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M. Kršiak - One of the best experts on this subject based on the ideXlab platform.
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The synergistic interaction between rilmenidine and paracetamol in the Writhing Test in mice
Naunyn-Schmiedeberg's Archives of Pharmacology, 2009Co-Authors: M. Soukupová, Tomas Dolezal, M. KršiakAbstract:The aim of the study was to ascertain antinociceptive effects of rilmenidine, a second-generation imidazoline-alpha-2-adrenoreceptor agonist, and to see whether rilmenidine was able to increase the analgesic effects of paracetamol in the Writhing Test in mice. An acetic acid (0.7%) solution was injected into the peritoneal cavity and the number of writhes was counted. The influence on locomotor performance was Tested using the rotarod Test. Rilmenidine, paracetamol, and rilmenidine–paracetamol fixed-ratio combinations produced dose-dependent antinociceptive effects. ED_50 values were estimated for the individual drugs and an isobologram was constructed. The derived theoretical additive ED_50 value for the rilmenidine–paracetamol combination was 109.23 ± 35.05 mg/kg. This value was significantly greater than the observed ED_50 value which was 56.35 ± 20.86 mg/kg, indicating a synergistic interaction. Rilmenidine did not impair motor coordination, as measured by the rotarod Test, at antinociceptive and higher doses.
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The synergistic interaction between rilmenidine and paracetamol in the Writhing Test in mice
Naunyn-Schmiedeberg's Archives of Pharmacology, 2009Co-Authors: M. Soukupová, Tomas Dolezal, M. KršiakAbstract:The aim of the study was to ascertain antinociceptive effects of rilmenidine, a second-generation imidazoline-alpha-2-adrenoreceptor agonist, and to see whether rilmenidine was able to increase the analgesic effects of paracetamol in the Writhing Test in mice. An acetic acid (0.7%) solution was injected into the peritoneal cavity and the number of writhes was counted. The influence on locomotor performance was Tested using the rotarod Test. Rilmenidine, paracetamol, and rilmenidine–paracetamol fixed-ratio combinations produced dose-dependent antinociceptive effects. ED_50 values were estimated for the individual drugs and an isobologram was constructed. The derived theoretical additive ED_50 value for the rilmenidine–paracetamol combination was 109.23 ± 35.05 mg/kg. This value was significantly greater than the observed ED_50 value which was 56.35 ± 20.86 mg/kg, indicating a synergistic interaction. Rilmenidine did not impair motor coordination, as measured by the rotarod Test, at antinociceptive and higher doses.
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Synergistic interaction between rilmenidine and ibuprofen in the Writhing Test in mice.
Neuro endocrinology letters, 2009Co-Authors: M. Soukupová, Tomas Dolezal, M. KršiakAbstract:OBJECTIVES: The aim of the study was to ascertain whether rilmenidine, a second generation imidazoline-alpha-2-adrenoreceptor agonist, is able to increase analgesic effects of ibuprofen in the Writhing Test in mice. Experimental studies combining these agents have not yet been published. METHODS: An acetic acid (0.7%) solution was injected into the peritoneal cavity and the number of writhes was counted. The influence on locomotor performance was Tested using the rotarod Test. RESULTS: Rilmenidine, ibuprofen, and rilmenidine-ibuprofen fixed-ratio combinations produced dose-dependent antinociceptive effects. ED 50 values were estimated for the individual drugs and an isobologram was constructed. The derived theoretical additive ED 50 value for the rilmenidine-ibuprofen combination was 34.00 ± 9.39 mg/kg. This value was significantly greater than the observed ED 50 value which was 18.07 ± 5.41 mg/kg, indicating a synergistic interaction. Rilmenidine did not impair motor coordination, as measured by the rotarod Test, at antinociceptive and higher doses. CONCLUSIONS: The present results suggest that rilmenidine enhances the analgesic activity of ibuprofen. If rilmenidine produces antinociception in humans, then the synergistic antinociception of rilmenidine with ibuprofen could offer therapeutic advantage for clinical treatment of pain.
