safety, pharmacokinetics, and ability to inhibit allopregnanolone effects in humans. METHODS: Safety and pharmacokinetics were studied in healthy adult males receiving ascending single or multiple oral GR3027 vs...
May 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29481795/neurosteroid-regulation-of-gaba-a-receptors-a-role-in-catamenial-epilepsy
#18
Suchitra Joshi, Jaideep Kapur
The female reproductive hormones progesterone and estrogen regulate network excitability. Fluctuations in the circulating levels of these hormones during the menstrual cycle cause frequent seizures during certain phases of the cycle in women with epilepsy. This seizure exacerbation, called catamenial epilepsy, is a dominant form of drug-refractory epilepsy in women of reproductive age. Progesterone, through its neurosteroid derivative allopregnanolone, increases γ-aminobutyric acid type-A receptor (GABAR)-mediated inhibition in the brain and keeps seizures under control...
February 23, 2018: Brain Research
https://www.readbyqxmd.com/read/29477545/neurosteroid-metabolites-of-testosterone-and-progesterone-differentially-inhibit-erk-phosphorylation-induced-by-amyloid-%C3%AE-in-sh-sy5y-cells-and-primary-cortical-neurons
#19
Ari L Mendell, Beryl Y T Chung, Carolyn E Creighton, Bettina E Kalisch, Craig D C Bailey, Neil J MacLusky
Gonadal steroid hormones exert neurotrophic and neuroprotective effects on the brain. Recent work suggests potential neuroprotective roles for the 3α-hydroxy, 5α-reduced metabolites of these hormones. Two such metabolites are 5α-androstane-3α,17β-diol (3α-diol) and 5α-pregnan-3α-ol-20-one (allopregnanolone; Allo), which may contribute to the overall protection conferred by their precursors (testosterone and progesterone, respectively) through mechanisms including potentiation of gamma-aminobutyric acid (GABA)A receptor (GABAA R) activity...
May 1, 2018: Brain Research
https://www.readbyqxmd.com/read/29453777/intramuscular-allopregnanolone-and-ganaxolone-in-a-mouse-model-of-treatment-resistant-status-epilepticus
#20
Dorota Zolkowska, Chun-Yi Wu, Michael A Rogawski
Allopregnanolone (5α-pregnan-3α-ol-20-one) and its synthetic 3β-methyl analog, ganaxolone, are positive allosteric modulators of synaptic and extrasynaptic γ-aminobutyric acid (GABA)A receptors that exhibit antiseizure activity in diverse animal seizure models, including models of status epilepticus (SE). The 2 neuroactive steroids are being investigated as treatments for SE, including as a treatment for SE induced by chemical threat agents. Intramuscular injection is the preferred route of administration in the prehospital treatment of SE...
February 17, 2018: Epilepsia
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