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[PMID]:28239856
[Au] Autor:Wilkes E; McConaghy FF; Thompson RL; Dawson K; Sangster NC; Hughes KJ
[Ad] Endereço:School of Animal and Veterinary Sciences, Charles Sturt University, Wagga Wagga, New South Wales, Australia.
[Ti] Título:Efficacy of a morantel-abamectin combination for the treatment of resistant ascarids in foals.
[So] Source:Aust Vet J;95(3):85-88, 2017 Mar.
[Is] ISSN:1751-0813
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: This study was performed to investigate the efficacy of a morantel-abamectin combination for the treatment of macrocyclic lactone (ML)-resistant Parascaris spp. infections in foals. METHODS: Foals on five properties with a Parascaris faecal egg count (FEC) > 50 eggs per gram were used to estimate the FEC reduction (FECR) and efficacy of the anthelmintic combination. RESULTS & CONCLUSION: On all properties, resistance to ivermectin and abamectin was present and the Parascaris FECR in foals administered the morantel-abamectin combination was > 99%, indicating that this combination effectively controlled ML-resistant parasites.
[Mh] Termos MeSH primário: Antinematódeos/uso terapêutico
Infecções por Ascaridida/veterinária
Ascaridoidea/efeitos dos fármacos
Doenças dos Cavalos/tratamento farmacológico
Ivermectina/análogos & derivados
Morantel/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Antinematódeos/administração & dosagem
Infecções por Ascaridida/tratamento farmacológico
Infecções por Ascaridida/parasitologia
Combinação de Medicamentos
Resistência a Medicamentos
Doenças dos Cavalos/parasitologia
Cavalos/parasitologia
Ivermectina/administração & dosagem
Ivermectina/uso terapêutico
Morantel/administração & dosagem
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Antinematodal Agents); 0 (Drug Combinations); 5U8924T11H (abamectin); 70288-86-7 (Ivermectin); 7NJ031HAX5 (Morantel)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170323
[Lr] Data última revisão:
170323
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170228
[St] Status:MEDLINE
[do] DOI:10.1111/avj.12559


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[PMID]:26625142
[Au] Autor:Courtot E; Charvet CL; Beech RN; Harmache A; Wolstenholme AJ; Holden-Dye L; O'Connor V; Peineau N; Woods DJ; Neveu C
[Ad] Endereço:INRA, UMR1282 Infectiologie et Santé Publique, Nouzilly, France.
[Ti] Título:Functional Characterization of a Novel Class of Morantel-Sensitive Acetylcholine Receptors in Nematodes.
[So] Source:PLoS Pathog;11(12):e1005267, 2015 Dec.
[Is] ISSN:1553-7374
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Acetylcholine receptors are pentameric ligand-gated channels involved in excitatory neuro-transmission in both vertebrates and invertebrates. In nematodes, they represent major targets for cholinergic agonist or antagonist anthelmintic drugs. Despite the large diversity of acetylcholine-receptor subunit genes present in nematodes, only a few receptor subtypes have been characterized so far. Interestingly, parasitic nematodes affecting human or animal health possess two closely related members of this gene family, acr-26 and acr-27 that are essentially absent in free-living or plant parasitic species. Using the pathogenic parasitic nematode of ruminants, Haemonchus contortus, as a model, we found that Hco-ACR-26 and Hco-ACR-27 are co-expressed in body muscle cells. We demonstrated that co-expression of Hco-ACR-26 and Hco-ACR-27 in Xenopus laevis oocytes led to the functional expression of an acetylcholine-receptor highly sensitive to the anthelmintics morantel and pyrantel. Importantly we also reported that ACR-26 and ACR-27, from the distantly related parasitic nematode of horses, Parascaris equorum, also formed a functional acetylcholine-receptor highly sensitive to these two drugs. In Caenorhabditis elegans, a free-living model nematode, we demonstrated that heterologous expression of the H. contortus and P. equorum receptors drastically increased its sensitivity to morantel and pyrantel, mirroring the pharmacological properties observed in Xenopus oocytes. Our results are the first to describe significant molecular determinants of a novel class of nematode body wall muscle AChR.
