ArticleNeurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics2009
Developing novel antiepileptic drugs: characterization of NAX 5055, a systemically-active galanin analog, in epilepsy models.
Article in Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 52 citations in OpenAlex.
- Sudden Unexpected Death in Epilepsy: Central Respiratory Chemoreception.International journal of molecular sciences · 2025Review
- Treatment of status epilepticus: Physiology, pharmacology, and future directions.Epilepsia open · 2023Article
- Galanin analogs prevent mortality from seizure-induced respiratory arrest in mice.Frontiers in neural circuits · 2022Article
- Intranasal Delivery of a Methyllanthionine-Stabilized Galanin Receptor-2-Selective Agonist Reduces Acute Food Intake.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2021Article
- Article
- Functions of galanin, spexin and kisspeptin in metabolism, mood and behaviour.Nature reviews. Endocrinology · 2021Review
- Protective Role of Galanin during Chemically Induced Inflammation in Zebrafish Larvae.Biology · 2021Article
- Insights into Potential Targets for Therapeutic Intervention in Epilepsy.International journal of molecular sciences · 2020Review
- G protein-coupled receptors in acquired epilepsy: Druggability and translatability.Progress in neurobiology · 2019Review
- Effect of Tadalafil on Seizure Threshold and Activity of Antiepileptic Drugs in Three Acute Seizure Tests in Mice.Neurotoxicity research · 2018Article
- Preclinical Analgesic and Safety Evaluation of the GalR2-preferring Analog, NAX 810-2.Neurochemical research · 2017Article
- Development and pharmacologic characterization of the rat 6 Hz model of partial seizures.Epilepsia · 2017Article
- Preclinical evaluation of intravenous NAX 810-2, a novel GalR2-preferring analog, for anticonvulsant efficacy and pharmacokinetics.Epilepsia · 2017Article
- Galanin regulates blood glucose level in the zebrafish: a morphological and functional study.Histochemistry and cell biology · 2016Article
- Glutamatergic Mechanisms Associated with Seizures and Epilepsy.Cold Spring Harbor perspectives in medicine · 2015Review
- Regulation of glucose and insulin release following acute and repeated treatment with the synthetic galanin analog NAX-5055.Neuropeptides · 2015Article
- Analgesic properties of a peripherally acting and GalR2 receptor-preferring galanin analog in inflammatory, neuropathic, and acute pain models.The Journal of pharmacology and experimental therapeutics · 2015Article
- Efficacy and tolerability of the galanin analog NAX 5055 in the multiple-hit rat model of symptomatic infantile spasms.Epilepsy research · 2014Article
- Generating orally active galanin analogues with analgesic activities.ChemMedChem · 2012Article
- Galanin receptors and ligands.Frontiers in endocrinology · 2012Article
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
The endogenous neuropeptide galanin and its associated receptors galanin receptor 1 and galanin receptor 2 are highly localized in brain limbic structures and play an important role in the control of seizures in animal epilepsy models. As such, galanin receptors provide an attractive target for the development of novel anticonvulsant drugs. Our efforts to engineer galanin analogs that can penetrate the blood-brain-barrier and suppress seizures, yielded NAX 5055 (Gal-B2), a systemically-active analog that maintains low nanomolar affinity for galanin receptors and displays a potent anticonvulsant activity. In this report, we show that NAX 5055 is active in three models of epilepsy: 1) the Frings audiogenic seizure-susceptible mouse, 2) the mouse corneal kindling model of partial epilepsy, and 3) the 6 Hz model of pharmacoresistant epilepsy. NAX 5055 was not active in the traditional maximal electroshock and subcutaneous pentylenetetrazol seizure models. Unlike most antiepileptic drugs, NAX 5055 showed high potency in the 6 Hz model of epilepsy across all three different stimulation currents; i.e., 22, 32 and 44 mA, suggesting a potential use in the treatment of pharmacoresistant epilepsy. Furthermore, NAX 5055 was found to be biologically active after intravenous, intraperitoneal, and subcutaneous administration, and efficacy was associated with a linear pharmacokinetic profile. The results of the present investigation suggest that NAX 5055 is a first-in-class neurotherapeutic for the treatment of epilepsy in patients refractory to currently approved antiepileptic drugs.
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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.