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[PMID]:28043192
[Au] Autor:Kassa J; Misik J; Hatlapatkova J; Zdarova Karasova J
[Ad] Endereço:a Department of Toxicology and Military Pharmacy, Faculty of Military Health Sciences , University of Defense , Hradec Kralove , Czech Republic.
[Ti] Título:A comparison of neuroprotective efficacy of two novel reactivators of acetylcholinesterase called K920 and K923 with the oxime K203 and trimedoxime in tabun-poisoned rats.
[So] Source:Toxicol Mech Methods;27(3):236-243, 2017 Mar.
[Is] ISSN:1537-6524
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The ability of two newly developed bispyridinium oximes (K920, K923) to reduce tabun-induced acute neurotoxic signs and symptoms was compared with the oxime K203 and trimedoxime using a functional observational battery (FOB). The neuroprotective effects of the oximes studied combined with atropine on rats poisoned with tabun at a sublethal dose (130 µg/kg i.m.; 80% of LD value) were evaluated. Tabun-induced neurotoxicity was monitored by FOB at 2 h after tabun administration. The results indicate that all tested oximes combined with atropine enable tabun-poisoned rats to survive till the end of experiment while one non-treated tabun-poisoned rat died within 2 h. Both newly developed oximes (K920, K923) combined with atropine were able to markedly decrease tabun-induced neurotoxicity in the case of sublethal poisoning although they did not eliminate all tabun-induced acute neurotoxic signs and symptoms. Their ability to decrease tabun-induced acute neurotoxicity did not prevail the neuroprotective efficacy of trimedoxime and the oxime K203. Therefore, the newly developed oximes are not suitable for the replacement of currently available oximes (especially trimedoxime) in the treatment of acute tabun poisonings.
[Mh] Termos MeSH primário: Reativadores da Colinesterase/uso terapêutico
Fármacos Neuroprotetores/uso terapêutico
Síndromes Neurotóxicas/prevenção & controle
Organofosfatos/toxicidade
Oximas/uso terapêutico
Compostos de Piridínio/uso terapêutico
Trimedoxima/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Reativadores da Colinesterase/química
Masculino
Estrutura Molecular
Fármacos Neuroprotetores/química
Síndromes Neurotóxicas/etiologia
Oximas/química
Compostos de Piridínio/química
Ratos Wistar
Trimedoxima/química
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)but-2-ene); 0 (Cholinesterase Reactivators); 0 (K920 compound); 0 (K923 compound); 0 (Neuroprotective Agents); 0 (Organophosphates); 0 (Oximes); 0 (Pyridinium Compounds); 56-97-3 (Trimedoxime); S45M750QSH (tabun)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170726
[Lr] Data última revisão:
170726
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170104
[St] Status:MEDLINE
[do] DOI:10.1080/15376516.2016.1275907


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[PMID]:26960827
[Au] Autor:Kassa J; Hatlapatková J; Zdárová Karasová J
[Ad] Endereço:Department of Toxicology and Military Pharmacy, Faculty of Military Health Sciences, University of Defense, Hradec Králové, Czech Republic. kassa@pmfhk.cz.
[Ti] Título:The Evaluation of the Potency of Newly Developed Oximes (K727, K733) and Trimedoxime to Counteract Acute Neurotoxic Effects of Tabun in Rats.
[So] Source:Acta Medica (Hradec Kralove);58(4):135-43, 2015.
[Is] ISSN:1211-4286
[Cp] País de publicação:Czech Republic
[La] Idioma:eng
[Ab] Resumo:AIM: The ability of two newly developed oximes (K727, K733) to reduce tabun-induced acute neurotoxic signs and symptoms was evaluated and compared with currently available trimedoxime in rats. METHODS: The neuroprotective effects of the oximes studied combined with atropine on Wistar rats poisoned with tabun at a lethal dose (380 µg/kg i.m.; 90% of LD50 value) were evaluated. Tabun-induced neurotoxicity was monitored by the functional observational battery consisting of 38 measurements of sensory, motor and autonomic nervous functions at 2 hours following tabun challenge. RESULTS: All tested oximes combined with atropine enable tabun-poisoned rats to survive till the end of experiment. Both newly developed oximes (K727, K733) combined with atropine were able to decrease tabun-induced neurotoxicity in the case of lethal poisoning although they did not eliminate all tabun-induced acute neurotoxic signs and symptoms. CONCLUSION: The ability of both novel bispyridinium oximes to decrease tabun-induced acute neurotoxicity was slightly lower than that of trimedoxime. Therefore, the newly developed oximes are not suitable for the replacement of commonly used oximes such as trimedoxime in the treatment of acute tabun poisonings.