[Mh] Termos MeSH primário: Proteínas de Helminto/metabolismo
Nematoides/metabolismo
Receptores Colinérgicos/metabolismo
[Mh] Termos MeSH secundário: Animais
Anti-Helmínticos/farmacologia
Ascaridoidea/genética
Ascaridoidea/metabolismo
Sequência de Bases
Haemonchus/genética
Haemonchus/metabolismo
Proteínas de Helminto/genética
Hibridização In Situ
Dados de Sequência Molecular
Morantel/farmacologia
Nematoides/genética
Técnicas de Patch-Clamp
Filogenia
Reação em Cadeia da Polimerase
Receptores Colinérgicos/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anthelmintics); 0 (Helminth Proteins); 0 (Receptors, Cholinergic); 7NJ031HAX5 (Morantel)
[Em] Mês de entrada:1604
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151202
[St] Status:MEDLINE
[do] DOI:10.1371/journal.ppat.1005267


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[PMID]:24373904
[Au] Autor:Chrisman PA; Podair JI; Jobe EM; Levandoski MM
[Ad] Endereço:Department of Chemistry, Programs in Biological Chemistry and Neuroscience, Grinnell College, 1116 8th Avenue, Grinnell, IA 50112, United States.
[Ti] Título:Intra-subunit flexibility underlies activation and allosteric modulation of neuronal nicotinic acetylcholine receptors.
[So] Source:Neuropharmacology;79:420-31, 2014 Apr.
[Is] ISSN:1873-7064
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Allosteric modulation is a general feature of nicotinic acetylcholine receptors, yet the structural components and movements important for conversions among functional states are not well understood. In this study, we examine the communication between the binding sites for agonist and the modulator morantel (Mor) of neuronal α3ß2 receptors, measuring evoked currents of receptors expressed in Xenopus oocytes with the two-electrode voltage-clamp method. We hypothesized that movement along an interface of ß sheets connecting the agonist and modulator sites is necessary for allosteric modulation. To address this, we created pairs of substituted cysteines that span the cleft formed where the outer ß sheet meets the ß sheet constituting the (-)-face of the α3 subunit; the three pairs were L158C-A179C, L158C-G181C and L158C-K183C. Employing a disulfide trapping approach in which bonds are formed between neighboring cysteines under oxidation conditions, we found that oxidation treatments decreased the amplitude of currents evoked by either the agonist (ACh) or co-applied agonist and modulator (ACh + Mor), by as much as 51%, consistent with the introduced bond decreasing channel efficacy. Reduction treatment increased evoked currents up to 89%. The magnitude of the oxidation effects depended on whether agonists were present during oxidation and on the cysteine pair. Additionally, the cysteine mutations themselves decreased Mor potentiation, implicating these residues in modulation. Our findings suggest that these ß sheets in the α3 subunit move with respect to each other during activation and modulation, and the residues studied highlight the contribution of this intramolecular allosteric pathway to receptor function.
[Mh] Termos MeSH primário: Receptores Nicotínicos/metabolismo
[Mh] Termos MeSH secundário: Acetilcolina/metabolismo
Regulação Alostérica/efeitos dos fármacos
Regulação Alostérica/fisiologia
Sequência de Aminoácidos
Animais
Sítios de Ligação/efeitos dos fármacos
Sítios de Ligação/fisiologia
Colinérgicos/farmacologia
Peróxido de Hidrogênio/farmacologia
Potenciais da Membrana/efeitos dos fármacos
Potenciais da Membrana/fisiologia
Modelos Moleculares
Morantel/farmacologia
Mutação
Oxidantes/farmacologia
Oxirredução/efeitos dos fármacos
Estrutura Secundária de Proteína
Ratos
Receptores Nicotínicos/genética
Xenopus laevis
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Cholinergic Agents); 0 (Oxidants); 0 (Receptors, Nicotinic); 0 (nicotinic receptor alpha3beta2); 7NJ031HAX5 (Morantel); BBX060AN9V (Hydrogen Peroxide); N9YNS0M02X (Acetylcholine)
[Em] Mês de entrada:1412
[Cu] Atualização por classe:161019
[Lr] Data última revisão:
161019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:131231
[St] Status:MEDLINE


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[PMID]:22425209
[Au] Autor:Ho C; Lee WO; Wong YT
[Ad] Endereço:Analytical and Advisory Services Division, Government Laboratory, 7/F Ho Man Tin Government Offices, Ho Man Tin, Kowloon, Hong Kong Special Administrative Region.
