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Stanislaw J Czuczwar - One of the best experts on this subject based on the ideXlab platform.
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EFFECTS OF TAMOXIFEN, MIFEPRISTONE AND CYPROTERONE ON THE ELECTROCONVULSIVE THRESHOLD AND Pentetrazole-INDUCED CONVULSIONS IN MICE
2014Co-Authors: Pol J. Pharmacol, Kinga K Borowicz, Stanisaw J. Czuczwar, Mariusz Matuszek, Z. Kleinrok, Stanislaw J CzuczwarAbstract:Effects of tamoxifen, mifepristone and cyproterone on the electroconvulsive threshold and Pentetrazole-induced convulsions in mice. K.K. BORO
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acute exposure to caffeine decreases the anticonvulsant action of ethosuximide but not that of clonazepam phenobarbital and valproate against Pentetrazole induced seizures in mice
Pharmacological Reports, 2006Co-Authors: Jarogniew J Luszczki, Katarzyna M. Sawicka, Marek Zuchora, Justyna Koziñska, Stanislaw J CzuczwarAbstract:This study examines the effect of acute administration of caffeine sodium benzoate (CAF) on the anticonvulsant action of four conventional antiepileptic drugs (AEDs: clonazepam - CZP, ethosuximide - ETS, phenobarbital - PB and valproate - VPA) against Pentetrazole (PTZ)-induced clonic seizures in mice. The results indicate that CAF at a dose of 92.4 mg/kg significantly reduced the threshold for PTZ-induced clonic seizures in mice from 69.5 to 51.7 mg/kg (p < 0.05), being ineffective at lower doses of 69.3 and 46.2 mg/kg. Moreover, CAF at doses of 69.3 and 92.4 mg/kg attenuated the protective action of ETS against PTZ-induced seizures, by increasing its median effective dose (ED 50 ) from 127.7 to 182.3 (p < 0.05), and 198.3 mg/kg (p < 0.01), respectively. In this case, no pharmacokinetic changes in total brain ETS concentrations after systemic ip administration of CAF (at 92.4 mg/kg) were observed, indicating a pharmacodynamic nature of interaction between ETS and CAF in the PTZ-test in mice. In contrast, CAF (at a dose of 92.4 mg/kg reducing the threshold for PTZ-induced seizures) combined with other AEDs (CZP, PB and VPA) did not affect their anticonvulsant action in the PTZ test in mice. Moreover, CAF (92.4 mg/kg) did not alter significantly total brain concentrations of the remaining AEDs (CZP, PB and VPA). The evaluation of potential acute adverse effects produced by AEDs in combination with CAF revealed that neither CAF (up to 92.4 mg/kg) administered alone nor combined with the studied drugs (at doses corresponding to their ED 50 values in the PTZ-test) affected motor performance of animals in the chimney test. In conclusion, the acute exposure to CAF may diminish the antiseizure protection offered by ETS in epileptic patients. Therefore, patients treated with ETS should avoid CAF.