[Mh] Termos MeSH primário: Inibidores da Colinesterase/toxicidade
Reativadores da Colinesterase/farmacologia
Sistema Nervoso/efeitos dos fármacos
Fármacos Neuroprotetores/farmacologia
Organofosfatos/toxicidade
Oximas/farmacologia
Compostos de Piridínio/farmacologia
Trimedoxima/farmacologia
[Mh] Termos MeSH secundário: Animais
Atropina/farmacologia
Masculino
Antagonistas Muscarínicos/farmacologia
Síndromes Neurotóxicas/tratamento farmacológico
Síndromes Neurotóxicas/etiologia
Intoxicação por Organofosfatos/tratamento farmacológico
Intoxicação por Organofosfatos/etiologia
Ratos
Ratos Wistar
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (4-(ethylcarboxyl)-2'-(hydroxyiminomethyl)-1,1'-(phenylene-1,3-diyl)-bispyridinium); 0 (Cholinesterase Inhibitors); 0 (Cholinesterase Reactivators); 0 (Muscarinic Antagonists); 0 (Neuroprotective Agents); 0 (Organophosphates); 0 (Oximes); 0 (Pyridinium Compounds); 0 (naphthylene-2,7-diyl-bis(2-hydroxyiminomethylpyridinium)); 56-97-3 (Trimedoxime); 7C0697DR9I (Atropine); S45M750QSH (tabun)
[Em] Mês de entrada:1607
[Cu] Atualização por classe:161021
[Lr] Data última revisão:
161021
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160311
[St] Status:MEDLINE
[do] DOI:10.14712/18059694.2016.6


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[PMID]:25225130
[Au] Autor:Kassa J; Sepsova V; Tumova M; Horova A; Musilek K
[Ad] Endereço:Department of Toxicology and Military Pharmacy, Faculty of Military Health Sciences, Hradec Kralove, Czech Republic.
[Ti] Título:A comparison of the reactivating and therapeutic efficacy of two newly developed oximes (k727 and k733) with oxime k203 and trimedoxime in tabun-poisoned rats and mice.
[So] Source:Basic Clin Pharmacol Toxicol;116(4):367-71, 2015 Apr.
[Is] ISSN:1742-7843
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The reactivating and therapeutic efficacy of three original bispyridinium oximes (K727, K733 and K203) and one currently available oxime (trimedoxime) was evaluated in tabun-poisoned rats and mice. The oxime-induced reactivation of tabun-inhibited acetylcholinesterase was measured in diaphragm and brain of tabun-poisoned rats. The results showed that the reactivating efficacy of two recently developed oximes (K727 and K733) does not achieve the level of the reactivation of tabun-inhibited acetylcholinesterase induced by oxime K203 and trimedoxime. While all oximes studied were able to increase the activity of tabun-inhibited acetylcholinesterase in diaphragm, oxime K733 was not able to reactivate tabun-inhibited acetylcholinesterase in the brain. The therapeutic efficacy of all oximes studied roughly corresponds to their reactivating efficacy. While both recently developed oximes were able to reduce acute toxicity of tabun less than 1.5-fold, another original oxime K203 and commonly used trimedoxime reduced the acute toxicity of tabun almost two times. In conclusion, the reactivating and therapeutic potency of both newly developed oximes does not prevail the effectiveness of oxime K203 and trimedoxime, and therefore, they are not suitable for their replacement of commonly used oximes for the antidotal treatment of acute tabun poisoning.