M. Soukupová - One of the best experts on this subject based on the ideXlab platform.
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The synergistic interaction between rilmenidine and paracetamol in the Writhing Test in mice
Naunyn-Schmiedeberg's Archives of Pharmacology, 2009Co-Authors: M. Soukupová, Tomas Dolezal, M. KršiakAbstract:The aim of the study was to ascertain antinociceptive effects of rilmenidine, a second-generation imidazoline-alpha-2-adrenoreceptor agonist, and to see whether rilmenidine was able to increase the analgesic effects of paracetamol in the Writhing Test in mice. An acetic acid (0.7%) solution was injected into the peritoneal cavity and the number of writhes was counted. The influence on locomotor performance was Tested using the rotarod Test. Rilmenidine, paracetamol, and rilmenidine–paracetamol fixed-ratio combinations produced dose-dependent antinociceptive effects. ED_50 values were estimated for the individual drugs and an isobologram was constructed. The derived theoretical additive ED_50 value for the rilmenidine–paracetamol combination was 109.23 ± 35.05 mg/kg. This value was significantly greater than the observed ED_50 value which was 56.35 ± 20.86 mg/kg, indicating a synergistic interaction. Rilmenidine did not impair motor coordination, as measured by the rotarod Test, at antinociceptive and higher doses.
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The synergistic interaction between rilmenidine and paracetamol in the Writhing Test in mice
Naunyn-Schmiedeberg's Archives of Pharmacology, 2009Co-Authors: M. Soukupová, Tomas Dolezal, M. KršiakAbstract:The aim of the study was to ascertain antinociceptive effects of rilmenidine, a second-generation imidazoline-alpha-2-adrenoreceptor agonist, and to see whether rilmenidine was able to increase the analgesic effects of paracetamol in the Writhing Test in mice. An acetic acid (0.7%) solution was injected into the peritoneal cavity and the number of writhes was counted. The influence on locomotor performance was Tested using the rotarod Test. Rilmenidine, paracetamol, and rilmenidine–paracetamol fixed-ratio combinations produced dose-dependent antinociceptive effects. ED_50 values were estimated for the individual drugs and an isobologram was constructed. The derived theoretical additive ED_50 value for the rilmenidine–paracetamol combination was 109.23 ± 35.05 mg/kg. This value was significantly greater than the observed ED_50 value which was 56.35 ± 20.86 mg/kg, indicating a synergistic interaction. Rilmenidine did not impair motor coordination, as measured by the rotarod Test, at antinociceptive and higher doses.
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Synergistic interaction between rilmenidine and ibuprofen in the Writhing Test in mice.
Neuro endocrinology letters, 2009Co-Authors: M. Soukupová, Tomas Dolezal, M. KršiakAbstract:OBJECTIVES: The aim of the study was to ascertain whether rilmenidine, a second generation imidazoline-alpha-2-adrenoreceptor agonist, is able to increase analgesic effects of ibuprofen in the Writhing Test in mice. Experimental studies combining these agents have not yet been published. METHODS: An acetic acid (0.7%) solution was injected into the peritoneal cavity and the number of writhes was counted. The influence on locomotor performance was Tested using the rotarod Test. RESULTS: Rilmenidine, ibuprofen, and rilmenidine-ibuprofen fixed-ratio combinations produced dose-dependent antinociceptive effects. ED 50 values were estimated for the individual drugs and an isobologram was constructed. The derived theoretical additive ED 50 value for the rilmenidine-ibuprofen combination was 34.00 ± 9.39 mg/kg. This value was significantly greater than the observed ED 50 value which was 18.07 ± 5.41 mg/kg, indicating a synergistic interaction. Rilmenidine did not impair motor coordination, as measured by the rotarod Test, at antinociceptive and higher doses. CONCLUSIONS: The present results suggest that rilmenidine enhances the analgesic activity of ibuprofen. If rilmenidine produces antinociception in humans, then the synergistic antinociception of rilmenidine with ibuprofen could offer therapeutic advantage for clinical treatment of pain.
Tomas Dolezal - One of the best experts on this subject based on the ideXlab platform.
