ArticleProceedings of the National Academy of Sciences of the United States of America2002
Anticonvulsant activity of a nonpeptide galanin receptor agonist.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers.
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Who cites it
42 citing papers in PubMed, 129 citations in OpenAlex.
- Six-Fold Methyl Internal Rotation andThe journal of physical chemistry. A · 2026Article
- Intravenous galanin (1-16) and a GalR1 agonist attenuate allodynia in rats with spared nerve injury.Pain reports · 2026Article
- Galanin Receptors in the Central Nervous System: Exploring Ligand Interactions, Signal Transduction, and Potential Clinical Implications.Molecules (Basel, Switzerland) · 2026Review
- Sudden Unexpected Death in Epilepsy: Central Respiratory Chemoreception.International journal of molecular sciences · 2025Review
- Assessment of resveratrol on diabetes of zebrafish (Journal of diabetes and metabolic disorders · 2022Article
- Galanin analogs prevent mortality from seizure-induced respiratory arrest in mice.Frontiers in neural circuits · 2022Article
- Cell-type specific expression and behavioral impact of galanin and GalR1 in the locus coeruleus during opioid withdrawal.Addiction biology · 2021Article
- Increased Serum Neuropeptide Galanin Level Is a Predictor of Cognitive Dysfunction in Patients with Hip Fracture.Disease markers · 2021Observational
- Insights into Potential Targets for Therapeutic Intervention in Epilepsy.International journal of molecular sciences · 2020Review
- Effects of galanin receptor 2 and receptor 3 knockout in mouse models of acute seizures.Epilepsia · 2018Article
- Preclinical Analgesic and Safety Evaluation of the GalR2-preferring Analog, NAX 810-2.Neurochemical research · 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
- The galanin receptor agonist, galnon, attenuates cocaine-induced reinstatement and dopamine overflow in the frontal cortex.Addiction biology · 2015Article
- Regulation of glucose and insulin release following acute and repeated treatment with the synthetic galanin analog NAX-5055.Neuropeptides · 2015Article
- Positive allosteric modulators to peptide GPCRs: a promising class of drugs.Acta pharmacologica Sinica · 2013Review
- Galanin-induced decreases in nucleus accumbens/striatum excitatory postsynaptic potentials and morphine conditioned place preference require both galanin receptor 1 and galanin receptor 2.The European journal of neuroscience · 2013Article
- Galnon facilitates extinction of morphine-conditioned place preference but also potentiates the consolidation process.PloS one · 2013Article
- Galanin receptors and ligands.Frontiers in endocrinology · 2012Article
- Synthesis and biological evaluation of novel pyrimidine derivatives as sub-micromolar affinity ligands of GalR2.Bioorganic & medicinal chemistry letters · 2011Article
Corrections and comments
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Authors and funding
14 authors at 1 institution in 1 country.
Funding
Abstract
Galanin is a neuropeptide with a wide variety of biological functions, including that of a strong endogenous anticonvulsant. No nonpeptide ligands, capable of activating galanin receptors, are available today. Based on known pharmacophores of galanin, a combinatorial library was designed, synthesized, and screened at the rat hippocampal galanin receptor. A low molecular weight galanin receptor agonist, 7-((9-fluorenylmethoxycarbonyl)cyclohexylalanyllysyl)amino-4-methylcoumarin (galnon) was found to displace (125)I-galanin with micromolar affinity at Bowes cellular and rat hippocampal membranes. Autoradiographic binding assay on rat spinal cord sections confirmed the ability of galnon to displace (125)I-galanin from its binding sites. Galnon inhibited adenylate cyclase activity, suggesting an agonist action at galanin receptors. When injected i.p. galnon reduced the severity and increased the latency of pentylenetetrazole-induced seizures in mice and reversed the proconvulsant effects of the galanin receptor antagonist M35, injected into a lateral ventricle. Intrahippocampal injection of galnon also shortened the duration of self-sustaining status epilepticus in rats, confirming its agonist properties in vivo. Pretreatment of rats with antisense peptide nucleic acid targeted to galanin receptor type 1 mRNA abolished the effect of galnon, suggesting mediation of its anticonvulsant properties through this receptor subtype. These findings introduce a systemically active nonpeptide galanin agonist anticonvulsant.
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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.