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influence of the antagonist of the glycine site of nmda receptors mrz 2 576 on the anticonvulsant activity of conventional antiepileptic drugs in mice
Pharmacological Reports, 2005Co-Authors: Katarzyna Makarskabialek, Rafal M Kaminski, Stanislaw J CzuczwarAbstract:The purpose of this study was to evaluate the influence of the glycine site antagonist of the NMDA receptor, MRZ 2/576 (8-chloro-4-hydroxy-l-oxo-l,2-dihydropyridazino[4,5-b]quinolin-5-oxide choline salt), on the anticonvulsive activity of carbamazepine, oxcarbazepine, diphenylhydantoin, phenobarbital and valproate against maximal electroshock (MES)-induced seizures and ethosuximide, valproate and clonazepam against Pentetrazole (PTZ)-induced seizures in mice. MRZ 2/576 applied intraperitoneally 5 min before electroconvulsions, at the dose of 10 and 15 mg/kg, significantly raised the convulsive threshold (from 6.9 to 8.8 and 10.8 mA respectively). At lower doses, it did not affect the threshold. MRZ 2/576 applied at the dose of 5, 10 and 20 mg/kg did not influence the clonic phase of PTZ-induced seizures, but protected the animals against the tonic phase. The anticonvulsant effect of a given antiepileptic drug was expressed as its ED 5 0 value (in mg/kg), which represents the dose of the drug required to protect 50% of animals against MES or PTZ seizures. MRZ 2/576 co-administered at a subprotective dose (5 mg/kg) with carbamazepine, oxcarbazepine, diphenylhydantoin, phenobarbital or valproate, significantly reduced their ED 5 0 values in MES test. Also, at the dose of 2.5 mg/kg it enhanced the protective activity of carbamazepine and valproate. At the lowest tested dose (1.25 mg/kg), it still potentiated the anticonvulsant activity of valproate. However, MRZ 2/576 (5 mg/kg) applied with valproate, ethosuximide or clonazepam did not influence their protective effects in the PTZ test. The combinations of MRZ 2/576 with almost every studied antiepileptic drug (providing a 50% protection against maximal electroshock or PTZ-induced seizures) did not produce motor impairment in the chimney test nor long-term memory deficit measured in the passive avoidance task. Only valproate alone or combined with MRZ 2/576 impaired both of these measures. It may be concluded that MRZ 2/576 enhanced the anticonvulsive activity of antiepileptic drugs against MES without accompanying potentiation of adverse effects. However, there was no positive interaction in the PTZ test. Finally, pharmacokinetic interactions do not seem responsible for the obtained results because MRZ 2/576 (5 mg/kg) did not alter the free plasma levels of the antiepileptics tested in the present study.
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RILUZOLE ENHANCES THE ANTISEIZURE ACTION OF CONVENTIONAL ANTIEPILEPTIC DRUGS AGAINST Pentetrazole-INDUCED CONVULSIONS IN MICE
2004Co-Authors: Stanislaw J Czuczwar, Kinga K Borowicz, Andrzej Sêkowski, Edyta Drelewska, J. Czuczwar, Pol J. PharmacolAbstract:Riluzole enhances the antiseizure action of conventional antiepileptic drugs against Pentetrazole-induced seizures in mice. K.K. BOROWICZ
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influence of sib 1893 a selective mglur5 receptor antagonist on the anticonvulsant activity of conventional antiepileptic drugs in two models of experimental epilepsy
Polish Journal of Pharmacology, 2003Co-Authors: Kinga K Borowicz, Barbara Piskorska, Jarogniew J łuszczki, Stanislaw J CzuczwarAbstract:: SIB 1893, a non-competitive antagonist of group I metabotropic glutamate receptor subtype 5, administered at doses ranging from 0.25 to 10 mg/kg, failed to influence Pentetrazole-induced convulsions in mice. Moreover, SIB 1893 (10 and 20 mg/kg) did not affect the protective action of valproate, ethosuximide, phenobarbital and clonazepam in this test. Similarly, the mGluR5 antagonist did not modulate the antiseizure activity of carbamazepine, diphenylhydantoin and phenobarbital against maximal electroshock in mice. The combined treatment of SIB 1893 with conventional antiepileptic drugs did not lead to motor impairment. Long-term memory disturbances were observed only in the case of the combination of SIB 1893 with phenobarbital.
Stanisaw J. Czuczwar - One of the best experts on this subject based on the ideXlab platform.