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The synergistic interaction between rilmenidine and paracetamol in the Writhing Test in mice
Naunyn-Schmiedeberg's Archives of Pharmacology, 2009Co-Authors: M. Soukupová, Tomas Dolezal, M. KršiakAbstract:The aim of the study was to ascertain antinociceptive effects of rilmenidine, a second-generation imidazoline-alpha-2-adrenoreceptor agonist, and to see whether rilmenidine was able to increase the analgesic effects of paracetamol in the Writhing Test in mice. An acetic acid (0.7%) solution was injected into the peritoneal cavity and the number of writhes was counted. The influence on locomotor performance was Tested using the rotarod Test. Rilmenidine, paracetamol, and rilmenidine–paracetamol fixed-ratio combinations produced dose-dependent antinociceptive effects. ED_50 values were estimated for the individual drugs and an isobologram was constructed. The derived theoretical additive ED_50 value for the rilmenidine–paracetamol combination was 109.23 ± 35.05 mg/kg. This value was significantly greater than the observed ED_50 value which was 56.35 ± 20.86 mg/kg, indicating a synergistic interaction. Rilmenidine did not impair motor coordination, as measured by the rotarod Test, at antinociceptive and higher doses.
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The synergistic interaction between rilmenidine and paracetamol in the Writhing Test in mice
Naunyn-Schmiedeberg's Archives of Pharmacology, 2009Co-Authors: M. Soukupová, Tomas Dolezal, M. KršiakAbstract:The aim of the study was to ascertain antinociceptive effects of rilmenidine, a second-generation imidazoline-alpha-2-adrenoreceptor agonist, and to see whether rilmenidine was able to increase the analgesic effects of paracetamol in the Writhing Test in mice. An acetic acid (0.7%) solution was injected into the peritoneal cavity and the number of writhes was counted. The influence on locomotor performance was Tested using the rotarod Test. Rilmenidine, paracetamol, and rilmenidine–paracetamol fixed-ratio combinations produced dose-dependent antinociceptive effects. ED_50 values were estimated for the individual drugs and an isobologram was constructed. The derived theoretical additive ED_50 value for the rilmenidine–paracetamol combination was 109.23 ± 35.05 mg/kg. This value was significantly greater than the observed ED_50 value which was 56.35 ± 20.86 mg/kg, indicating a synergistic interaction. Rilmenidine did not impair motor coordination, as measured by the rotarod Test, at antinociceptive and higher doses.
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Synergistic interaction between rilmenidine and ibuprofen in the Writhing Test in mice.
Neuro endocrinology letters, 2009Co-Authors: M. Soukupová, Tomas Dolezal, M. KršiakAbstract:OBJECTIVES: The aim of the study was to ascertain whether rilmenidine, a second generation imidazoline-alpha-2-adrenoreceptor agonist, is able to increase analgesic effects of ibuprofen in the Writhing Test in mice. Experimental studies combining these agents have not yet been published. METHODS: An acetic acid (0.7%) solution was injected into the peritoneal cavity and the number of writhes was counted. The influence on locomotor performance was Tested using the rotarod Test. RESULTS: Rilmenidine, ibuprofen, and rilmenidine-ibuprofen fixed-ratio combinations produced dose-dependent antinociceptive effects. ED 50 values were estimated for the individual drugs and an isobologram was constructed. The derived theoretical additive ED 50 value for the rilmenidine-ibuprofen combination was 34.00 ± 9.39 mg/kg. This value was significantly greater than the observed ED 50 value which was 18.07 ± 5.41 mg/kg, indicating a synergistic interaction. Rilmenidine did not impair motor coordination, as measured by the rotarod Test, at antinociceptive and higher doses. CONCLUSIONS: The present results suggest that rilmenidine enhances the analgesic activity of ibuprofen. If rilmenidine produces antinociception in humans, then the synergistic antinociception of rilmenidine with ibuprofen could offer therapeutic advantage for clinical treatment of pain.
Qonita Nim011611133231 - One of the best experts on this subject based on the ideXlab platform.