[Ti] Título:Determination of N-methyl-1,3-propanediamine in bovine muscle by liquid chromatography with triple quadrupole and ion trap tandem mass spectrometry detection.
[So] Source:J Chromatogr A;1235:103-14, 2012 Apr 27.
[Is] ISSN:1873-3778
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Morantel, pyrantel and their drug-related metabolites in food of animal-origin are regulated as sum of residues which may be hydrolysed to N-methyl-1,3-propanediamine (NMPA). In this study, an isotope dilution liquid chromatography tandem mass spectrometry (LC-MS/MS) method with pentafluoropropionic acid anhydride (PFPA) derivatization was developed for the determination of NMPA in bovine muscle. A stable isotope labeled internal standard N-methyl-d(3)-3,3'-d(2)-propane-1,3-diamine (NMPA-d(5)) was synthesized as internal standard. NMPA was derivatized with PFPA to form an N,N'-bis (pentafluoroacyl) derivative (NMPA-PFPA) and analyzed by liquid chromatography triple quadrupole mass spectrometry (LC-QqQ-MS/MS) and liquid chromatography ion trap mass spectrometry (LC-IT-MS/MS) using negative ion electrospray ionization (ESI). Chromatographic behavior of several perfluorocarboxylic acid anhydride derivatives of NMPA and other structurally related diamines on C-18 and perfluorophenyl (PFP) columns was studied. Conversion of the parent drugs to NMPA under various hydrolysis conditions was evaluated. In addition, comparison of the matrix effect and linearity with isotopically labeled internal standard (I.S.) and analogous I.S. were performed and investigated. The method was validated using fortified bovine muscle samples. The apparent recovery (obtained after correction with an isotopically labeled I.S.) was between 89% and 97% and repeatability was less than 10%. The lowest LOD and LOQ (0.42 and 1.39µg/kg, respectively) were obtained with LC-QqQ-MS/MS.
[Mh] Termos MeSH primário: Poluentes Ocupacionais do Ar/análise
Diaminas/análise
Músculos/química
[Mh] Termos MeSH secundário: Animais
Antinematódeos/análise
Bovinos
Cromatografia Líquida/métodos
Fluorcarbonetos/química
Limite de Detecção
Morantel/análise
Pirantel/análise
Espectrometria de Massas em Tandem/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Air Pollutants, Occupational); 0 (Antinematodal Agents); 0 (Diamines); 0 (Fluorocarbons); 422-64-0 (perfluoropropionic acid); 4QIH0N49E7 (Pyrantel); 7NJ031HAX5 (Morantel); I98I2UEC03 (3-dimethylaminopropylamine)
[Em] Mês de entrada:1205
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120320
[St] Status:MEDLINE
[do] DOI:10.1016/j.chroma.2012.02.060


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[PMID]:22064677
[Au] Autor:Cesa LC; Higgins CA; Sando SR; Kuo DW; Levandoski MM
[Ad] Endereço:Department of Chemistry, Grinnell College, Grinnell, Iowa, USA.
[Ti] Título:Specificity determinants of allosteric modulation in the neuronal nicotinic acetylcholine receptor: a fine line between inhibition and potentiation.
[So] Source:Mol Pharmacol;81(2):239-49, 2012 Feb.