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Effect of NG-nitro-L-arginine on the anti-
2014Co-Authors: Short Communication, Jarogniew J. £uszczki, Marcin Szadkowski, Stanisaw J. CzuczwarAbstract:convulsant action of four second-generation antiepileptic drugs in Pentetrazole-induced clonic seizures in mic
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INFLUENCE OF VIGABATRIN, A NOVEL ANTIEPILEPTIC DRUG, ON THE ANTICONVULSANT ACTIVITY OF CONVENTIONAL ANTIEPILEPTICS IN Pentetrazole-INDUCED SEIZURES IN MICE
2014Co-Authors: Pol J. Pharmacol, Marian Wielosz, Stanisaw J. CzuczwarAbstract:Influence of vigabatrin, a novel antiepileptic drug, on the anticonvulsant activity of conventional antiepileptics in Pentetrazole-induced seizures in mice. M. ŒWI¥DER, J. £USZCZKI, M. WIELOSZ, S.J. CZUCZWAR. Pol
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EFFECTS OF TAMOXIFEN, MIFEPRISTONE AND CYPROTERONE ON THE ELECTROCONVULSIVE THRESHOLD AND Pentetrazole-INDUCED CONVULSIONS IN MICE
2014Co-Authors: Pol J. Pharmacol, Kinga K Borowicz, Stanisaw J. Czuczwar, Mariusz Matuszek, Z. Kleinrok, Stanislaw J CzuczwarAbstract:Effects of tamoxifen, mifepristone and cyproterone on the electroconvulsive threshold and Pentetrazole-induced convulsions in mice. K.K. BORO
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INFLUENCE OF SIB 1893, A SELECTIVE mGluR5 RECEPTOR ANTAGONIST, ON THE ANTICONVULSANT ACTIVITY OF CONVENTIONAL ANTIEPILEPTIC DRUGS IN TWO MODELS OF EXPERIMENTAL EPILEPSY
2013Co-Authors: Pol J. Pharmacol, Kinga K Borowicz, Barbara Piskorska, Stanisaw J. CzuczwarAbstract:Influence of SIB 1893, a selective mGluR5 receptor antagonist, on the anticonvulsant activity of conventional antiepileptic drugs in two models of experimental epilepsy. K.K. BOROWICZ, B. PISKORSKA, J. £USZCZKI, S.J. CZUCZWAR. Pol. J. Pharmacol., 2003, 55, 735–740. SIB 1893, a non-competitive antagonist of group I metabotropic glutamate receptor subtype 5, administered at doses ranging from 0.25 to 10 mg/kg, failed to influence Pentetrazole-induced convulsions in mice. Moreover, SIB 1893 (10 and 20 mg/kg) did not affect the protective action of valproate, ethosuximide, phenobarbital and clonazepam in this test. Similarly, the mGluR5 antagonist did not modulate the antiseizure activity of carbamazepine, diphenylhydantoin and phenobarbital against maximal electroshock in mice. The combined treatment of SIB 1893 with conventional antiepileptic drugs did not lead to motor impairment. Long-term memory disturbances were observed only in the case of the combination of SIB 1893 with phenobarbital
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Copyright © 2006 by Institute of Pharmacology Polish Academy of Sciences
2006Co-Authors: Short Communication, Marian Wielosz, Mariusz J. Œwider, Jacek Porêbiak, Stanisaw J. CzuczwarAbstract:Influence of cimetidine on the anticonvulsant activity of conventional antiepileptic drugs against Pentetrazole-induced seizures in mic
Pol J. Pharmacol - One of the best experts on this subject based on the ideXlab platform.
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Lack of interaction between the behavioral effects of ketamine and benzodiazepines
2014Co-Authors: Sylwia Fidecka, Ewa Pirogowicz, In Mice S. Fidecka, Pol J. Pharmacol, Correspondence S. FideckaAbstract:The effect of co-administration of ketamine at the sub-effective dose with diazepam, chlordiazepoxide and clonazepam on their antinociceptive and protective efficacy against Pentetrazole-induced seizures were studied in mice. Ketamine alone produces dose-dependent antinociception manifested as reduction in the number of writhing episodes evoked by acetic acid. In the writhing test, the antinociceptive effects of the threshold doses of diazepam, chlordiazepoxide or clonazepam were not changed by ketamine, whereas that of morphine was intensified by ketamine. In the hot plate test, slight antinociceptive effects of the threshold dose of diazepam, but not that of chlordiazepoxide (except the results at 120 min of observation), were significantly intensified by ketamine vs ketamine alone. Ketamine alone was able to protect mice, in the dose-related manner, against Pentetrazole-induced seizures. The anticonvulsant effects of the threshold doses of diazepam, chlordiazepoxide and clonazepam were not changed by ketamine. These findings indicate that co-administration of ketamine (at the sub-effective dose) with diazepam, chlordiazepoxide and clonazepam (at non-effective doses) resulted in an intensification of neither antinociceptive nor protective effect against Pentetrazole-induced seizures in mice. These data seem to indicate the lack of interaction between ketamine and benzodiazepines with respect to their antinociceptive and anticonvulsant efficacy