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UJI EFEK ANALGESIK EKSTRAK ETANOL RIMPANG ZINGIBER CASSUMUNAR ROXB. PADA MENCIT MUS MUSCULUS DENGAN METODE Writhing Test
2019Co-Authors: Qonita Nim011611133231Abstract:Latar Belakang : Data menyebutkan bahwa 95% responden yang berasal dari 32 negara pernah mengalami rasa nyeri selama hidup mereka. Penggunaan obat analgesik menunjukkan angka yang tinggi, masyarakat juga mulai mencari alternatif obat tradisional yang memiliki efek analgesik. Zingiber cassumunar Roxb. merupakan salah satu tanaman yang biasa digunakan sebagai obat tradisional karena bekerja menurunkan PGE2 dan ekspresi COX-2. Namun penggunaannya secara luas masih sedikit dipelajari. Oleh karena itu, disusun rencana penelitian untuk mengkaji penggunaan ekstrak rimpang Zingiber cassumunar Roxb. sebagai analgesik pada mencit dengan metode Writhing Test. Metode : Penelitian ini adalah penelitian eksperimental dengan postTest only control design. Sampel penelitian terdiri dari 25 mencit terbagi dalam tiga kelompok perlakuan ekstrak rimpang Zingiber cassumunar Roxb. dosis 100 mg/kg, 200 mg/kg, 400 mg/kg, kelompok kontrol negatif aquades, serta kelompok kontrol positif aspirin. Efek analgesik didapatkan dengan melakukan Writhing Test. Hasil : Hasil penelitian menunjukkan bahwa ekstrak rimpang pada dosis 100 mg/kg dan 200 mg/kg secara signifikan menurunkan jumlah geliat pada mencit dibandingkan kelompok kontrol, dengan presentase proteksi geliat sebesar 49,53% dan 57,01%, sebanding dengan proteksi geliat kelompok positif aspirin, yaitu 53,27%. Kesimpulan : Terdapat efek analgesik pada penggunaan ekstrak rimpang Zingiber cassumunar Roxb., serta dosis ekstrak rimpang yang efektif mengurangi rasa nyeri yaitu sebesar 100 mg/kg dan 200 mg/kg
G. Guillaumet - One of the best experts on this subject based on the ideXlab platform.
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Substituted pyrido[3,2-b]oxazin-3(4H)-ones: synthesis and evaluation of antinociceptive activity
Bioorganic & medicinal chemistry, 1998Co-Authors: Laurence Savelon, M.‐c. Viaud, Jean-guy Bizot-espiard, Bruno Pfeiffer, Pierre Renard, Daniel-henri Caignard, G. GuillaumetAbstract:Abstract A new series of N -substituted pyrido[3,2- b ]oxazinones has been synthesized, pharmacologically evaluated, and compared with acetyl salicylic acid. The compound with the maximal combination of safety and analgesic efficacy was 4-{3-[4-(4-fluorophenyl-1-piperazinyl)propyl]}-2 H -pyrido[3,2- b ]-1,4-oxazin-3(4 H )-one ( 6c ) with ED 50 values of 12.5 mg/kg po (mouse: phenylquinone Writhing Test) and 27.8 mg/kg po (rat: acetic acid Writhing Test), respectively. Compound 6c proved to be more active than aspirin with a safety index of 5.1.
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N-substituted aminohydroxypyridines as potential non-opioid analgesic agents.
Bioorganic & medicinal chemistry, 1995Co-Authors: M.‐c. Viaud, P. Jamoneau, Jean-guy Bizot-espiard, Bruno Pfeiffer, Pierre Renard, Daniel-henri Caignard, G. Adam, G. GuillaumetAbstract:A series of new N-substituted aminohydroxypyridines have been synthesized, pharmacologically evaluated and compared with their N-substituted oxazolopyridone analogs. The compound with the maximal combination of safety and analgesic efficacy was 3-[2-[4-(4-fluorophenyl)-1-piperazinyl]ethyl]amino-2-hydroxypyridine (compound 10a), with ED50 values 0.4 mg kg−1 po (mouse: phenylquinone Writhing Test) and 0.5 mg kg−1 po (rat: acetic acid Writhing Test). Compound 10a possesses a potent non-opioid antinociceptive activity with moderate anti-inflammatory properties.