[Mh] Termos MeSH primário: Antídotos/uso terapêutico
Substâncias para a Guerra Química/toxicidade
Inibidores da Colinesterase/toxicidade
Reativadores da Colinesterase/uso terapêutico
Organofosfatos/toxicidade
Oximas/uso terapêutico
Compostos de Piridínio/uso terapêutico
Trimedoxima/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Atropina/farmacologia
Injeções Intramusculares
Dose Letal Mediana
Masculino
Camundongos
Parassimpatolíticos/farmacologia
Ratos
Ratos Wistar
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)but-2-ene); 0 (4-(ethylcarboxyl)-2'-(hydroxyiminomethyl)-1,1'-(phenylene-1,3-diyl)-bispyridinium); 0 (Antidotes); 0 (Chemical Warfare Agents); 0 (Cholinesterase Inhibitors); 0 (Cholinesterase Reactivators); 0 (Organophosphates); 0 (Oximes); 0 (Parasympatholytics); 0 (Pyridinium Compounds); 0 (naphthylene-2,7-diyl-bis(2-hydroxyiminomethylpyridinium)); 56-97-3 (Trimedoxime); 7C0697DR9I (Atropine); S45M750QSH (tabun)
[Em] Mês de entrada:1601
[Cu] Atualização por classe:150313
[Lr] Data última revisão:
150313
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140917
[St] Status:MEDLINE
[do] DOI:10.1111/bcpt.12327


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[PMID]:24295433
[Au] Autor:Kassa J; Sepsova V; Tumova M; Musilek K; Horova A
[Ad] Endereço:Department of Toxicology, Faculty of Military Health Sciences, Trebesska, Hradec Kralove , Czech Republic.
[Ti] Título:The evaluation of the reactivating and therapeutic efficacy of two novel oximes (K361 and K378) in comparison with the oxime K203 and trimedoxime in tabun-poisoned rats and mice.
[So] Source:Toxicol Mech Methods;24(3):173-8, 2014 Mar.
[Is] ISSN:1537-6524
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The potency of two newly developed oximes (K361 and K378) to reactivate tabun-inhibited cholinesterase and to reduce acute toxicity of tabun was compared with the oxime K203 and trimedoxime using in vivo methods. The study determining percentage of reactivation of tabun-inhibited diaphragm cholinesterase in poisoned rats showed that the reactivating efficacy of the oxime K378 is slightly lower than the reactivating potency of the oxime K203 and trimedoxime while the ability of the oxime K361 to reactivate tabun-inhibited cholinesterase is markedly lower compared with the oxime K203 and trimedoxime. In the brain, the potency of both newly developed oximes to reactivate tabun-inhibited cholinesterase was negligible. The therapeutic efficacy of both newly developed oximes roughly corresponds to their weak reactivating efficacy. Their potency to reduce acute toxicity of tabun was significantly lower compared with the oxime K203 as well as trimedoxime. In conclusion, the reactivating and therapeutic potency of both newly developed oximes does not prevail the effectiveness of the oxime K203 and trimedoxime and, therefore, they are not suitable for their replacement of commonly used oximes for the treatment of acute tabun poisoning.
[Mh] Termos MeSH primário: Inibidores da Colinesterase/envenenamento
Reativadores da Colinesterase/uso terapêutico
Organofosfatos/toxicidade
Oximas/uso terapêutico
Compostos de Piridínio/uso terapêutico
Trimedoxima/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Barreira Hematoencefálica
Masculino
Camundongos
Ratos Wistar
Relação Estrutura-Atividade
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (1-(3-phenylpropyl)-4-hydroxyiminomethylpyridinium); 0 (1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)but-2-ene); 0 (4-(1-amino-1-hydroxyiminomethyl)-4'-hydroxyiminomethyl-1,1'-(but-1,4-diyl)bispyridinium); 0 (Cholinesterase Inhibitors); 0 (Cholinesterase Reactivators); 0 (Organophosphates); 0 (Oximes); 0 (Pyridinium Compounds); 56-97-3 (Trimedoxime); S45M750QSH (tabun)
[Em] Mês de entrada:1412
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:131204
[St] Status:MEDLINE
[do] DOI:10.3109/15376516.2013.871766


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[PMID]:24065055
[Au] Autor:Gupta B; Sharma R; Singh N; Kuca K; Acharya JR; Ghosh KK
[Ad] Endereço:School of Studies in Chemistry, Pt. Ravishankar Shukla University, Raipur, 492010, CG, India.
