3β-Methyl-Neurosteroid Analogs Are Preferential Positive Allosteric Modulators and Direct Activators of Extrasynaptic δ-Subunit γ-Aminobutyric Acid Type A Receptors in the Hippocampus Dentate Gyrus Subfield. (Q54981484)

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English	3β-Methyl-Neurosteroid Analogs Are Preferential Positive Allosteric Modulators and Direct Activators of Extrasynaptic δ-Subunit γ-Aminobutyric Acid Type A Receptors in the Hippocampus Dentate Gyrus Subfield.	scientific article

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29602830 AND SRC:MED&resulttype=core&format=json

22 March 2020

3β-Methyl-Neurosteroid Analogs Are Preferential Positive Allosteric Modulators and Direct Activators of Extrasynaptic δ-Subunit γ-Aminobutyric Acid Type A Receptors in the Hippocampus Dentate Gyrus Subfield (English)

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22 March 2020

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22 March 2020

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22 March 2020

author name string

Doodipala Samba Reddy

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30 June 2019

http://europepmc.org/abstract/PMC/8631194

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30 March 2018

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22 March 2020

Journal of Pharmacology and Experimental Therapeutics

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22 March 2020

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22 March 2020

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22 March 2020

583-601

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:29602830 AND SRC:MED&resulttype=core&format=json

22 March 2020

Neurosteroids act on recombinant human GABAA receptors

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

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Experimental models of temporal lobe epilepsy: new insights from the study of kindling and synaptic reorganization

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

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Anticonvulsant profile of the progesterone metabolite 5 alpha-pregnan-3 alpha-ol-20-one

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

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Structure-activity relationships for steroid interaction with the gamma-aminobutyric acidA receptor complex

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

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Isolation of neurons suitable for patch-clamping from adult mammalian central nervous systems

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

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Modification of seizure activity by electrical stimulation. II. Motor seizure

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

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Anticonvulsant drugs and their antagonism of kindled amygdaloid seizures in rats

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

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Anticonvulsant activity of neurosteroids: correlation with gamma-aminobutyric acid-evoked chloride current potentiation

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

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Progesterone receptor-mediated effects of neuroactive steroids

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

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A putative receptor for neurosteroids on the GABAA receptor complex: the pharmacological properties and therapeutic potential of epalons

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

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Modulation of amino acid-gated ion channels by protein phosphorylation

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

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Ligand-gated ion channel subunit partnerships: GABAA receptor alpha6 subunit gene inactivation inhibits delta subunit expression.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

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3 alpha-Hydroxy-3 beta-(phenylethynyl)-5 beta-pregnan-20-ones: synthesis and pharmacological activity of neuroactive steroids with high affinity for GABAA receptors

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Characterization of the anticonvulsant properties of ganaxolone (CCD 1042; 3alpha-hydroxy-3beta-methyl-5alpha-pregnan-20-one), a selective, high-affinity, steroid modulator of the gamma-aminobutyric acid(A) receptor

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

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Neuroactive steroids protect against pilocarpine- and kainic acid-induced limbic seizures and status epilepticus in mice

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

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Effects of PKC activation and receptor desensitization on neurosteroid modulation of GABAA receptors

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Initial human experience with ganaxolone, a neuroactive steroid with antiepileptic activity

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Adjacent phosphorylation sites on GABAA receptor beta subunits determine regulation by cAMP-dependent protein kinase

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Attenuated sensitivity to neuroactive steroids in gamma-aminobutyrate type A receptor delta subunit knockout mice.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

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Acute and chronic effects of the synthetic neuroactive steroid, ganaxolone, against the convulsive and lethal effects of pentylenetetrazol in seizure-kindled mice: comparison with diazepam and valproate

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Neurosteroid modulation of GABA IPSCs is phosphorylation dependent.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Enantioselectivity of pregnanolone-induced gamma-aminobutyric acid(A) receptor modulation and anesthesia

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Effect of ganaxolone on flurothyl seizures in developing rats

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

GABAA receptor phosphorylation and functional modulation in cortical neurons by a protein kinase C-dependent pathway.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Assessment of ganaxolone's anticonvulsant activity using a randomized, double-blind, presurgical trial design. Ganaxolone Presurgical Study Group.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

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Ganaxolone for treating intractable infantile spasms: a multicenter, open-label, add-on trial

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

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Chronic treatment with the neuroactive steroid ganaxolone in the rat induces anticonvulsant tolerance to diazepam but not to itself

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Generating diversity at GABAergic synapses

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Enhanced anticonvulsant activity of neuroactive steroids in a rat model of catamenial epilepsy.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Enhanced neurosteroid potentiation of ternary GABA(A) receptors containing the delta subunit.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

GABA(A) receptor changes in delta subunit-deficient mice: altered expression of alpha4 and gamma2 subunits in the forebrain

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

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Stress-induced deoxycorticosterone-derived neurosteroids modulate GABA(A) receptor function and seizure susceptibility.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Behavior and physiology of mice lacking the GABAA-receptor delta subunit

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Pharmacological characterization of a novel cell line expressing human alpha(4)beta(3)delta GABA(A) receptors

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Slow phases of GABA(A) receptor desensitization: structural determinants and possible relevance for synaptic function

