Remacemide is a potential anticonvulsant drug with an active metabolite, desglycinyl-remacemide (DGR). Both moieties have been reported to block neuronal Na(+) channels and the N-methyl-D-aspartate (NMDA) subtype of glutamate receptor. The effects of remacemide and DGR on zero Mg(2+)/4-aminopyridine-induced epileptiform discharges were investigated in the rat hippocampal slice preparation and compared with carbamazepine (CBZ), a prototypic Na(+) channel blocker, and AR-R15896AR, a putative NMDA channel blocker. Remacemide (0-100 microM) was without significant effect, while DGR, CBZ and AR-R15896AR all decreased burst frequency in a concentration (0-100 microM) dependent manner. These findings suggest that remacemide is not sufficiently potent at the Na(+) channel or NMDA receptor to attenuate epileptiform activity in this model and that the anticonvulsant effects of the drug may be mediated by DGR.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/s0304-3940(01)02511-3 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Pharmacological characterizations of the 'legal high' fluorolintane and isomers.
Eur J Pharmacol
August 2019
Department of Pharmaceutical Sciences, University of the Sciences, Philadelphia, PA, USA; Department of Chemistry and Biochemistry, University of the Sciences, Philadelphia, PA, USA.
1,2-Diarylethylamines represent a class of molecules that have shown potential in the treatment of pain, epilepsy, neurodegenerative disease and depression. Examples include lefetamine, remacemide, and lanicemine. Recently, several 1,2-diarylethylamines including the dissociatives diphenidine, methoxphenidine and ephenidine as well as the opioid MT-45, have appeared as 'research chemicals' or 'legal highs'.
View Article and Find Full Text PDFDo antiepileptic drugs increase the risk of infectious diseases? A meta-analysis of placebo-controlled studies.
Br J Clin Pharmacol
September 2017
Pharmacovigilance Centre, Florence Health Authority, Florence, Italy.
Aims: Experimental studies show that some antiepileptic drugs (AEDs) may modify natural immune defences, thus influencing the risk of developing infectious diseases. The aim of this meta-analysis was to explore whether AEDs as a class of drugs or singularly may increase risk of infectious diseases.
Methods: A meta-analysis of all randomized, double-blind, placebo-controlled trials (RCTs) investigating any AED in any condition was performed.
Anticonvulsant effects of isomeric nonimidazole histamine H receptor antagonists.
Drug Des Devel Ther
April 2017
Biocenter, Institute of Pharmaceutical Chemistry, Goethe University, Frankfurt, Germany; Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmaceutical and Medicinal Chemistry, Heinrich Heine University, Düsseldorf, Germany.
Phenytoin (PHT), valproic acid, and modern antiepileptic drugs (AEDs), eg, remacemide, loreclezole, and safinamide, are only effective within a maximum of 70%-80% of epileptic patients, and in many cases the clinical use of AEDs is restricted by their side effects. Therefore, a continuous need remains to discover innovative chemical entities for the development of active and safer AEDs. Ligands targeting central histamine H receptors (HRs) for epilepsy might be a promising therapeutic approach.
View Article and Find Full Text PDFPharmacological Investigations of the Dissociative 'Legal Highs' Diphenidine, Methoxphenidine and Analogues.
PLoS One
July 2017
Pharmaceutical Sciences, Philadelphia College of Pharmacy, University of the Sciences, Philadelphia Pennsylvania, United States of America.
1,2-Diarylethylamines including lanicemine, lefetamine, and remacemide have clinical relevance in a range of therapeutic areas including pain management, epilepsy, neurodegenerative disease and depression. More recently 1,2-diarylethylamines have been sold as 'legal highs' in a number of different forms including powders and tablets. These compounds are sold to circumvent governmental legislation regulating psychoactive drugs.
View Article and Find Full Text PDFHomology modelling and molecular docking studies of human placental cadherin protein for its role in teratogenic effects of anti-epileptic drugs.
Comput Biol Chem
February 2016
Toxicology and Computational Biology Group, Centre for Bioinformatics, M.D. University, Rohtak, Haryana 124001, India. Electronic address:
Article Synopsis
- Anti-epileptic drugs (AEDs) pose a risk of causing neural tube defects in pregnant women, leading to concerns about their safety during pregnancy.
- A study explored the interaction between major AEDs and human placental cadherin protein (hp-cadherin) to understand its role in teratogenic effects and the influence of Ca(2+) ions on the protein's function.
- Results indicated that four AEDs—Gabapentin, Pregabalin, Remacimide, and Vigabatrin—showed a strong affinity for hp-cadherin, highlighting its potential involvement in the drugs' teratogenic properties, with Ca(2+) ions essential for the protein’s effective functioning.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!