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  1. Article ; Online: Anticonvulsant activity of Tetrahydrolinalool: behavioral, electrophysiological, and molecular docking approaches.

    Fonsêca, Diogo V / da Silva, Pablo R / Pires, Hugo F O / Rocha, Juliana S / de Oliveira, Leandra Eugênia G / Reis, Flavia M S / Cavalho, Erika B M / Pazos, Natalia D N / de Sousa, Natália F / Guedes, Erika C / Ribeiro, Leandro R / Sá, Rita de Cassia S / Salvadori, Mirian G S S / Sousa, Damião P / Scotti, Marcus T / Felipe, Cicero F B / de Almeida, Reinaldo N / Scotti, Luciana

    ChemMedChem

    2024  , Page(s) e202400135

    Abstract: Tetrahydrolinalool (THL) is an acyclic monoterpene alcohol, produced during linalol metabolism and also a constituent of essential oils. As described in the literature, many monoterpenes present anticonvulsant properties, and thus we became interested in ...

    Abstract Tetrahydrolinalool (THL) is an acyclic monoterpene alcohol, produced during linalol metabolism and also a constituent of essential oils. As described in the literature, many monoterpenes present anticonvulsant properties, and thus we became interested in evaluating the anticonvulsant activity of Tetrahydrolinalool using in mice model as well as in silico approaches. Our results demonstrated that THL increased latency to seizure onset and also reduced the mortality, in picrotoxin induced seizure tests. The results may be related to GABAergic regulation, which was also suggested in seizure testing induced by 3-mercapto-propionic acid. In the strychnine-induced seizure testing, none of the groups pretreated with THL modulated the parameters indicative of anticonvulsant effect. The electrophysiological results revealed that THL treatment reduces seizures induced by pentylenetetrazole. The in silico molecular docking studies showed that the interaction between THL and a GABAA receptor model formed a stable complex, in comparison to the crystaligraphic structure of diazepam, a structurally related ligand. In conclusion, all the evidences showed that THL presents effective anticonvulsant activity related to the GABAergic pathway, being a candidate for treatment of epileptic syndromes.
    Language English
    Publishing date 2024-04-30
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 2218496-X
    ISSN 1860-7187 ; 1860-7179
    ISSN (online) 1860-7187
    ISSN 1860-7179
    DOI 10.1002/cmdc.202400135
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

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  2. Article ; Online: Monoterpenoid terpinen-4-ol exhibits anticonvulsant activity in behavioural and electrophysiological studies.

    Nóbrega, Franklin F F / Salvadori, Mirian G S S / Masson, Cintia J / Mello, Carlos F / Nascimento, Tiago S / Leal-Cardoso, José H / de Sousa, Damião P / Almeida, Reinaldo N

    Oxidative medicine and cellular longevity

    2014  Volume 2014, Page(s) 703848

    Abstract: Terpinen-4-ol (4TRP) is a monoterpenoid alcoholic component of essential oils obtained from several aromatic plants. We investigated the psychopharmacological and electrophysiological activities of 4TRP in male Swiss mice and Wistar rats. 4TRP was ... ...

    Abstract Terpinen-4-ol (4TRP) is a monoterpenoid alcoholic component of essential oils obtained from several aromatic plants. We investigated the psychopharmacological and electrophysiological activities of 4TRP in male Swiss mice and Wistar rats. 4TRP was administered intraperitoneally (i.p.) at doses of 25 to 200 mg/kg and intracerebroventricularly (i.c.v.) at concentrations of 10, 20, and 40 ng/2 μL. For in vitro experiments, 4TRP concentrations were 0.1 mM and 1.0 mM. 4TRP (i.p.) inhibited pentylenetetrazol- (PTZ-) induced seizures, indicating anticonvulsant effects. Electroencephalographic recordings showed that 4TRP (i.c.v.) protected against PTZ-induced seizures, corroborating the behavioural results. To determine whether 4TRP exerts anticonvulsant effects via regulation of GABAergic neurotransmission, we measured convulsions induced by 3-mercapto-propionic acid (3-MP). The obtained results showed involvement of the GABAergic system in the anticonvulsant action exerted by 4TRP, but flumazenil, a selective antagonist of the benzodiazepine site of the GABAA receptor, did not reverse the anticonvulsant effect, demonstrating that 4TRP does not bind to the benzodiazepine-binding site. Furthermore, 4TRP decreased the sodium current through voltage-dependent sodium channels, and thus its anticonvulsant effect may be related to changes in neuronal excitability because of modulation of these channels.
    MeSH term(s) Animals ; Anticonvulsants/chemistry ; Anticonvulsants/pharmacology ; Anticonvulsants/therapeutic use ; Behavior, Animal/drug effects ; Binding Sites ; Electrophysiological Phenomena/drug effects ; Flumazenil/pharmacology ; GABA-A Receptor Antagonists/pharmacology ; GABAergic Neurons/drug effects ; GABAergic Neurons/metabolism ; Infusions, Intraventricular ; Injections, Intraperitoneal ; Male ; Mice ; Monoterpenes/chemistry ; Monoterpenes/pharmacology ; Monoterpenes/therapeutic use ; Pentylenetetrazole/toxicity ; Rats ; Rats, Wistar ; Receptors, GABA-A/chemistry ; Receptors, GABA-A/metabolism ; Seizures/chemically induced ; Seizures/drug therapy ; Seizures/pathology ; Terpenes/chemistry ; Terpenes/pharmacology ; Terpenes/therapeutic use
    Chemical Substances Anticonvulsants ; GABA-A Receptor Antagonists ; Monoterpenes ; Receptors, GABA-A ; Terpenes ; Flumazenil (40P7XK9392) ; terpinenol-4 (562-74-3) ; Pentylenetetrazole (WM5Z385K7T)
    Language English
    Publishing date 2014-08-10
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2455981-7
    ISSN 1942-0994 ; 1942-0994
    ISSN (online) 1942-0994
    ISSN 1942-0994
    DOI 10.1155/2014/703848
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Fish oil attenuates methylmalonate-induced seizures.