[Ti] Título:In vitro reactivation kinetics of paraoxon- and DFP-inhibited electric eel AChE using mono- and bis-pyridinium oximes.
[So] Source:Arch Toxicol;88(2):381-90, 2014 Feb.
[Is] ISSN:1432-0738
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Oxime-assisted reactivation of organophosphate (OP)-inhibited acetylcholinesterase (AChE) is a crucial step in the post-inhibitory treatment of OP intoxication. The limited efficacy of oxime reactivators for all OP nerve agents and pesticides led to the development of various novel oximes and their thorough kinetic investigations. Hence, in the present investigation, we have tested 10 structurally different pyridinium oxime-based reactivators for their in vitro potency to reactivate paraoxon- and DFP-inhibited electric eel AChE. From structure activity relationship point of view, various oximes such as mono-quaternary (2-PAM, K100, K024) and bis-quaternary symmetric (obidoxime, TMB-4) and asymmetric (K027, K048, K203, K618, K628) oximes bearing different connecting linkers (oxybismethylene, trimethylene, propane, butane, butene, and xylene) have been studied. The observed kinetic data demonstrate that not only the position of oxime group is decisive for the increased reactivation ability of oximes, but the role of connecting linker is also significant. Oximes with aliphatic linkers are superior reactivators than the oximes with unsaturated and aromatic linkers. The optimal chain length for plausible reactivation ability for paraoxon- and DFP-inhibited AChE is 3 or 4 carbon-carbon connecting linker between prydinium rings.
[Mh] Termos MeSH primário: Inibidores da Colinesterase/farmacologia
Reativadores da Colinesterase/química
Reativadores da Colinesterase/farmacologia
Isoflurofato/toxicidade
Paraoxon/toxicidade
Compostos de Piridínio/farmacologia
[Mh] Termos MeSH secundário: Acetilcolinesterase/metabolismo
Alcenos/química
Animais
Butanos/química
Inibidores da Colinesterase/toxicidade
Reativadores da Colinesterase/farmacocinética
Electrophorus
Cinética
Cloreto de Obidoxima/química
Cloreto de Obidoxima/farmacologia
Compostos de Piridínio/química
Relação Estrutura-Atividade
Trimedoxima/química
Trimedoxima/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Alkenes); 0 (Butanes); 0 (Cholinesterase Inhibitors); 0 (Cholinesterase Reactivators); 0 (Pyridinium Compounds); 12UHW9R67N (Isoflurophate); 25167-67-3 (butylene); 3HXR312Z9M (Obidoxime Chloride); 56-97-3 (Trimedoxime); 6LV4FOR43R (butane); EC 3.1.1.7 (Acetylcholinesterase); Q9CX8P80JW (Paraoxon)
[Em] Mês de entrada:1409
[Cu] Atualização por classe:140130
[Lr] Data última revisão:
140130
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130926
[St] Status:MEDLINE
[do] DOI:10.1007/s00204-013-1136-z


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[PMID]:23647829
[Au] Autor:Kassa J; Misik J; Karasova JZ
[Ad] Endereço:Department of Toxicology, Faculty of Military Health Sciences, Hradec Kralove, Czech Republic. kassa@pmfhk.cz
[Ti] Título:Evaluation of the potency of two novel bispyridinium oximes (K456, K458) in comparison with oxime K203 and trimedoxime to counteract tabun-induced neurotoxicity in rats.
[So] Source:Basic Clin Pharmacol Toxicol;113(3):201-8, 2013 Sep.