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INFLUENCE OF VIGABATRIN, A NOVEL ANTIEPILEPTIC DRUG, ON THE ANTICONVULSANT ACTIVITY OF CONVENTIONAL ANTIEPILEPTICS IN Pentetrazole-INDUCED SEIZURES IN MICE
2014Co-Authors: Pol J. Pharmacol, Marian Wielosz, Stanisaw J. CzuczwarAbstract:Influence of vigabatrin, a novel antiepileptic drug, on the anticonvulsant activity of conventional antiepileptics in Pentetrazole-induced seizures in mice. M. ŒWI¥DER, J. £USZCZKI, M. WIELOSZ, S.J. CZUCZWAR. Pol
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STUDY ON THE INFLUENCE OF POTENT INHIBITORS OF NEURONAL NITRIC OXIDE SYNTHASE ON THE ANTINOCICEPTIVE AND ANTICONVULSANT ACTIVITY OF BENZODIAZEPINES IN MICE
2014Co-Authors: Pol J. Pharmacol, Sylwia FideckaAbstract:Study on the influence of potent inhibitors of neuronal nitric oxide synthase on the antinociceptive and anticonvulsant activity of benzodiazepines in mice. S. FIDECKA, Pol. J. Pharmacol., 2003, 55, 193–201. The influence of 1-(2-trifluoromethylphenyl)imidazole (TRIM) and 3-bromo-7-nitroindazole (3-Br-7-NI), potent and relatively selective inhibitors of neuronal nitric oxide (NO) synthase, on the antinociceptive and anticonvulsive effects of diazepam and clonazepam was investigated in mice. The effects were assessed in the writhing test and Pentetrazole-induced seizures, respectively. The antinociceptive effects of the threshold doses of diazepam (1 mg/kg) and clonazepam (0.0375 mg/kg) were significantly increased by TRIM (7.5 mg/kg) but not by 3-Br-7-NI (10 mg/kg). L-arginine (125 mg/kg) was able to reverse the effects produced by co-administration of TRIM (7.5 mg/kg) with diazepam (1 mg/kg), and also of TRIM (7.5 mg/kg) with clonazepam (0.0375 mg/kg). Protective efficacy of the threshold dose (0.05 mg/kg) of diazepam against Pentetrazole-induced tonic convulsions and death was significantly increased by TRIM (25 mg/kg) but not by 3-Br-7-NI (10 and 100 mg/kg). TRIM (25 mg/kg) intensified the protective efficacy of the threshold dose (0.005 mg/kg) of clonazepam, but the effect was not reversed by L-arginine (125 mg/kg). The present results seem to confirm, at least partly, participation of NO in antinociceptive and anticonvulsant effects of benzodiazepines, and point to TRIM as a better tool than 3-Br-7NI for examination of the role of NO in behavioral studies
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EFFECTS OF TAMOXIFEN, MIFEPRISTONE AND CYPROTERONE ON THE ELECTROCONVULSIVE THRESHOLD AND Pentetrazole-INDUCED CONVULSIONS IN MICE
2014Co-Authors: Pol J. Pharmacol, Kinga K Borowicz, Stanisaw J. Czuczwar, Mariusz Matuszek, Z. Kleinrok, Stanislaw J CzuczwarAbstract:Effects of tamoxifen, mifepristone and cyproterone on the electroconvulsive threshold and Pentetrazole-induced convulsions in mice. K.K. BORO
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SYNTHESIS AND ANTICONVULSANT ACTIVITIES OF 4-N-SUBSTITUTED ARYLSEMICARBAZONES
2013Co-Authors: Pol J. Pharmacol, J. P. Stables, S N Pandeya, Surendra N. P, Sonia Kohli, Nadeem Siddique, N. SiddiquiAbstract:A series of 4-N-substituted arylsemicarbazones with increased lipophilicity were synthesized and evaluated for anticonvulsant activity. The compounds provided significant protection against maximal electroshock induced seizures (MES) and seizures indicated by sc Pentetrazole administration (sc PTZ) at 300 mg/kg after 0.5 h. The compounds 8 and 4 were active in MES and sc PTZ indicated seizure. The study has shown that introduction of alkyl (ethyl) at the terminal amino group and alkoxy (methoxy) moiety at the distal aryl ring led to increased activity and decreased toxicity
Kinga K Borowicz - One of the best experts on this subject based on the ideXlab platform.
