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[PMID]:27736935
[Au] Autor:Wang S; Zhang S; Xu C; Barron A; Galiano F; Patel D; Lee YJ; Caldwell GA; Caldwell KA; Witt SN
[Ad] Endereço:Department of Biochemistry and Molecular Biology, Louisiana State University Health Sciences Center, Shreveport, LA, United States of America.
[Ti] Título:Chemical Compensation of Mitochondrial Phospholipid Depletion in Yeast and Animal Models of Parkinson's Disease.
[So] Source:PLoS One;11(10):e0164465, 2016.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:We have been investigating the role that phosphatidylethanolamine (PE) and phosphatidylcholine (PC) content plays in modulating the solubility of the Parkinson's disease protein alpha-synuclein (α-syn) using Saccharomyces cerevisiae and Caenorhabditis elegans. One enzyme that synthesizes PE is the conserved enzyme phosphatidylserine decarboxylase (Psd1/yeast; PSD-1/worms), which is lodged in the inner mitochondrial membrane. We previously found that decreasing the level of PE due to knockdown of Psd1/psd-1 affects the homeostasis of α-syn in vivo. In S. cerevisiae, the co-occurrence of low PE and α-syn in psd1Δ cells triggers mitochondrial defects, stress in the endoplasmic reticulum, misprocessing of glycosylphosphatidylinositol-anchored proteins, and a 3-fold increase in the level of α-syn. The goal of this study was to identify drugs that rescue this phenotype. We screened the Prestwick library of 1121 Food and Drug Administration-approved drugs using psd1Δ + α-syn cells and identified cyclosporin A, meclofenoxate hydrochloride, and sulfaphenazole as putative protective compounds. The protective activity of these drugs was corroborated using C. elegans in which α-syn is expressed specifically in the dopaminergic neurons, with psd-1 depleted by RNAi. Worm populations were examined for dopaminergic neuron survival following psd-1 knockdown. Exposure to cyclosporine, meclofenoxate, and sulfaphenazole significantly enhanced survival at day 7 in α-syn-expressing worm populations whereby 50-55% of the populations displayed normal neurons, compared to only 10-15% of untreated animals. We also found that all three drugs rescued worms expressing α-syn in dopaminergic neurons that were deficient in the phospholipid cardiolipin following cardiolipin synthase (crls-1) depletion by RNAi. We discuss how these drugs might block α-syn pathology in dopaminergic neurons.
[Mh] Termos MeSH primário: Mitocôndrias/metabolismo
Doença de Parkinson/patologia
Fosfatidilcolinas/metabolismo
Fosfatidiletanolaminas/metabolismo
Saccharomyces cerevisiae/metabolismo
[Mh] Termos MeSH secundário: Animais
Caenorhabditis elegans
Proteínas de Caenorhabditis elegans/antagonistas & inibidores
Proteínas de Caenorhabditis elegans/genética
Proteínas de Caenorhabditis elegans/metabolismo
Carboxiliases/antagonistas & inibidores
Carboxiliases/genética
Carboxiliases/metabolismo
Ciclosporina/farmacologia
Modelos Animais de Doenças
Neurônios Dopaminérgicos/efeitos dos fármacos
Neurônios Dopaminérgicos/metabolismo
Estresse do Retículo Endoplasmático/efeitos dos fármacos
Meclofenoxate/farmacologia
Proteínas de Membrana/antagonistas & inibidores
Proteínas de Membrana/genética
Proteínas de Membrana/metabolismo
Proteínas Mitocondriais/antagonistas & inibidores
Proteínas Mitocondriais/genética
Proteínas Mitocondriais/metabolismo
Doença de Parkinson/metabolismo
Substâncias Protetoras/farmacologia
Solubilidade
Sulfafenazol/farmacologia
Transferases (Outros Grupos de Fosfato Substituídos)/antagonistas & inibidores
Transferases (Outros Grupos de Fosfato Substituídos)/genética
Transferases (Outros Grupos de Fosfato Substituídos)/metabolismo
alfa-Sinucleína/química
alfa-Sinucleína/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Caenorhabditis elegans Proteins); 0 (Membrane Proteins); 0 (Mitochondrial Proteins); 0 (Phosphatidylcholines); 0 (Phosphatidylethanolamines); 0 (Protective Agents); 0 (alpha-Synuclein); 0J8L4V3F81 (Sulfaphenazole); 39382-08-6 (phosphatidylethanolamine); 83HN0GTJ6D (Cyclosporine); C76QQ2I0RG (Meclofenoxate); EC 2.7.8.- (Transferases (Other Substituted Phosphate Groups)); EC 2.7.8.- (cardiolipin synthetase); EC 4.1.1.- (Carboxy-Lyases); EC 4.1.1.- (Psd1 protein, S cerevisiae); EC 4.1.1.65 (phosphatidylserine decarboxylase)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170516
[Lr] Data última revisão:
170516
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161014
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0164465


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[PMID]:24862015
[Au] Autor:Zs-Nagy I
[Ad] Endereço:Faculty of Medicine, Medical and Health Science Center, University of Debrecen, Debrecen, Hungary.