[Is] ISSN:1521-0111
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:We are interested in the allosteric modulation of neuronal nicotinic acetylcholine receptors (nAChRs). We have postulated that the anthelmintic morantel (Mor) positively modulates (potentiates) rat α3ß2 receptors through a site located at the ß(+)/α(-) interface that is homologous to the canonical agonist site (J Neurosci 29:8734-8742, 2009). On this basis, we aimed to determine the site specificity by studying differences in modulation between α3ß2 and α4ß2 receptors. We also compared modulation by Mor with that of the related compound oxantel (Oxa). Whereas Mor and Oxa each potentiated α3ß2 receptors 2-fold at saturating acetylcholine (ACh) concentrations, Mor had no effect on α4ß2 receptors, and Oxa inhibited ACh-evoked responses. The inhibition was noncompetitive, but not due to open channel block. Furthermore, the nature and extent of modulation did not depend on subunit stoichiometry. We studied six positions at the α(-) interface that differ between α3 and α4. Two positions (α3Ile57 and α3Thr115) help mediate the effects of the modulators but do not seem to contribute to specificity. Mutations in two others (α3Leu107 and α3Ile117) yielded receptors with appreciable α4-character; that is, Mor potentiation was reduced compared with wild-type α3ß2 control and Oxa inhibition was evident. A fifth position (α3Glu113) was unique in that it discriminated between the two compounds, showing no change in Mor potentiation from control but substantial Oxa inhibition. Our work has implications for rational drug design for nicotinic receptors and sheds light on mechanisms of allosteric modulation in nAChRs, especially the subtle differences between potentiation and inhibition.
[Mh] Termos MeSH primário: Sítio Alostérico
Desenho de Drogas
Receptores Nicotínicos/metabolismo
[Mh] Termos MeSH secundário: Regulação Alostérica
Animais
Anti-Helmínticos
Morantel
Mutação
Agonistas Nicotínicos/farmacologia
Antagonistas Nicotínicos/farmacologia
Subunidades Proteicas
Pirantel/análogos & derivados
Ratos
Receptores Nicotínicos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anthelmintics); 0 (Nicotinic Agonists); 0 (Nicotinic Antagonists); 0 (Protein Subunits); 0 (Receptors, Nicotinic); 4QIH0N49E7 (Pyrantel); 7NJ031HAX5 (Morantel); 94AJJ30D9E (oxantel)
[Em] Mês de entrada:1205
[Cu] Atualização por classe:161019
[Lr] Data última revisão:
161019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:111109
[St] Status:MEDLINE
[do] DOI:10.1124/mol.111.076059


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[PMID]:19587280
[Au] Autor:Seo S; Henry JT; Lewis AH; Wang N; Levandoski MM
[Ad] Endereço:Department of Chemistry, Grinnell College, Grinnell, Iowa 50112, USA.
[Ti] Título:The positive allosteric modulator morantel binds at noncanonical subunit interfaces of neuronal nicotinic acetylcholine receptors.
[So] Source:J Neurosci;29(27):8734-42, 2009 Jul 08.
[Is] ISSN:1529-2401
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:We are interested in the positive allosteric modulation of neuronal nicotinic acetylcholine (ACh) receptors and have recently shown that the anthelmintic compound morantel potentiates by enhancing channel gating of the alpha3beta2 subtype. Based on the demonstration that morantel-elicited currents were inhibited by the classic ACh competitor dihydro-beta-erythroidine in a noncompetitive manner and that morantel still potentiates at saturating concentrations of agonist (Wu et al., 2008), we hypothesized that morantel binds at the noncanonical beta2(+)/alpha3(-) subunit interface. In the present study, we created seven cysteine-substituted subunits by site-directed mutagenesis, choosing residues in the putative morantel binding site with the aid of structural homology models. We coexpressed the mutant subunits and their respective wild-type partners in Xenopus oocytes and characterized the morantel potentiation of ACh-evoked currents, as well as morantel-evoked currents, before and after treatment with a variety of methanethiosulfonate (MTS)-based compounds, using voltage-clamp recordings. The properties of four of the seven mutants, two residues on each side of the interface, were changed by MTS treatments. Coapplication with ACh enhanced the extent of MTS modification for alpha3A106Cbeta2 and alpha3beta2S192C receptors. The activities of two mutants, alpha3T115Cbeta2 and alpha3beta2T150C, were dramatically altered by MTS modification. For alpha3beta2T150C, while peak current amplitudes were reduced, potentiation was enhanced. For alpha3T115Cbeta2, both current amplitudes and potentiation were reduced. MTS modification and morantel were mutually inhibitory: MTS treatment decreased morantel-evoked currents and morantel decreased the rate of MTS modification. We conclude that the four residues showing MTS effects contribute to the morantel binding site.