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EFFECTS OF TAMOXIFEN, MIFEPRISTONE AND CYPROTERONE ON THE ELECTROCONVULSIVE THRESHOLD AND Pentetrazole-INDUCED CONVULSIONS IN MICE
2014Co-Authors: Pol J. Pharmacol, Kinga K Borowicz, Stanisaw J. Czuczwar, Mariusz Matuszek, Z. Kleinrok, Stanislaw J CzuczwarAbstract:Effects of tamoxifen, mifepristone and cyproterone on the electroconvulsive threshold and Pentetrazole-induced convulsions in mice. K.K. BORO
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INFLUENCE OF SIB 1893, A SELECTIVE mGluR5 RECEPTOR ANTAGONIST, ON THE ANTICONVULSANT ACTIVITY OF CONVENTIONAL ANTIEPILEPTIC DRUGS IN TWO MODELS OF EXPERIMENTAL EPILEPSY
2013Co-Authors: Pol J. Pharmacol, Kinga K Borowicz, Barbara Piskorska, Stanisaw J. CzuczwarAbstract:Influence of SIB 1893, a selective mGluR5 receptor antagonist, on the anticonvulsant activity of conventional antiepileptic drugs in two models of experimental epilepsy. K.K. BOROWICZ, B. PISKORSKA, J. £USZCZKI, S.J. CZUCZWAR. Pol. J. Pharmacol., 2003, 55, 735–740. SIB 1893, a non-competitive antagonist of group I metabotropic glutamate receptor subtype 5, administered at doses ranging from 0.25 to 10 mg/kg, failed to influence Pentetrazole-induced convulsions in mice. Moreover, SIB 1893 (10 and 20 mg/kg) did not affect the protective action of valproate, ethosuximide, phenobarbital and clonazepam in this test. Similarly, the mGluR5 antagonist did not modulate the antiseizure activity of carbamazepine, diphenylhydantoin and phenobarbital against maximal electroshock in mice. The combined treatment of SIB 1893 with conventional antiepileptic drugs did not lead to motor impairment. Long-term memory disturbances were observed only in the case of the combination of SIB 1893 with phenobarbital
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Polish Academy of Sciences Review Melatonin in experimental seizures and epilepsy
2013Co-Authors: Monika Banach, Elwira Gurdziel, Marian Jêdrych, Kinga K BorowiczAbstract:Although melatonin is approved only for the treatment of jet-lag syndrome and some types of insomnia, clinical data suggest that it is effective in the adjunctive therapy of osteoporosis, cataract, sepsis, neurodegenerative diseases, hypertension, and even cancer. Melatonin also modulates the electrical activity of neurons by reducing glutamatergic and enhancing GABA-ergic neurotransmission. The indoleamine may also be metabolized to kynurenic acid, an endogenous anticonvulsant. Finally, the hormone and its metabolites act as free radical scavengers and antioxidants. The vast majority of experimental data indicates anticonvulsant properties of the hormone. Melatonin inhibited audiogenic and electrical seizures, as well as reduced convulsions induced by Pentetrazole, pilocarpine, L-cysteine and kainate. Only a few studies have shown direct or indirect proconvulsant effects of melatonin. For instance, melatonin enhanced low Mg 2+-induced epileptiform activity in the hippocampus, whereas melatonin antagonists delayed the onset of pilocarpine-induced seizures. However, the relatively high doses of melatonin required to inhibit experimental seizures can induce some undesired effects (e.g., cognitive and motor impairment and decreased body temperature). In humans, melatonin may attenuate seizures, and it is most effective in the treatment of juvenile intractable epilepsy. Its additional benefits include improved physical, emotional, cognitive, and social functions. On the other hand, melatonin has been shown to induce electroencephalographic abnormalities in patients with temporal lobe epilepsy and increase seizure activity in neurologically disabled children. The hormone showed very low toxicity in clinical practice. The reported adverse effects (nightmares, hypotension, and sleep disorders) were rare and mild. However, more placebo-controlled, double-blind randomized clinical trials are neede
