Evidence map›Paper›PMID 32248400›Full record

ArticleNeurochemical research2020

Pharmacological Characterization of a Betaine/GABA Transporter 1 (BGT1) Inhibitor Displaying an Unusual Biphasic Inhibition Profile and Anti-seizure Effects.

Maria E K Lie, Stefanie Kickinger, Jonas Skovgaard-Petersen, Gerhard F Ecker, Rasmus P Clausen, Arne Schousboe, H Steve White, Petrine Wellendorph

Open access · hybridAbstract read
In one paragraph

Article in Neurochemical research, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
0.6field-weighted citation impact, top 39% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

6 citing papers in PubMed, 10 citations in OpenAlex.

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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

8 authors at 3 institutions in 3 countries.

Maria E K LieDepartment of Drug Design and Pharmacology, University of Copenhagen, Copenhagen, Denmark. maria.lie@sund.ku.dk.ORCID http://orcid.org/0000-0002-1947-9125
Stefanie KickingerDepartment of Pharmaceutical Chemistry, University of Vienna, Vienna, Austria.ORCID http://orcid.org/0000-0003-1640-7940
Jonas Skovgaard-PetersenDepartment of Drug Design and Pharmacology, University of Copenhagen, Copenhagen, Denmark.
Gerhard F EckerDepartment of Pharmaceutical Chemistry, University of Vienna, Vienna, Austria.ORCID http://orcid.org/0000-0003-4209-6883
Rasmus P ClausenDepartment of Drug Design and Pharmacology, University of Copenhagen, Copenhagen, Denmark.ORCID http://orcid.org/0000-0001-9466-9431
Arne SchousboeDepartment of Drug Design and Pharmacology, University of Copenhagen, Copenhagen, Denmark.ORCID http://orcid.org/0000-0001-9600-402X
H Steve WhiteDepartment of Pharmacy, University of Washington, Washington, USA.ORCID http://orcid.org/0000-0003-4550-4408
Petrine WellendorphDepartment of Drug Design and Pharmacology, University of Copenhagen, Copenhagen, Denmark.ORCID http://orcid.org/0000-0002-5455-8013
University of Copenhagen · DKUniversity of Vienna · ATUniversity of Washington · US

Funding

Austrian Science Fund (AT) W1232Austrian Science Fund FWF W 1232Lundbeckfonden (DK) R118-A11564
6 · The paper itself

Abstract

Focal epileptic seizures can in some patients be managed by inhibiting γ-aminobutyric acid (GABA) uptake via the GABA transporter 1 (GAT1) using tiagabine (Gabitril®). Synergistic anti-seizure effects achieved by inhibition of both GAT1 and the betaine/GABA transporter (BGT1) by tiagabine and EF1502, compared to tiagabine alone, suggest BGT1 as a target in epilepsy. Yet, selective BGT1 inhibitors are needed for validation of this hypothesis. In that search, a series of BGT1 inhibitors typified by (1R,2S)-2-((4,4-bis(3-methylthiophen-2-yl)but-3-en-yl)(methyl)amino)cyclohexanecarboxylic acid (SBV2-114) was developed. A thorough pharmacological characterization of SBV2-114 using a cell-based [

Indexed as

Acoustic StimulationAnimalsAnticonvulsantsCHO CellsCricetulusEpilepsy, ReflexGABA Plasma Membrane Transport ProteinsHEK293 CellsHumansMaleMiceMice, TransgenicProtein BindingProtein Structure, SecondarySeizuresTreatment OutcomeAnticonvulsantsGABA Plasma Membrane Transport ProteinsSlc6a12 protein, mouseEpilepsyGABA uptakeGAT1Homology modellingQ299L

Identifiers

PMID32248400
PMCPMC7297817
OpenAlexW3014146330

What OpenQuestion holds

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LicenceCC BY
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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.