anticonvulsant effects
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Author(s):  
Marzieh Hashemi ◽  
Mehdi Abbasnejad ◽  
Ali Moghimi ◽  
Saeed Esmaeili-Mahani ◽  
Mahnaz Zamyad ◽  
...  

Biomedicines ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 53
Author(s):  
An Buckinx ◽  
Dimitri De Bundel ◽  
Ron Kooijman ◽  
Ilse Smolders

Epilepsy is a neurological disease affecting more than 50 million individuals worldwide. Notwithstanding the availability of a broad array of antiseizure drugs (ASDs), 30% of patients suffer from pharmacoresistant epilepsy. This highlights the urgent need for novel therapeutic options, preferably with an emphasis on new targets, since “me too” drugs have been shown to be of no avail. One of the appealing novel targets for ASDs is the ghrelin receptor (ghrelin-R). In epilepsy patients, alterations in the plasma levels of its endogenous ligand, ghrelin, have been described, and various ghrelin-R ligands are anticonvulsant in preclinical seizure and epilepsy models. Up until now, the exact mechanism-of-action of ghrelin-R-mediated anticonvulsant effects has remained poorly understood and is further complicated by multiple downstream signaling pathways and the heteromerization properties of the receptor. This review compiles current knowledge, and discusses the potential mechanisms-of-action of the anticonvulsant effects mediated by the ghrelin-R.


2021 ◽  
Vol 12 ◽  
Author(s):  
Ben A. Chindo ◽  
Melanie-Jayne R. Howes ◽  
Sawsan Abuhamdah ◽  
Musa I. Yakubu ◽  
Godwin I. Ayuba ◽  
...  

Melissa officinalis L. is used in traditional European and Iranian folk medicines to treat a plethora of neurological diseases including epilepsy. We utilized the in vitro and in vivo models of epilepsy to probe the anticonvulsant potentials of essential oil from M. officinalis (MO) to gain insight into the scientific basis for its applications in traditional medicine for the management of convulsive disorders. MO was evaluated for effects on maximal electroshock (MES) and pentylenetetrazole (PTZ) -induced seizures in mice, on 4–aminopyridine (4-AP)-brain slice model of epilepsy and sustained repetitive firing of current clamped neurons; and its ameliorative effects were examined on seizure severity, anxiety, depression, cognitive dysfunction, oxidative stress and neuronal cell loss in PTZ-kindled rats. MO reversibly blocked spontaneous ictal-like discharges in the 4-AP-brain slice model of epilepsy and secondary spikes from sustained repetitive firing, suggesting anticonvulsant effects and voltage-gated sodium channel blockade. MO protected mice from PTZ– and MES–induced seizures and mortality, and ameliorated seizure severity, fear-avoidance, depressive-like behavior, cognitive deficits, oxidative stress and neuronal cell loss in PTZ–kindled rats. The findings warrant further study for the potential use of MO and/or its constituent(s) as adjunctive therapy for epileptic patients.


Author(s):  
Arzuhan Cetindag Ciltas ◽  
Ercan Ozdemir ◽  
Erkan Gumus ◽  
Ahmet Sevki Taskiran ◽  
Handan Gunes ◽  
...  

Neurología ◽  
2021 ◽  
Author(s):  
E. Tahmasebi ◽  
H. Monsef-Esfahani ◽  
M. Vazirian ◽  
P. Sharafi-Badr ◽  
M. Sharifzadeh ◽  
...  

2021 ◽  
Vol 25 ◽  
Author(s):  
Anna Wójcicka

: 2,7-Naphthyridine is one of the six structural isomers of pyridopyridine. Biological investigations have shown that these compounds have a broad spectrum of activity. They have been found to have antitumor, antimicrobial, analgesic and anticonvulsant effects. The broad spectrum of biological activity of 2,7-naphthyridine derivatives is the main reason for the preparation of new compounds containing this scaffold. This review aims to present various methods of obtaining 2,7-naphthyridine analogs. Compounds containing a 2,7-naphthyridine moiety can be synthesized from a variety of substrates and may be classified into four main categories: those derived from acyclic compounds, from quinoline derivatives, from pyridine derivatives, and from other compounds. Most of them were obtained by the cyclocondensation or intramolecular cyclization of pyridine derivatives. Cyclocondensations of non-cyclic substrates also produced 2,7-naphthyridine derivatives. Tricyclic benzo[2,7]naphthyridines were prepared from quinolines. The 2,7-naphthyridine scaffold has also been synthesized by the rearrangement of pyrrolo[3,4-c]pyridines, pyrano[3,4-c]pyridines or thiopyrano[3,4-c]pyridines.


2021 ◽  
Vol 11 (1) ◽  
pp. 14-21
Author(s):  
Ramtin Gholizadeh ◽  
Zohreh Abdolmaleki ◽  
Taraneh Bahremand ◽  
Mehdi Ghasemi ◽  
Mehdi Gharghabi ◽  
...  

Background and Purpose: Licofelone is a dual 5-lipoxygenase/cyclooxygenase inhibitor, with well-documented anti-inflammatory and analgesic effects, which is used for treatment of osteoarthritis. Recent preclinical studies have also suggested neuroprotective and anti-oxidative properties of this drug in some neurological conditions such as seizure and epilepsy. We have recently demonstrated a role for nitric oxide (NO) signaling in the anti-epileptic activity of licofelone in two seizure models in rodents. Given the important role of N-methyl-D-aspartate receptors (NMDARs) activation in the NO production and its function in the nervous system, in the present study, we further investigated the involvement of NMDAR in the effects of licofelone (1, 3, 5, 10, and 20 mg/kg, intraperitoneal [i.p.]) in an in vivo model of seizure in mice.Methods: Clonic seizures were induced in male NMRI mice by intravenous administration of pentylenetetrazol (PTZ).Results: Acute administration of licofelone exerted anticonvulsant effects at 10 (p<0.01) and 20 mg/kg (p<0.001). A combined treatment with sub-effective doses of the selective NMDAR antagonist MK-801 (0.05 mg/kg, i.p.) and licofelone (5 mg/kg, i.p.) significantly (p<0.001) exerted an anticonvulsant effect on the PTZ-induced clonic seizures in mice. Notably, pre-treatment with the NMDAR co-agonist D-serine (30 mg/kg, i.p.) partially hindered the anticonvulsant effects of licofelone (20 mg/kg).Conclusions: Our data suggest a possible role for the NMDAR in the anticonvulsant effects of licofelone on the clonic seizures induced by PTZ in mice.


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