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RILUZOLE ENHANCES THE ANTISEIZURE ACTION OF CONVENTIONAL ANTIEPILEPTIC DRUGS AGAINST Pentetrazole-INDUCED CONVULSIONS IN MICE
2004Co-Authors: Stanislaw J Czuczwar, Kinga K Borowicz, Andrzej Sêkowski, Edyta Drelewska, J. Czuczwar, Pol J. PharmacolAbstract:Riluzole enhances the antiseizure action of conventional antiepileptic drugs against Pentetrazole-induced seizures in mice. K.K. BOROWICZ
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influence of sib 1893 a selective mglur5 receptor antagonist on the anticonvulsant activity of conventional antiepileptic drugs in two models of experimental epilepsy
Polish Journal of Pharmacology, 2003Co-Authors: Kinga K Borowicz, Barbara Piskorska, Jarogniew J łuszczki, Stanislaw J CzuczwarAbstract:: SIB 1893, a non-competitive antagonist of group I metabotropic glutamate receptor subtype 5, administered at doses ranging from 0.25 to 10 mg/kg, failed to influence Pentetrazole-induced convulsions in mice. Moreover, SIB 1893 (10 and 20 mg/kg) did not affect the protective action of valproate, ethosuximide, phenobarbital and clonazepam in this test. Similarly, the mGluR5 antagonist did not modulate the antiseizure activity of carbamazepine, diphenylhydantoin and phenobarbital against maximal electroshock in mice. The combined treatment of SIB 1893 with conventional antiepileptic drugs did not lead to motor impairment. Long-term memory disturbances were observed only in the case of the combination of SIB 1893 with phenobarbital.
Sylwia Fidecka - One of the best experts on this subject based on the ideXlab platform.
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Lack of interaction between the behavioral effects of ketamine and benzodiazepines
2014Co-Authors: Sylwia Fidecka, Ewa Pirogowicz, In Mice S. Fidecka, Pol J. Pharmacol, Correspondence S. FideckaAbstract:The effect of co-administration of ketamine at the sub-effective dose with diazepam, chlordiazepoxide and clonazepam on their antinociceptive and protective efficacy against Pentetrazole-induced seizures were studied in mice. Ketamine alone produces dose-dependent antinociception manifested as reduction in the number of writhing episodes evoked by acetic acid. In the writhing test, the antinociceptive effects of the threshold doses of diazepam, chlordiazepoxide or clonazepam were not changed by ketamine, whereas that of morphine was intensified by ketamine. In the hot plate test, slight antinociceptive effects of the threshold dose of diazepam, but not that of chlordiazepoxide (except the results at 120 min of observation), were significantly intensified by ketamine vs ketamine alone. Ketamine alone was able to protect mice, in the dose-related manner, against Pentetrazole-induced seizures. The anticonvulsant effects of the threshold doses of diazepam, chlordiazepoxide and clonazepam were not changed by ketamine. These findings indicate that co-administration of ketamine (at the sub-effective dose) with diazepam, chlordiazepoxide and clonazepam (at non-effective doses) resulted in an intensification of neither antinociceptive nor protective effect against Pentetrazole-induced seizures in mice. These data seem to indicate the lack of interaction between ketamine and benzodiazepines with respect to their antinociceptive and anticonvulsant efficacy
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STUDY ON THE INFLUENCE OF POTENT INHIBITORS OF NEURONAL NITRIC OXIDE SYNTHASE ON THE ANTINOCICEPTIVE AND ANTICONVULSANT ACTIVITY OF BENZODIAZEPINES IN MICE