[Ti] Título:Aging of cell membranes: facts and theories.
[So] Source:Interdiscip Top Gerontol;39:62-85, 2014.
[Is] ISSN:1662-3800
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:This chapter is intended to outline the main results of a research trend realized by the author during the last 45 years, focused on the main role played by the cell membrane in the aging process. It is a very wide field; therefore, the reader cannot expect in this limited space a detailed description, but will be given a wide, interdisciplinary insight into the main facts and theories regarding cellular aging. The central idea described here is the concept called the membrane hypothesis of aging (MHA). The history, the chemical roots, physicochemical facts, biophysical processes, as well as the obligatory biochemical consequences are all touched in by indicating the most important sources of detailed knowledge for those who are more interested in the basic biology of the aging process. This chapter covers also the available anti-aging interventions on the cell membrane by means of the centrophenoxine treatment based on the MHA. It also briefly interprets the possibilities of a just developing anti-aging method by using the recombinant human growth hormone, essential basis of which is the species specificity, and the general presence of receptors of this hormone in the plasma membrane of all types of cells.
[Mh] Termos MeSH primário: Permeabilidade da Membrana Celular/fisiologia
Membrana Celular/fisiologia
Senescência Celular/fisiologia
[Mh] Termos MeSH secundário: Animais
Eletrólitos/metabolismo
Depuradores de Radicais Livres/farmacologia
Radicais Livres/metabolismo
Hormônio do Crescimento Humano/deficiência
Hormônio do Crescimento Humano/fisiologia
Seres Humanos
Líquido Intracelular/fisiologia
Transporte de Íons/fisiologia
Meclofenoxate/farmacologia
Proteínas de Membrana/fisiologia
Modelos Biológicos
Fármacos Neuroprotetores/farmacologia
Oncogenes/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Electrolytes); 0 (Free Radical Scavengers); 0 (Free Radicals); 0 (Membrane Proteins); 0 (Neuroprotective Agents); 12629-01-5 (Human Growth Hormone); C76QQ2I0RG (Meclofenoxate)
[Em] Mês de entrada:1501
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140528
[St] Status:MEDLINE
[do] DOI:10.1159/000358900


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[PMID]:24816669
[Au] Autor:Ismagul A; Iskakova G; Harris JC; Eliby S
[Ad] Endereço:Australian Centre for Plant Functional Genomics, University of Adelaide, PMB 1, Glen Osmond, SA, Australia.
[Ti] Título:Biolistic transformation of wheat with centrophenoxine as a synthetic auxin.
[So] Source:Methods Mol Biol;1145:191-202, 2014.
[Is] ISSN:1940-6029
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Cereal crops, including bread wheat (Triticum aestivum L.), are an important staple food worldwide. With a growing global population, it is evident that current crop production will not meet the rising demands being placed on modern agriculture. Efforts to improve crop yield and stress-tolerance by traditional breeding are labor intensive, time consuming, and highly dependent upon the ability to capture existing and novel genetic variation from a restricted genetic pool. Genetic engineering of crop species is one of several alternatives to traditional breeding for the introduction of novel genetic variation. This recently established technology has proved useful for the introduction of novel traits like pest resistance and herbicide tolerance. As a universal tool for genetic transformation, the Biolistic Gene Gun allows for the genomic integration of novel gene sequences from various sources into a whole host of living organisms.In this chapter, we present a novel and detailed protocol for the Biolistic Transformation of bread wheat that uses the pharmaceutical compound, Centrophenoxine (CPX). The application of CPX as the main auxin-like plant growth regulator in cereal genetic transformation replaces the potent but more toxic herbicide 2,4-D.