[Is] ISSN:1742-7843
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The ability of two newly developed bispyridinium oximes (K456, K458) to reduce tabun-induced acute neurotoxic signs and symptoms was compared with oxime K203 and trimedoxime using the functional observational battery. The neuroprotective effects of the oximes studied combined with atropine on rats poisoned with tabun at a sublethal dose (200 µg/kg i.m.; 85% of LD50 value) were evaluated. Tabun-induced neurotoxicity was monitored by the functional observational battery and automatic measurement of motor activity at 2 hr after tabun challenge. The results indicate that all tested oximes combined with atropine enable tabun-poisoned rats to survive till the end of experiment. Both newly developed oximes (K456, K458) combined with atropine were able to decrease tabun-induced neurotoxicity in the case of sublethal poisonings although they did not eliminate all tabun-induced acute neurotoxic signs and symptoms. Their ability to decrease tabun-induced acute neurotoxicity was slightly higher than that of trimedoxime and oxime K203, but the difference in neuroprotective efficacy among all oximes studied is not large enough to make a decision about replacement of commonly used oximes (especially trimedoxime and obidoxime) in the treatment of acute tabun poisonings.
[Mh] Termos MeSH primário: Fármacos Neuroprotetores/farmacologia
Síndromes Neurotóxicas/prevenção & controle
Oximas/farmacologia
Compostos de Piridínio/farmacologia
[Mh] Termos MeSH secundário: Animais
Atropina/farmacologia
Substâncias para a Guerra Química/toxicidade
Masculino
Organofosfatos/toxicidade
Ratos
Ratos Wistar
Trimedoxima/farmacologia
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)but-2-ene); 0 (Chemical Warfare Agents); 0 (K456 compound); 0 (K458 compound); 0 (Neuroprotective Agents); 0 (Organophosphates); 0 (Oximes); 0 (Pyridinium Compounds); 56-97-3 (Trimedoxime); 7C0697DR9I (Atropine); S45M750QSH (tabun)
[Em] Mês de entrada:1311
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130508
[St] Status:MEDLINE
[do] DOI:10.1111/bcpt.12083


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[PMID]:23461011
[Au] Autor:Iudin MA; Lantukhov DV; Vengerovich NG
[Ti] Título:[Studying kinetics of oxime-induced reactivation of malathion-inhibited cholinesterase].
[So] Source:Eksp Klin Farmakol;76(1):21-4, 2013.
[Is] ISSN:0869-2092
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:The kinetics of oxime-induced reactivation of malathion-inhibited cholinesterase has been experimentally studied in vitro. It is shown that oximes do not restore the activity of inhibited butyrylcholinesterase. Acetylcholinesterase reactivation peak (5-mins long) was found to take place upon introduction of dipyroxime (32.5%), pralidoxime (18%), carboxyme (16%) at a concentration of 2.5 x 10(-4) mol/l or toxogonine (26%) at a concentration of 5 x 10(-4) mol/l. Toxogonine demonstrated the maximum affinity to phosphorylated enzyme, while dipyroxime is characterized by a high reactivity with respect to oxime. Significant reactivating ability of these preparations (kR -2300 mol(-1) min(-1) makes them promising solution for the treatment of malathion intoxication.
[Mh] Termos MeSH primário: Acetilcolinesterase/química
Antídotos/química
Butirilcolinesterase/química
Inibidores da Colinesterase/química
Reativadores da Colinesterase/química
Malation/química
[Mh] Termos MeSH secundário: Animais
Ativação Enzimática
Eritrócitos/química
Eritrócitos/enzimologia
Cavalos
Cinética
Cloreto de Obidoxima/química
Compostos de Pralidoxima/química
Soluções
Torpedo
Trimedoxima/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antidotes); 0 (Cholinesterase Inhibitors); 0 (Cholinesterase Reactivators); 0 (Pralidoxime Compounds); 0 (Solutions); 3HXR312Z9M (Obidoxime Chloride); 56-97-3 (Trimedoxime); EC 3.1.1.7 (Acetylcholinesterase); EC 3.1.1.8 (Butyrylcholinesterase); P7MU9UTP52 (pralidoxime); U5N7SU872W (Malathion)
[Em] Mês de entrada:1304
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130307
[St] Status:MEDLINE


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[PMID]:22901042
[Au] Autor:Kassa J; Sepsova V; Musilek K; Horova A
[Ad] Endereço:Department of Toxicology, Faculty of Military Health Sciences , Trebesska 1575, 500 01 Hradec Kralove, Czech Republic. kassa@pmfhk.cz
[Ti] Título:The evaluation of the reactivating and therapeutic efficacy of three novel bispyridinium oximes (K454, K456, K458) in comparison with the oxime K203 and trimedoxime in tabun-poisoned rats and mice.