2014Co-Authors: Pol J. Pharmacol, Sylwia FideckaAbstract:Study on the influence of potent inhibitors of neuronal nitric oxide synthase on the antinociceptive and anticonvulsant activity of benzodiazepines in mice. S. FIDECKA, Pol. J. Pharmacol., 2003, 55, 193–201. The influence of 1-(2-trifluoromethylphenyl)imidazole (TRIM) and 3-bromo-7-nitroindazole (3-Br-7-NI), potent and relatively selective inhibitors of neuronal nitric oxide (NO) synthase, on the antinociceptive and anticonvulsive effects of diazepam and clonazepam was investigated in mice. The effects were assessed in the writhing test and Pentetrazole-induced seizures, respectively. The antinociceptive effects of the threshold doses of diazepam (1 mg/kg) and clonazepam (0.0375 mg/kg) were significantly increased by TRIM (7.5 mg/kg) but not by 3-Br-7-NI (10 mg/kg). L-arginine (125 mg/kg) was able to reverse the effects produced by co-administration of TRIM (7.5 mg/kg) with diazepam (1 mg/kg), and also of TRIM (7.5 mg/kg) with clonazepam (0.0375 mg/kg). Protective efficacy of the threshold dose (0.05 mg/kg) of diazepam against Pentetrazole-induced tonic convulsions and death was significantly increased by TRIM (25 mg/kg) but not by 3-Br-7-NI (10 and 100 mg/kg). TRIM (25 mg/kg) intensified the protective efficacy of the threshold dose (0.005 mg/kg) of clonazepam, but the effect was not reversed by L-arginine (125 mg/kg). The present results seem to confirm, at least partly, participation of NO in antinociceptive and anticonvulsant effects of benzodiazepines, and point to TRIM as a better tool than 3-Br-7NI for examination of the role of NO in behavioral studies
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Fidecka S: Role of nitric oxide in anticonvulsant effects of benzodiazepines in mice
2014Co-Authors: Sylwia Talarek, Sylwia FideckaAbstract:The influence of nitric oxide (NO) on anticonvulsant activity of diazepam and clonazepam was examined in the Pentetrazole- and electroshockinduced seizure models in mice. Protective efficacy of the threshold dose of diazepam against Pentetrazole-induced clonic and tonic seizures, and death was significantly increased by N /-nitro-L-arginine methyl ester hydrochloride (L-NAME) while 7-nitroindazole (7-NI) was slightly less effective. The above intensifying effect of L-NAME on antiepileptic activity of diazepam was reversed by L-arginine, a substrate for NO formation, but not by D-arginine. Methylene blue, the guanylate cyclase inhibitor, increased the protective efficacy of diazepam and clonazepam in the Pentetrazole-induced seizures. 7-NI was able to potentiate the protective efficacy of diazepam and clonazepam in electroshock-induced tonic hindlimb extension. These findings suggest that the cGMP/NO system may participate in antiepileptic effects of benzodiazepines. Key words: nitric oxide, benzodiazepines, seizures, mic
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the benzodiazepine withdrawal signs in mice
2006Co-Authors: Joanna Listos, Danuta Malec, Sylwia FideckaAbstract:The aim of the present experiment was to assess the involvement of adenosine receptor antagonists in benzodiazepine (BDZ) withdrawal signs, observed as the seizure susceptibility in mice. The discontinuation of chronic treatment with temazepam or diazepam decreased seizure threshold (one of BDZ withdrawal signs). The concomitant application of subconvulsive dose of Pentetrazole (55.0 mg/kg) with low dose of flumazenil (5.0 mg/kg) – a BDZ receptor antagonist, immediately induced BDZ withdrawal signs in these animals. The non-selective adenosine receptor antagonist (caffeine), and the selective adenosine A1 receptor antagonist (DPCPX), injected 15 min before the application of Pentetrazole and flumazenil, were able to intensify BDZ withdrawal signs in mice. The most apparent effects were observed after administration of DPCPX, indicating that the adenosine A1 receptor may play a more important role in these effects. The obtained data demonstrate that the adenosinergic system is involved in BDZ withdrawal signs in mice, and adenosine A1 receptor plays an important role in this process. Key words: temazepam, diazepam, BDZ withdrawal signs, adenosine receptor antagonist