[Mh] Termos MeSH primário: Biolística
Ácidos Indolacéticos/farmacologia
Meclofenoxate/farmacologia
Triticum/genética
[Mh] Termos MeSH secundário: Genes de Plantas
Engenharia Genética
Plantas Geneticamente Modificadas/genética
Transformação Genética
Triticum/crescimento & desenvolvimento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Indoleacetic Acids); C76QQ2I0RG (Meclofenoxate)
[Em] Mês de entrada:1501
[Cu] Atualização por classe:140512
[Lr] Data última revisão:
140512
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140513
[St] Status:MEDLINE
[do] DOI:10.1007/978-1-4939-0446-4_15


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[PMID]:22632051
[Au] Autor:El-Nashar RM; Abdel Ghani NT; Hassan SM
[Ad] Endereço:Chemistry Department, Faculty of Science, Cairo University, Giza, Egypt. rasha.elnashar@guc.edu.eg
[Ti] Título:Construction and performance characteristics of new ion selective electrodes based on carbon nanotubes for determination of meclofenoxate hydrochloride.
[So] Source:Anal Chim Acta;730:99-111, 2012 Jun 12.
[Is] ISSN:1873-4324
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:This work offers construction and comparative evaluation the performance characteristics of conventional polymer (I), carbon paste (II) and carbon nanotubes chemically modified carbon paste ion selective electrodes (III) for meclofenoxate hydrochloride are described. These electrodes depend mainly on the incorporation of the ion pair of meclofenoxate hydrochloride with phosphomolybdic acid (PMA) or phosphotungestic acid (PTA). They showed near Nernestian responses over usable concentration range 1.0 × 10(-5) to 1.0 × 10(-2)M with slopes in the range 55.15-59.74 mV(concentrationdecade)(-1). These developed electrodes were fully characterized in terms of their composition, response time, working concentration range, life span, usable pH and temperature range. The electrodes showed a very good selectivity for Meclo with respect to a large number of inorganic cations, sugars and in the presence of the degradation product of the drug (p-chloro phenoxy acetic acid). The standard additions method was applied to the determination of MecloCl in pure solution, pharmaceutical preparations and biological samples. Dissolution testing was also applied using the proposed sensors.
[Mh] Termos MeSH primário: Eletrodos Íon-Seletivos
Meclofenoxate/análise
Nanotubos de Carbono/química
[Mh] Termos MeSH secundário: Carbono/química
Seres Humanos
Concentração de Íons de Hidrogênio
Meclofenoxate/sangue
Meclofenoxate/urina
Molibdênio/química
Ácidos Fosfóricos/química
Ácido Fosfotúngstico/química
Polímeros/química
Potenciometria
Sensibilidade e Especificidade
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Nanotubes, Carbon); 0 (Phosphoric Acids); 0 (Polymers); 12067-99-1 (Phosphotungstic Acid); 7440-44-0 (Carbon); 81AH48963U (Molybdenum); C76QQ2I0RG (Meclofenoxate); RN225F04V1 (phosphomolybdic acid)
[Em] Mês de entrada:1210
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120529
[St] Status:MEDLINE
[do] DOI:10.1016/j.aca.2011.10.069


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[PMID]:20515527
[Au] Autor:Ni B; Zhang J; Zou J; Zhao W; Li J
[Ad] Endereço:Department of Cardiovascular and thoracic Surgery, the First Affiliated Hospital, Soochow University, Soochou, China.
[Ti] Título:A simple and sensitive HPLC method for quantification of the metabolin of meclofenoxate in human plasma.
[So] Source:J Chromatogr Sci;48(5):353-7, 2010 May-Jun.