    Banderó, Cristina Ruedell Reschke / Salvadori, Mirian G S S / Gomes, Anajara Teixeira / Dal Ri, Nadja M K / Furian, Ana Flávia / Oliveira, Mauro Schneider / Rambo, Leonardo Magno / Scorza, Fulvio A / Cysneiros, Roberta M / Emanuelli, Tatiana / Mello, Carlos Fernando

    Epilepsy research

    2013  Volume 105, Issue 1-2, Page(s) 69–76

    Abstract: Methylmalonic acidemias are inherited metabolic disorders characterized by methylmalonate (MMA) accumulation and neurological dysfunction, including seizures. Dietary fatty acids are known as an important energy source and reduce seizure activity in ... ...

    Abstract Methylmalonic acidemias are inherited metabolic disorders characterized by methylmalonate (MMA) accumulation and neurological dysfunction, including seizures. Dietary fatty acids are known as an important energy source and reduce seizure activity in selected acute animal models. This study investigated whether chronic treatment with fish oil or with oleic acid attenuates MMA-induced seizures and whether maintenance of Na(+),K(+)-ATPase activity was involved in such an effect. Adult male Wistar rats were given fish oil (85 mg/kg), oleic acid (85 mg/kg) or vehicle (0.42% aqueous Cremophor EL™, 4 mL/kg/body weight/day), p.o., for 75 days. On the 73th day a cannula was implanted in the right lateral ventricle with electrodes over the parietal cortex for EEG recording. On the 76th day the animals were injected with NaCl (2.5 μmol/2.5 μL, i.c.v.), or with MMA (2.5 μmol/2.5 μL, i.c.v.), and seizure activity was measured by electroencephagraphic (EEG) recording with concomitant behavior monitoring. The effect of prostaglandin E2 (PGE2) on Na(+),K(+)-ATPase activity of slices of cerebral cortex from NaCl-injected animals was determined. Fish oil increased the latency to MMA-induced tonic-clonic seizures, reduced the mean amplitude of ictal EEG recordings, and prevented PGE2-induced decrease of Na(+),K(+)-ATPase activity in cortical slices in vitro. Oleic acid decreased mean amplitude of ictal EEG recordings. The results support that fish oil decreases MMA-induced seizures. The decreased sensitivity of Na(+),K(+)-ATPase to the inhibitory effect of PGE2 in fish oil-treated animals may be related to the currently reported anticonvulsant activity.
    MeSH term(s) Animals ; Anticonvulsants/therapeutic use ; Electroencephalography/methods ; Fish Oils/therapeutic use ; Male ; Methylmalonic Acid/toxicity ; Random Allocation ; Rats ; Rats, Wistar ; Seizures/chemically induced ; Seizures/physiopathology ; Seizures/prevention & control
    Chemical Substances Anticonvulsants ; Fish Oils ; Methylmalonic Acid (8LL8S712J7)
    Language English
    Publishing date 2013-07
    Publishing country Netherlands
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 632939-1
    ISSN 1872-6844 ; 0920-1211
    ISSN (online) 1872-6844
    ISSN 0920-1211
    DOI 10.1016/j.eplepsyres.2013.01.005
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 2193: Show issues Location:
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    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)

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