Evidence map›Paper›PMID 28098336›Full record

ArticleEpilepsia2017

Preclinical evaluation of intravenous NAX 810-2, a novel GalR2-preferring analog, for anticonvulsant efficacy and pharmacokinetics.

Cameron S Metcalf, Brian D Klein, Daniel R McDougle, Liuyin Zhang, Dan Kaufmann, Grzegorz Bulaj, H Steve White

Open access · greenAbstract read
In one paragraph

Article in Epilepsia, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed
1.3field-weighted citation impact, top 24% 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

8 citing papers in PubMed, 19 citations in OpenAlex.

  1. Article
  2. Article
  3. Insights into Potential Targets for Therapeutic Intervention in Epilepsy.International journal of molecular sciences · 2020
    Review
  4. Review
  5. Article
  6. Article
  7. Article
  8. Article
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

7 authors at 1 institution in 1 country.

Cameron S MetcalfDepartment of Pharmacology & Toxicology, College of Pharmacy, University of Utah, Salt Lake City, Utah, U.S.A.
Brian D KleinDepartment of Pharmacology & Toxicology, College of Pharmacy, University of Utah, Salt Lake City, Utah, U.S.A.
Daniel R McDougleNeuroAdjuvants, Inc., Salt Lake City, Utah, U.S.A.
Liuyin ZhangDepartment of Medicinal Chemistry, College of Pharmacy, University of Utah, Salt Lake City, Utah, U.S.A.
Dan KaufmannDepartment of Neurology, University of Utah Health Sciences Center, Salt Lake City, Utah, U.S.A.
Grzegorz BulajDepartment of Medicinal Chemistry, College of Pharmacy, University of Utah, Salt Lake City, Utah, U.S.A.
H Steve WhiteDepartment of Pharmacology & Toxicology, College of Pharmacy, University of Utah, Salt Lake City, Utah, U.S.A.
University of Washington · US

Funding

Development of a galanin-based therapy for the treatment of refractory epilepsyU01NS066911 · NINDS · UNIVERSITY OF UTAH · PI WHITE, H STEVE · 2010 to 2014
$3.4M
NINDS NIH HHS U01 NS066911
6 · The paper itself

Abstract

objectivePotential clinical utility of galanin or peptidic analogs has been hindered by poor metabolic stability, lack of brain penetration, and hyperglycemia due to galanin receptor subtype 1 (GalR1) activation. NAX 810-2, a galanin receptor subtype 2 (GalR2)-preferring galanin analog, possesses 15-fold greater affinity for GalR2 over GalR1 and protects against seizures in the mouse 6 Hz, corneal kindling, and Frings audiogenic seizure models. The purpose of these studies was to further evaluate the preclinical efficacy and pharmacokinetics of NAX 810-2 in mice.

methodsNAX 810-2 was administered by intravenous (i.v.; tail vein, bolus) injection to fully kindled (corneal kindling assay) or naive CF-1 mice (6 Hz assay and pharmacokinetic studies). Plasma NAX 810-2 levels were determined from trunk blood samples. NAX 810-2 was also added to human plasma at various concentrations for determination of plasma protein binding.

resultsIn the mouse corneal kindling model, NAX 810-2 dose-dependently blocked seizures following intravenous administration (median effective dose [ED SIGNIFICANCE: These studies further suggest the potential utility of NAX 810-2 as a novel therapy for epilepsy.

Indexed as

Drug Evaluation, PreclinicalAnimalsAnticonvulsantsArea Under CurveCorneaDisease Models, AnimalDose-Response Relationship, DrugElectric StimulationGalaninInjections, IntravenousKindling, NeurologicMaleMiceMovement DisordersProtein BindingReceptor, Galanin, Type 1AnticonvulsantsGalaninNAX 810-2Receptor, Galanin, Type 1Receptor, Galanin, Type 2Antiseizure drugBlood-brain barrierDrug discoveryEpilepsyGalaninNeuropeptidePharmacokineticSeizure

Identifiers

PMID28098336
PMCPMC5291807
OpenAlexW2575108029

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

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.