[Is] ISSN:1945-239X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A simple and sensitive high-performance liquid chromatographic method was developed for quantification of the metabolin of meclofenoxate, chlorophenoxyacetic acid, in human plasma. Ibuprofen was used as an internal standard. The present method used protein precipitation for extraction of chlorophenoxyacetic acid from human plasma. Separation was carried out on a reversed-phase C(18) column. The column effluent was monitored by UV detection at 254 nm. The mobile phase was a mixture of methanol and water containing 1.0% glacial acetic acid (70:30 v/v) at a flow rate of 1.0 mL/min. The column temperature was 20 degrees C. This method was linear over the range of 0.047-28.20 microg/mL with a regression coefficient greater than 0.99. The mean recovery of chlorophenoxyacetic acid and IS were (79.54 +/- 6.33)% and (78.48 +/- 2.14)%, respectively, and the method was found to be precise, accurate, and specific during the study. The method was successfully applied for pharmacokinetic study of chlorophenoxyacetic acid in human.
[Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/métodos
Meclofenoxate/metabolismo
[Mh] Termos MeSH secundário: Acetatos/sangue
Acetatos/metabolismo
Seres Humanos
Meclofenoxate/sangue
Sensibilidade e Especificidade
[Pt] Tipo de publicação:EVALUATION STUDIES; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Acetates); C76QQ2I0RG (Meclofenoxate); YRC253429Q (phenoxyacetic acid)
[Em] Mês de entrada:1011
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:100603
[St] Status:MEDLINE


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[PMID]:19375462
[Au] Autor:Verma R; Nehru B
[Ad] Endereço:Department of Biophysics, Panjab University, Chandigarh 160014, India.
[Ti] Título:Effect of centrophenoxine against rotenone-induced oxidative stress in an animal model of Parkinson's disease.
[So] Source:Neurochem Int;55(6):369-75, 2009 Nov.
[Is] ISSN:1872-9754
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Oxidative stress has been implicated in the etiology of Parkinson's disease (PD). The important biochemical features of PD, being profound deficit in dopamine (DA) content, reduced glutathione (GSH), and enhanced lipid peroxidation (LPO) in dopaminergic (DA-ergic) neurons resulting in oxidative stress, mitochondrial dysfunction and apoptosis. Rotenone-induced neurotoxicity is a well acknowledged preclinical model for studying PD in rodents as it produces selective DA-ergic neuronal degeneration. In our previous study, we have shown that chronic administration of rotenone to rats is able to produce motor dysfunction, which increases progressively with rotenone treatment and centrophenoxine (CPH) co-treatment is able to attenuate these motor defects. The present study was carried out to evaluate the antioxidant potential of CPH against rotenone-induced oxidative stress. Chronic administration of rotenone to SD rats resulted in marked oxidative damage in the midbrain region compared to other regions of the brain and CPH co-treatment successfully attenuated most of these changes. CPH significantly attenuated rotenone-induced depletion in DA, GSH and increase in LPO levels. In addition, the drug prevented the increase in nitric oxide (NO) and citrulline levels and also enhanced the activity of catalase and superoxide dismutase (SOD). Histological analysis carried out using hematoxylin and eosin staining has indicated severe damage to mid brain in comparison to cortex and cerebellum and this damage is attenuated by CPH co-treatment. Our results strongly indicate the possible therapeutic potential of centrophenoxine as an antioxidant in Parkinson's disease and other movement disorders where oxidative stress is a key player in the disease process.
[Mh] Termos MeSH primário: Meclofenoxate/farmacologia
Estresse Oxidativo/efeitos dos fármacos
Doença de Parkinson/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Antiparkinsonianos/farmacologia
Cerebelo/efeitos dos fármacos
Cerebelo/patologia
Cerebelo/fisiopatologia
Córtex Cerebral/efeitos dos fármacos
Córtex Cerebral/patologia
Córtex Cerebral/fisiopatologia
Citoproteção/efeitos dos fármacos
Citoproteção/fisiologia
Modelos Animais de Doenças
Masculino
Fármacos Neuroprotetores/farmacologia
Estresse Oxidativo/fisiologia
Doença de Parkinson/metabolismo
Doença de Parkinson/fisiopatologia
Ratos
Ratos Sprague-Dawley
Rotenona/antagonistas & inibidores
Rotenona/toxicidade
Substância Negra/efeitos dos fármacos
Substância Negra/patologia
Substância Negra/fisiopatologia
Desacopladores/antagonistas & inibidores
Desacopladores/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antiparkinson Agents); 0 (Neuroprotective Agents); 0 (Uncoupling Agents); 03L9OT429T (Rotenone); C76QQ2I0RG (Meclofenoxate)
[Em] Mês de entrada:0910
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090421
[St] Status:MEDLINE
[do] DOI:10.1016/j.neuint.2009.04.001


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[PMID]:18840370
[Au] Autor:Zou JJ; Ji HJ; Wu DW; Yao J; Hu Q; Xiao DW; Wang GJ
[Ad] Endereço:Department of Clinical Pharmacology, Nanjing First Hospital of Nanjing Medical University, Nanjing, China.