[Mh] Termos MeSH primário: Morantel/metabolismo
Neurônios/metabolismo
Subunidades Proteicas/metabolismo
Receptores Nicotínicos/metabolismo
[Mh] Termos MeSH secundário: Regulação Alostérica/efeitos dos fármacos
Regulação Alostérica/genética
Animais
Potenciais Evocados/efeitos dos fármacos
Potenciais Evocados/genética
Feminino
Morantel/farmacologia
Neurônios/efeitos dos fármacos
Neurônios/fisiologia
Ligação Proteica/efeitos dos fármacos
Ligação Proteica/genética
Subunidades Proteicas/genética
Subunidades Proteicas/fisiologia
Ratos
Receptores Nicotínicos/genética
Receptores Nicotínicos/fisiologia
Xenopus laevis
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Protein Subunits); 0 (Receptors, Nicotinic); 0 (nicotinic receptor alpha3beta2); 7NJ031HAX5 (Morantel)
[Em] Mês de entrada:0908
[Cu] Atualização por classe:161122
[Lr] Data última revisão:
161122
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090710
[St] Status:MEDLINE
[do] DOI:10.1523/JNEUROSCI.1859-09.2009


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[PMID]:19506073
[Au] Autor:Bartos M; Price KL; Lummis SC; Bouzat C
[Ad] Endereço:Instituto de Investigaciones Bioquímicas, UNS-CONICET, Bahía Blanca 8000, Argentina.
[Ti] Título:Glutamine 57 at the complementary binding site face is a key determinant of morantel selectivity for {alpha}7 nicotinic receptors.
[So] Source:J Biol Chem;284(32):21478-87, 2009 Aug 07.
[Is] ISSN:0021-9258
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Nicotinic receptors (AChRs) play key roles in synaptic transmission. We explored activation of neuronal alpha7 and mammalian muscle AChRs by morantel and oxantel. Our results revealed a novel action of morantel as a high efficacy and more potent agonist than ACh of alpha7 receptors. The EC(50) for activation by morantel of both alpha7 and alpha7-5HT(3A) receptors is 7-fold lower than that determined for ACh. The minimum morantel concentration required to activate alpha7-5HT(3A) channels is 6-fold lower than that of ACh, and activation episodes are more prolonged than in the presence of ACh. By contrast, oxantel is a weak agonist of alpha7 and alpha7-5HT(3A), and both drugs are very low efficacy agonists of muscle AChRs. The replacement of Gln(57) in alpha7 by glycine, which is found in the equivalent position of the muscle AChR, decreases the efficacy for activation and turns morantel into a partial agonist. The reverse mutation in the muscle AChR (epsilonG57Q) increases 7-fold the efficacy of morantel. The mutations do not affect activation by ACh or oxantel, indicating that this position is selective for morantel. In silico studies show that the tetrahydropyrimidinyl group, common to both drugs, is close to Trp(149) of the principal face of the binding site, whereas the other cyclic group is proximal to Gln(57) of the complementary face in morantel but not in oxantel. Thus, position 57 at the complementary face is a key determinant of the high selectivity of morantel for alpha7. These results provide new information for further progress in drug design.
