Last update 01 Nov 2024

GABRA2 x GABRD

Last update 01 Nov 2024

Basic Info

Related Targets

GABRA2GABRD

Drugs associated with GABRA2 x GABRD

Cyclobutyl gababutin

Target

GABRA2 x GABRD

Mechanism

GABRA2 modulators [+1]

Active Org.-

Originator Org.

Pfizer Inc.

Active Indication-

Inactive Indication

Neuralgia

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with GABRA2 x GABRD

100 Translational Medicine associated with GABRA2 x GABRD

0 Patents (Medical) associated with GABRA2 x GABRD

Literatures (Medical) associated with GABRA2 x GABRD

01 Dec 2019·Behavioural Brain ResearchQ3 · PSYCHOLOGY

GABAa receptor subunits expression in silver catfish (Rhamdia quelen) brain and its modulation by Nectandra grandiflora Nees essential oil and isolated compounds

Q3 · PSYCHOLOGY

Article

Author: Rodrigues, Patrícia ; Baldisserotto, Bernardo ; Garlet, Quelen I ; Martinez-Rodríguez, Gonzalo ; Souza, Carine F ; Heinzmann, Berta M ; Descovi, Sharine N

Studies using silver catfish (Rhamdia quelen) as experimental models are often applied to screen essential oils (EO) with GABAergic-mediated effects. However, the expression of GABAa receptors in the silver catfish brain remains unknown. Thus, we assessed whether silver catfish express GABAa receptor subunits associated with sedation/anesthetic process and/or neurological diseases. Additionally, we evaluated the brain expression of GABAa receptor subunits in fish sedated with Nectandra grandiflora EO and its isolated compounds, the fish anesthetic (+)-dehydrofukinone (DHF), and dehydrofukinone epoxide (DFX), eremophil-11-en-10-ol (ERM) and selin-11-en-4-α-ol (SEL), which have GABAa-mediated anxiolytic-like effects in mice. The expression of the subunits gabra1, gabra2, gabra3, gabrb1, gabrd and gabrg2 in the silver catfish brain were assessed after a 24h-sedation bath by real time PCR. Since qPCR data rarely describes mechanisms of action, which are usually found through interactions with receptors, we also performed an antagonist-driven experiment using flumazenil (FMZ). Real-time PCR detected the mRNA expression of all targeted genes in R. quelen brain. The expression of gabra1 was decreased in fish sedated with ERM; EO increased gabra2, gabra3, gabrb1 and gabrg2 expression; SEL increased gabrb1, gabrd and gabrg2 expression. EO and compounds DFX, SEL and ERM induced sustained sedation in fish and FMZ-bath prompted the recovery from ERM- and DFX-induced sedation. Our results suggest that the EO, SEL, ERM and DFX sedative effects involve interaction with the GABAergic system. Our findings support the use of the silver catfish as robust and reliable experimental model to evaluate the efficacy of drugs with putative GABAergic-mediated effects.

01 Dec 2014·Balkan Journal of Medical GeneticsQ4 · MEDICINE

Genome-Wide Methylation Profiling of Schizophrenia

Q4 · MEDICINE

ArticleOA

Author: Toncheva, D. ; Staneva, R. ; Milanova, V. ; Hadjidekova, S. ; Rukova, B. ; Stamenov, G.

Abstract Schizophrenia is one of the major psychiatric disorders. It is a disorder of complex inheritance, involving both heritable and environmental factors. DNA methylation is an inheritable epigenetic modification that stably alters gene expression. We reasoned that genetic modifications that are a result of environmental stimuli could also make a contribution. We have performed 26 high-resolution genomewide methylation array analyses to determine the methylation status of 27,627 CpG islands and compared the data between patients and healthy controls. Methylation profiles of DNAs were analyzed in six pools: 220 schizophrenia patients; 220 age-matched healthy controls; 110 female schizophrenia patients; 110 age-matched healthy females; 110 male schizophrenia patients; 110 age-matched healthy males. We also investigated the methylation status of 20 individual patient DNA samples (eight females and 12 males. We found significant differences in the methylation profile between schizophrenia and control DNA pools. We found new candidate genes that principally participate in apoptosis, synaptic transmission and nervous system development (GABRA2, LIN7B, CASP3). Methylation profiles differed between the genders. In females, the most important genes participate in apoptosis and synaptic transmission (XIAP, GABRD, OXT, KRT7), whereas in the males, the implicated genes in the molecular pathology of the disease were DHX37, MAP2K2, FNDC4 and GIPC1. Data from the individual methylation analyses confirmed, the gender-specific pools results. Our data revealed major differences in methylation profiles between schizophrenia patients and controls and between male and female patients. The dysregulated activity of the candidate genes could play a role in schizophrenia pathogenesis.

01 Nov 2014·American Journal of Medical Genetics Part AQ3 · BIOLOGY

A novel variant in GABRB2 associated with intellectual disability and epilepsy

Q3 · BIOLOGY

Article

Author: Cohen, Julie ; McKnight, Dianalee ; Butler, Elizabeth ; Pevsner, Jonathan ; Johnston, Michael ; Aradhya, Swaroop ; Fatemi, Ali ; Srivastava, Siddharth

The γ‐aminobutyric acid type A (GABAA) receptor is one of the three main classes of receptors activated by GABA, the principal inhibitory neurotransmitter in the central nervous system. Mutations in genes encoding various subunits of this receptor (GABRA1, GABRA2, GABRA4, GABRA5, GABRA6, GABRB1, GABRB3, GABRG1, GABRG2, GABRG3, and GABRD) are implicated in a number of neurological and developmental disorders, including epilepsy and autism. To date, no human genetics studies have implicated mutations in GABRB2, encoding the β2 subunit of the GABAA receptor, with neurodevelopmental disorders. Here we present a 12‐year‐old girl with intellectual disability and epilepsy, who was discovered by whole exome sequencing to have a de novo heterozygous missense variant in exon 4 of GABRB2 (c.236T > C; p.M79T). This variant is likely pathogenic, based on in silico analyses, as well as the fact that it results in the non‐conservative substitution of a non‐polar amino acid with a polar amino acid at a position that is evolutionarily conserved across multiple species. Our findings underscore the need for further investigation into the mechanisms by which mutations in GABRB2 contribute to neurological and developmental dysfunction. © 2014 Wiley Periodicals, Inc.

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