[Ti] Título:Bioequivalence and pharmacokinetic comparison of a single 200-mg dose of meclofenoxate hydrochloride capsule and tablet formulations in healthy Chinese adult male volunteers: a randomized sequence, open-label, two-period crossover study.
[So] Source:Clin Ther;30(9):1651-7, 2008 Sep.
[Is] ISSN:0149-2918
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Meclofenoxate hydrochloride is a psychostimulant in the nootropic agent group available in capsule and tablet formulations approved for traumatic cataphora, alcoholic poisoning, anoxia neonatorum, and children's enuresis in China. Although these 2 generic formulations are marketed in China, information regarding their pharmacokinetics and bioequivalence in humans has not been published. OBJECTIVE: The aim of this study was to compare the pharmacokinetic properties and bioequivalence of the capsule (test) and tablet (reference) formulations of meclofenoxate hydrochloride 200 mg in healthy Chinese volunteers. METHODS: This single-dose, randomized-sequence, open-label, 2-period crossover study was performed at the Nanjing First Hospital of Nanjing Medical University, Nanjing, China. Eligible subjects were healthy male volunteers who were randomly assigned at a 1:1 ratio to receive a single 200-mg dose of the test or reference formulation, followed by a 1-week washout period and administration of the alternate formulation. The study drugs were administered after a 12-hour overnight fast. As a prodrug, meclofenoxate is hydrolyzed into 4-chlorophenoxyacetic acid and is not detected in plasma. The active metabolite of meclofenoxate, chlorophenoxyacetic acid, was assayed using a high-performance liquid chromatography method. For analysis of pharmacokinetic properties, including Cmax, AUC0-24, and AUC0-infinity, blood samples were obtained at 0.33, 0.67, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 14, and 24 hours after administration. The formulations were considered bioequivalent if the log-transformed ratios of Cmax and AUC were within the predetermined equivalence range (80%-125%) as established by the US Food and Drug Administration (FDA). Subjects were interviewed concerning the occurrence of adverse events including excitement, insomnia, lassitude, and headache. Tolerability was assessed at baseline (before administration) and at 1, 2, 6, and 12 hours after administration by monitoring vital signs and laboratory tests (hematology, blood biochemistry, hepatic function, and urinalysis). RESULTS: Twenty-four Chinese male subjects (mean [range]age,23.5[22-30]years;weight,63.3[56-68]kg; height, 171 [165-184] cm) were enrolled; all completed the study. No period or sequence effect was observed. The 90% CIs for the log-transformed ratios of chlorophenoxyacetic acid Cmax, AUC0-24, and AUC0-infinity were 95.7 to 122.9, 97.6 to 111.9, and 97.8 to 111.7, respectively (all, P>0.05). Similar results were found for the data without log-transformation. No adverse events were reported or observed during this single-dose study. CONCLUSIONS: In this small study in healthy Chinese adult male volunteers, a single 200-mg dose of the capsule formulation was found to be bioequivalent to a single 200-mg dose of the tablet formulation based on the US FDA's regulatory definition (rate and extent of absorption). Both formulations were well tolerated.