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

GABA(A) receptor delta subunit deletion prevents neurosteroid modulation of inhibitory synaptic currents in cerebellar neurons.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Intact synaptic GABAergic inhibition and altered neurosteroid modulation of thalamic relay neurons in mice lacking delta subunit.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Reduced inhibition and sensitivity to neurosteroids in hippocampus of mice lacking the GABA(A) receptor delta subunit

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Protective efficacy of neuroactive steroids against cocaine kindled-seizures in mice

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Phosphorylation influences neurosteroid modulation of synaptic GABAA receptors in rat CA1 and dentate gyrus neurones

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Neuroactive steroids reduce neuronal excitability by selectively enhancing tonic inhibition mediated by delta subunit-containing GABAA receptors

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Neurosteroids shift partial agonist activation of GABA(A) receptor channels from low- to high-efficacy gating patterns.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Anticonvulsant activity of progesterone and neurosteroids in progesterone receptor knockout mice.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Allopregnanolone analogs that positively modulate GABA receptors protect against partial seizures induced by 6-Hz electrical stimulation in mice

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Neurosteroid binding sites on GABA(A) receptors

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Clinical evaluation of ganaxolone in pediatric and adolescent patients with refractory epilepsy

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Neurosteroid modulation of GABAA receptors: molecular determinants and significance in health and disease

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

The influence of neuroactive steroid lipophilicity on GABAA receptor modulation: evidence for a low-affinity interaction

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Ganaxolone suppression of behavioral and electrographic seizures in the mouse amygdala kindling model

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

The testosterone-derived neurosteroid androstanediol is a positive allosteric modulator of GABAA receptors

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Disease-modifying activity of progesterone in the hippocampus kindling model of epileptogenesis

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Protein kinase C phosphorylation regulates membrane insertion of GABAA receptor subtypes that mediate tonic inhibition.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Development and persistence of limbic epileptogenesis are impaired in mice lacking progesterone receptors

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Profound desensitization by ambient GABA limits activation of δ-containing GABAA receptors during spillover

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

A mouse kindling model of perimenstrual catamenial epilepsy

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Activity-dependent phosphorylation of GABAA receptors regulates receptor insertion and tonic current

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Estrous cycle regulation of extrasynaptic δ-containing GABA(A) receptor-mediated tonic inhibition and limbic epileptogenesis

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Neuroactive steroids for the treatment of status epilepticus

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Neurosteroid interactions with synaptic and extrasynaptic GABA(A) receptors: regulation of subunit plasticity, phasic and tonic inhibition, and neuronal network excitability

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Neurosteroid analogues. 18. Structure-activity studies of ent-steroid potentiators of γ-aminobutyric acid type A receptors and comparison of their activities with those of alphaxalone and allopregnanolone.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Neurosteroids promote phosphorylation and membrane insertion of extrasynaptic GABAA receptors

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Phosphorylation of GABAA receptors influences receptor trafficking and neurosteroid actions

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Altered expression of δGABAA receptors in health and disease

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Modulation of neurosteroid potentiation by protein kinases at synaptic- and extrasynaptic-type GABAA receptors

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Perimenstrual-like hormonal regulation of extrasynaptic δ-containing GABAA receptors mediating tonic inhibition and neurosteroid sensitivity.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Progress report on new antiepileptic drugs: A summary of the Twelfth Eilat Conference (EILAT XII).

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Antiseizure Activity of Midazolam in Mice Lacking δ-Subunit Extrasynaptic GABA(A) Receptors

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

The GABAA receptor is an FMRP target with therapeutic potential in fragile X syndrome.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Neurosteroid Structure-Activity Relationships for Functional Activation of Extrasynaptic δGABA(A) Receptors.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Catamenial Epilepsy: Discovery of an Extrasynaptic Molecular Mechanism for Targeted Therapy

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Clinical Potential of Neurosteroids for CNS Disorders.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Neurosteroids for the potential protection of humans against organophosphate toxicity.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Zinc Selectively Blocks Neurosteroid-Sensitive Extrasynaptic δGABAA Receptors in the Hippocampus.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Endogenous and synthetic neuroactive steroids evoke sustained increases in the efficacy of GABAergic inhibition via a protein kinase C-dependent mechanism.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

PR-independent neurosteroid regulation of α2-GABA-A receptors in the hippocampus subfields.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Novel therapeutic approaches for disease-modification of epileptogenesis for curing epilepsy.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Randomized, double-blind, placebo-controlled phase 2 study of ganaxolone as add-on therapy in adults with uncontrolled partial-onset seizures

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Catamenial-like seizure exacerbation in mice with targeted ablation of extrasynaptic δGABA-a receptors in the brain.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

A resurging boom in new drugs for epilepsy and brain disorders.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Genetic and Molecular Regulation of Extrasynaptic GABA-A Receptors in the Brain: Therapeutic Insights for Epilepsy.

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

GABA-A Receptors Mediate Tonic Inhibition and Neurosteroid Sensitivity in the Brain

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Role of β2/3-specific GABA-A receptor isoforms in the development of hippocampus kindling epileptogenesis

1 reference

https://pubmed.ncbi.nlm.nih.gov/29602830

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

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10.1124/JPET.117.246660

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22 March 2020

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22 March 2020

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