[So] Source:Toxicol Mech Methods;23(2):94-8, 2013 Feb.
[Is] ISSN:1537-6524
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The potency of three newly developed bispyridinium compounds (K454, K456, K458) to reactivate tabun-inhibited acetylcholinesterase and reduce tabun-induced lethal toxic effects was compared with the oxime K203 and trimedoxime using in vivo methods. The study determining percentage of reactivation of tabun-inhibited diaphragm and brain acetylcholinesterase in poisoned rats showed that the reactivating efficacy of all newly developed oximes is comparable with K203 but lower than the reactivating potency of trimedoxime in diaphragm. In the brain, their potency to reactivate tabun-inhibited acetylcholinesterase is lower compared with trimedoxime and the oxime K203. All three newly developed oximes were also found to be relatively effective in reducing lethal toxic effects in tabun-poisoned mice. Their therapeutic efficacy is consistent with the therapeutic potency of the oxime K203. On the other hand, their potency to reduce acute toxicity of tabun is significantly lower compared with trimedoxime. In conclusion, the reactivating and therapeutic potency of all three newly developed oximes does not prevail the effectiveness of the oxime K203 and trimedoxime and, therefore, they are not suitable for their replacement of commonly used oximes for the treatment of acute tabun poisoning.
[Mh] Termos MeSH primário: Substâncias para a Guerra Química/envenenamento
Inibidores da Colinesterase/toxicidade
Reativadores da Colinesterase/toxicidade
Organofosfatos/toxicidade
Compostos de Piridínio/toxicidade
Trimedoxima/toxicidade
[Mh] Termos MeSH secundário: Acetilcolinesterase/metabolismo
Animais
Encéfalo/efeitos dos fármacos
Encéfalo/enzimologia
Diafragma/efeitos dos fármacos
Diafragma/enzimologia
Masculino
Camundongos
Camundongos Endogâmicos
Ratos
Ratos Wistar
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Chemical Warfare Agents); 0 (Cholinesterase Inhibitors); 0 (Cholinesterase Reactivators); 0 (Organophosphates); 0 (Pyridinium Compounds); 56-97-3 (Trimedoxime); EC 3.1.1.7 (Acetylcholinesterase); S45M750QSH (tabun)
[Em] Mês de entrada:1307
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120821
[St] Status:MEDLINE
[do] DOI:10.3109/15376516.2012.720304


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[PMID]:21717485
[Au] Autor:Karasova JZ; Chladek J; Hroch M; Josef F; Hnidkova D; Kuca K
[Ad] Endereço:Department of Public Health, Faculty of Health Sciences, Defence University, Hradec Kralove, Czech Republic. karasova@pmfhk.cz
[Ti] Título:Pharmacokinetic study of two acetylcholinesterase reactivators, trimedoxime and newly synthesized oxime K027, in rat plasma.
[So] Source:J Appl Toxicol;33(1):18-23, 2013 Jan.
[Is] ISSN:1099-1263
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:K027 [1-(4-hydroxyiminomethylpyridinium)-3-(4-carbamoylpyridinium)-propane dibromide] is a promising new reactivator of organophosphate- or organophosphonate-inhibited acetylcholinesterase (AChE) with low acute toxicity and broad spectrum efficacy. The aim of the present study was to compare the pharmacokinetics of both compounds. Male Wistar rats (body weight = 320 ± 10 g) were administered a single intramuscular dose of K027 (22.07 mg kg(-1)) and an equimolar dose of trimedoxime. Blood was collected at various time intervals until 180 min. Plasma samples were analyzed by reversed-phase HPLC with ultraviolet (UV) detection. The recovery of both oximes from the plasma was approximately 90% and a linear relationship (R(2) > 0.998) was observed between the peak areas and concentrations of calibrated standards in the range 1-100 µg ml(-1). Near-identical plasma profiles were obtained for both compounds. No differences were found in the mean ± SD values of C(max) (18.6 ± 2.5 vs 20.0 ± 6.3 µg ml(-1), P = 0.72) and AUC(0-180min) (2290 ± 304 vs 2269 ± 197 min µg ml(-1), P = 0.84). However, the percentage coefficient of variation of the first-order rate constant of absorption (k(a)) was 3-fold higher (P < 0.01) providing evidence for more erratic absorption of intramuscular trimedoxime as compared with K027. In conclusion, oxime K027 might have superior pK properties that may be translated in its faster absorption and subsequent tissue distribution.
