Evidence map›Paper›PMID 39113108›Full record

ArticleMolecular brain2024

Determinants of interactions of a novel next-generation gabapentinoid NVA1309 and mirogabalin with the Cavα2δ-1 subunit.

Ivana A Souza, Maria A Gandini, Md Yousof Ali, Franz Kricek, George Skouteris, Gerald W Zamponi

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Molecular brain, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
–field-weighted citation impact
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

2 citing papers in PubMed.

  1. Shaping the Action Potential in Dorsal Root and Trigeminal Ganglia Neurons: Relevance to Pain Mechanisms.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2026
    Review
  2. Review
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

6 authors.

Ivana A SouzaDepartment of Clinical Neurosciences, Cumming School of Medicine, Hotchkiss Brain Institute, Alberta Children's Hospital Research Institute, University of Calgary, Calgary, AB, Canada.
Maria A GandiniDepartment of Clinical Neurosciences, Cumming School of Medicine, Hotchkiss Brain Institute, Alberta Children's Hospital Research Institute, University of Calgary, Calgary, AB, Canada.
Md Yousof AliDepartment of Clinical Neurosciences, Cumming School of Medicine, Hotchkiss Brain Institute, Alberta Children's Hospital Research Institute, University of Calgary, Calgary, AB, Canada.
Franz KricekDepartment of Experimental Neurosciences, Novassay SA, Biopôle, 1066, Epalinges, Switzerland.
George SkouterisDepartment of Experimental Neurosciences, Novassay SA, Biopôle, 1066, Epalinges, Switzerland.
Gerald W ZamponiDepartment of Clinical Neurosciences, Cumming School of Medicine, Hotchkiss Brain Institute, Alberta Children's Hospital Research Institute, University of Calgary, Calgary, AB, Canada. zamponi@ucalgary.ca.ORCID 0000-0002-0644-9066

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

NVA1309 is a non-brain penetrant next-generation gabapentinoid shown to bind Cavα2δ at R243 within a triple Arginine motif forming the binding site for gabapentin and pregabalin. In this study we have compared the effects of NVA1309 with Mirogabalin, a gabapentinoid drug with higher affinity for the voltage-gated calcium channel subunit Cavα2δ-1 than pregabalin which is approved for post-herpetic neuralgia in Japan, Korea and Taiwan. Both NVA1309 and mirogabalin inhibit Cav2.2 currents in vitro and decrease Cav2.2 plasma membrane expression with higher efficacy than pregabalin. Mutagenesis of the classical binding residue arginine R243 and the newly identified binding residue lysine K615 reverse the effect of mirogabalin on Cav2.2 current, but not that of NVA1309.

Indexed as

GabapentinAnimalsBridged Bicyclo CompoundsCalcium ChannelsCalcium Channels, N-TypeCell Membranegamma-Aminobutyric AcidHEK293 CellsHumansPregabalinProtein BindingProtein SubunitsBridged Bicyclo CompoundsCalcium ChannelsCalcium Channels, N-TypeGabapentingamma-Aminobutyric AcidmirogabalinPregabalinProtein SubunitsCalcium channelCavα2δGabapentinoidsMirogabalinNeuropathic pain

Identifiers

PMID39113108
PMCPMC11308618

What OpenQuestion holds

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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.