[Mh] Termos MeSH primário: Meclofenoxate/farmacocinética
Nootrópicos/farmacocinética
[Mh] Termos MeSH secundário: Adulto
Análise de Variância
Área Sob a Curva
Grupo com Ancestrais do Continente Asiático
Disponibilidade Biológica
Cápsulas/farmacocinética
China
Cromatografia Líquida de Alta Pressão
Estudos Cross-Over
Relação Dose-Resposta a Droga
Composição de Medicamentos
Tolerância a Medicamentos
Seres Humanos
Masculino
Meclofenoxate/administração & dosagem
Experimentação Humana não Terapêutica
Nootrópicos/administração & dosagem
Valores de Referência
Comprimidos/farmacocinética
Equivalência Terapêutica
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Capsules); 0 (Nootropic Agents); 0 (Tablets); C76QQ2I0RG (Meclofenoxate)
[Em] Mês de entrada:0901
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:081009
[St] Status:MEDLINE
[do] DOI:10.1016/j.clinthera.2008.09.013


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[PMID]:18652247
[Au] Autor:Salimov RM; Kovalev GI
[Ti] Título:[Effects of nicotinic cholinoreceptor ligands and nootropic drugs on the spontaneous exploratory activity in a labyrinth in mice].
[So] Source:Eksp Klin Farmakol;71(3):3-5, 2008 May-Jun.
[Is] ISSN:0869-2092
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:We have studied the effects of nicotine (0.125, 0.25, and 0.5 mg/kg) and mecamylamine (0.5, 1.5, and 3 mg/kg) in comparison to reference cognition-enhancing drugs piracetam (100 and 300 mg/kg) and meclofenoxate (20, 50, and 100 mg/kg) administered to male C57BL mice intraperitoneally 30 min prior to behavioral test. The behavioral drug effect was evaluated as influencing the activity in visiting arms of a closed plus-maze. Piracetam (300 mg/kg) and meclofenoxate (100 mg/kg) improved the exploratory activity. Mecamylamine (0.5 mg/kg) also improved the exploratory activity, while nicotine (0.5 mg/kg) deteriorated it.
[Mh] Termos MeSH primário: Comportamento Exploratório/efeitos dos fármacos
Agonistas Nicotínicos/farmacologia
Nootrópicos/farmacologia
Receptores Nicotínicos/metabolismo
[Mh] Termos MeSH secundário: Animais
Ligantes
Masculino
Mecamilamina/farmacologia
Meclofenoxate/farmacologia
Camundongos
Camundongos Endogâmicos C57BL
Nicotina/farmacologia
Piracetam/farmacologia
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Ligands); 0 (Nicotinic Agonists); 0 (Nootropic Agents); 0 (Receptors, Nicotinic); 6EE945D3OK (Mecamylamine); 6M3C89ZY6R (Nicotine); C76QQ2I0RG (Meclofenoxate); ZH516LNZ10 (Piracetam)
[Em] Mês de entrada:0808
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080726
[St] Status:MEDLINE


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[PMID]:18365480
[Au] Autor:Kovalev GI; Firstova IuIu; Salimov RM
[Ti] Título:[Effects of piracetam and meclofenoxate on the brain NMDA and nicotinic receptors in mice with different exploratory efficacy in the cross maze test].
[So] Source:Eksp Klin Farmakol;71(1):12-7, 2008 Jan-Feb.
[Is] ISSN:0869-2092
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:A population of outbred mice of the ICR strain was divided into two subpopulations according to their high (EH mice) or low (EL mice) exploratory efficacy in the closed cross maze test. In addition, the EH and EL mice differed in the number of binding sites of (i) [G-3H]-MK-801 with NMDA receptors from hippocampus and (ii) [G-3H]-nicotine with nicotine cholinoreceptors (nACh) from neocortex. A subchronic administration of the cognition enhancer piracetam (200 mg/kg, once per day for 5 days) increased by 70% the number of binding sites of NMDA receptors in the EL mice. At the same time, this treatment decreased the density of neocortical nACh receptors in both EL and EH mice (by 55% and 40%, respectively). A subchronic administration of the cognition enhancer and anti-oxidant meclofenoxate (100 mg/kg, once per day for 5 days) also decreased the density of neocortical nACh receptors in both EL and EH mice (by 48% and 20%, respectively). However, meclofenoxate also increased by 41% the number of binding sites of NMDA receptors in the EH mice.