[Mh] Termos MeSH primário: Reativadores da Colinesterase/farmacocinética
Oximas/farmacocinética
Compostos de Piridínio/farmacocinética
Trimedoxima/farmacocinética
[Mh] Termos MeSH secundário: Animais
Reativadores da Colinesterase/sangue
Cromatografia Líquida de Alta Pressão
Injeções Intramusculares
Masculino
Oximas/sangue
Compostos de Piridínio/sangue
Ratos
Ratos Wistar
Espectrofotometria Ultravioleta/métodos
Distribuição Tecidual
Trimedoxima/sangue
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (1-(4-hydroxyiminomethylpyridinium)-3-(carbamoylpyridinium) propane dibromide); 0 (Cholinesterase Reactivators); 0 (Oximes); 0 (Pyridinium Compounds); 56-97-3 (Trimedoxime)
[Em] Mês de entrada:1305
[Cu] Atualização por classe:121129
[Lr] Data última revisão:
121129
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:110701
[St] Status:MEDLINE
[do] DOI:10.1002/jat.1699


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[PMID]:22696932
[Au] Autor:Kassa J; Karasová JZ; Pavlíková R; Caisberger F; Bajgar J
[Ad] Endereço:University of Defence, Faculty of Military Health Sciences, Hradec Králové, Czech Republic. kassa@pmfhk.cz
[Ti] Título:The ability of oxime mixtures to increase the reactivating and therapeutic efficacy of antidotal treatment of cyclosarin poisoning in rats and mice.
[So] Source:Acta Medica (Hradec Kralove);55(1):27-31, 2012.
[Is] ISSN:1211-4286
[Cp] País de publicação:Czech Republic
[La] Idioma:eng
[Ab] Resumo:The reactivating and therapeutic efficacy of two combinations ofoximes (HI-6 + trimedoxime and HI-6 + K203) was compared with the effectiveness of antidotal treatment involving single oxime (HI-6, trimedoxime, K203) using in vivo methods. In vivo determined percentage of reactivation of cyclosarin-inhibited blood and tissue acetylcholinesterase in poisoned rats showed that the reactivating efficacy of both combinations of oximes is slightly higher than the reactivating efficacy of the most effective individual oxime in blood, diaphragm as well as in brain. Moreover, both combinations of oximes were found to be slightly more efficacious in the reduction of acute lethal toxic effects in cyclosarin-poisoned mice than the antidotal treatment involving single oxime. Based on the obtained data, we can conclude that the antidotal treatment involving chosen combinations of oximes brings a beneficial effect for its ability to counteract the acute poisoning with cyclosarin.
[Mh] Termos MeSH primário: Antídotos/uso terapêutico
Reativadores da Colinesterase/uso terapêutico
Compostos Organofosforados/toxicidade
[Mh] Termos MeSH secundário: Animais
Camundongos
Camundongos Endogâmicos
Oximas/uso terapêutico
Compostos de Piridínio/uso terapêutico
Ratos
Ratos Wistar
Trimedoxima/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)but-2-ene); 0 (Antidotes); 0 (Cholinesterase Reactivators); 0 (Organophosphorus Compounds); 0 (Oximes); 0 (Pyridinium Compounds); 56-97-3 (Trimedoxime); HUV88P6SJS (asoxime chloride); VM36F9N236 (cyclohexyl methylphosphonofluoridate)
[Em] Mês de entrada:1207
[Cu] Atualização por classe:161021
[Lr] Data última revisão:
161021
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120616
[St] Status:MEDLINE



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