[Mh] Termos MeSH primário: Aprendizagem em Labirinto/fisiologia
Meclofenoxate/farmacologia
Nootrópicos/farmacologia
Piracetam/farmacologia
Receptores de N-Metil-D-Aspartato/metabolismo
Receptores Nicotínicos/metabolismo
[Mh] Termos MeSH secundário: Animais
Antioxidantes/farmacologia
Hipocampo/metabolismo
Masculino
Aprendizagem em Labirinto/efeitos dos fármacos
Camundongos
Camundongos Endogâmicos ICR
Neocórtex/metabolismo
Receptores de N-Metil-D-Aspartato/agonistas
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Nootropic Agents); 0 (Receptors, N-Methyl-D-Aspartate); 0 (Receptors, Nicotinic); C76QQ2I0RG (Meclofenoxate); ZH516LNZ10 (Piracetam)
[Em] Mês de entrada:0805
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080328
[St] Status:MEDLINE


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[PMID]:18308296
[Au] Autor:Nehru B; Verma R; Khanna P; Sharma SK
[Ad] Endereço:Department of Biophysics, Panjab University, Chandigarh-160014, India. bnehru@pu.ac.in
[Ti] Título:Behavioral alterations in rotenone model of Parkinson's disease: attenuation by co-treatment of centrophenoxine.
[So] Source:Brain Res;1201:122-7, 2008 Mar 27.
[Is] ISSN:0006-8993
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Rotenone, a potent specific inhibitor of mitochondrial complex-1, appears to reproduce the behavioral features of Parkinson's disease in rats. It destroys dopaminergic neurons selectively, causing deficiency of dopamine in striatum which leads to impaired motor functions. Oxidative stress generated as a result of mitochondrial dysfunction and metabolism of dopamine has been implicated as an important factor in the etiology of Parkinson's disease. Present study explores the potential of centrophenoxine (a well known anti-aging and antioxidant drug) against rotenone induced motor dysfunction. Sprague Dawley male rats were administered with rotenone on a daily basis by subcutaneous injection of dose: 2 mg/kg body weight over a period of 35 days. Data showed impaired motor function, significant increase in catalepsy, decrease in locomotor activity and decrease in muscle activity. Dopamine content of rotenone treated animals was found to decrease significantly and lipid peroxidation was found to increase significantly in rotenone treated animals when compared with co-treated group. Co-treatment with centrophenoxine (100 mg/kg i.p. for 35 days) significantly attenuated the extent of motor dysfunction and changes in the level of dopamine and lipid peroxidation induced by rotenone toxicity. Thus, the present study provides evidence that centrophenoxine co-treatment attenuates rotenone induced motor dysfunction by virtue of its antioxidant action.
[Mh] Termos MeSH primário: Comportamento Animal/efeitos dos fármacos
Encéfalo/efeitos dos fármacos
Meclofenoxate/farmacologia
Transtornos Parkinsonianos/tratamento farmacológico
Rotenona/análogos & derivados
[Mh] Termos MeSH secundário: Animais
Antioxidantes/farmacologia
Comportamento Animal/fisiologia
Encéfalo/metabolismo
Catalepsia/induzido quimicamente
Catalepsia/tratamento farmacológico
Catalepsia/prevenção & controle
Modelos Animais de Doenças
Dopamina/metabolismo
Esquema de Medicação
Interações Medicamentosas/fisiologia
Peroxidação de Lipídeos/efeitos dos fármacos
Peroxidação de Lipídeos/fisiologia
Masculino
Atividade Motora/efeitos dos fármacos
Atividade Motora/fisiologia
Fármacos Neuroprotetores/farmacologia
Neurotoxinas/antagonistas & inibidores
Neurotoxinas/toxicidade
Estresse Oxidativo/efeitos dos fármacos
Estresse Oxidativo/fisiologia
Transtornos Parkinsonianos/metabolismo
Transtornos Parkinsonianos/fisiopatologia
Ratos
Ratos Sprague-Dawley
Rotenona/antagonistas & inibidores
Rotenona/toxicidade
Resultado do Tratamento
Desacopladores/antagonistas & inibidores
Desacopladores/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Neuroprotective Agents); 0 (Neurotoxins); 0 (Uncoupling Agents); 03L9OT429T (Rotenone); 4439-62-7 (rotenonone); C76QQ2I0RG (Meclofenoxate); VTD58H1Z2X (Dopamine)
[Em] Mês de entrada:0807
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080301
[St] Status:MEDLINE
[do] DOI:10.1016/j.brainres.2008.01.074



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