[Mh] Termos MeSH primário: Glutamina/metabolismo
Morantel/metabolismo
Receptores Nicotínicos/metabolismo
[Mh] Termos MeSH secundário: Sítios de Ligação
Relação Dose-Resposta a Droga
Desenho de Drogas
Eletrofisiologia/métodos
Seres Humanos
Potenciais da Membrana
Modelos Biológicos
Modelos Químicos
Morantel/farmacologia
Músculos/metabolismo
Mutagênese Sítio-Dirigida
Mutação
Pirantel/análogos & derivados
Pirantel/metabolismo
Pirantel/farmacologia
Receptor Nicotínico de Acetilcolina alfa7
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Chrna7 protein, human); 0 (Receptors, Nicotinic); 0 (alpha7 Nicotinic Acetylcholine Receptor); 0RH81L854J (Glutamine); 4QIH0N49E7 (Pyrantel); 7NJ031HAX5 (Morantel); 94AJJ30D9E (oxantel)
[Em] Mês de entrada:0909
[Cu] Atualização por classe:170922
[Lr] Data última revisão:
170922
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090610
[St] Status:MEDLINE
[do] DOI:10.1074/jbc.M109.013797


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[PMID]:18811226
[Au] Autor:Jensen J; Diao X; Hansen AD
[Ad] Endereço:Danish National Environmental Research Institute, Aarhus University, P.O. Box 314, Vejlsøvej 25, DK-8600 Silkeborg, Denmark. jje@dmu.dk
[Ti] Título:Single- and two-species tests to study effects of the anthelmintics ivermectin and morantel and the coccidiostatic monensin on soil invertebrates.
[So] Source:Environ Toxicol Chem;28(2):316-23, 2009 Feb.
[Is] ISSN:0730-7268
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Soil invertebrates in arable land are potentially exposed to veterinary medicines excreted by husbandry. The toxicity of three widely used pharmaceuticals was therefore investigated with the use of common soil invertebrates exposed in the laboratory in single- or two-species test system. The anthelmintic morantel did not cause significant mortality to either Folsomia fimetaria or Enchytraeus crypticus even at the highest tested concentration of 900 mg kg(-1) dry soil. The coccidiostatic monensin affected the reproduction of F. fimetaria and E. crypticus with soil concentrations estimated to cause a 10% effect at values of approximately 109 and 71.8 mg kg(-1) dry soil, respectively, but caused no mortality to adult. The anthelmintic ivermectin did not affect the survival of adult Hypoaspis aculeifer. Reproduction of H. aculeifer declined approximately 45% in response to ivermectin exposure of 5 mg kg(-1) dry soil. Ivermectin was highly toxic to F. fimetaria and affected the survival of adults with soil concentrations estimated to cause a 50% mortality at values of 5.3 mg kg(-1) dry soil in the single-species test system and 0.14 mg kg(-1) dry soil in the two-species test system. Reproduction of F. fimetaria was reduced by ivermectin with 10% effective concentration at 0.19 mg kg(-1) dry soil in the single-species test system and 0.02 mg kg(-1) dry soil in two-species test system. It was shown that species interactions may influence the response of test organisms to toxic substances. The data from this study and previously published data showed that, whereas ivermectin is likely to pose a risk to soil-dwelling invertebrates, adverse effects of morantel and monensin are unlikely to occur as a result of residue excretion from treated farm animals.
[Mh] Termos MeSH primário: Anti-Helmínticos/toxicidade
Invertebrados/efeitos dos fármacos
Ivermectina/toxicidade
Morantel/toxicidade
Solo
[Mh] Termos MeSH secundário: Animais
Especificidade da Espécie
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anthelmintics); 0 (Soil); 70288-86-7 (Ivermectin); 7NJ031HAX5 (Morantel)
[Em] Mês de entrada:0905
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080925
[St] Status:MEDLINE
[do] DOI:10.1897/08-069.1


  9 / 182 MEDLINE  
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[PMID]:18458055
[Au] Autor:Wu TY; Smith CM; Sine SM; Levandoski MM
[Ad] Endereço:Department of Chemistry, Grinnell College, Grinnell, Iowa 50112, USA.
[Ti] Título:Morantel allosterically enhances channel gating of neuronal nicotinic acetylcholine alpha 3 beta 2 receptors.
[So] Source:Mol Pharmacol;74(2):466-75, 2008 Aug.
[Is] ISSN:1521-0111
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:We studied allosteric potentiation of rat alpha3beta2 neuronal nicotinic acetylcholine receptors (nAChRs) by the anthelmintic compound morantel. Macroscopic currents evoked by acetylcholine (ACh) from nAChRs expressed in Xenopus laevis oocytes increase up to 8-fold in the presence of low concentrations of morantel (< or =10 microM); the magnitude of the potentiation depends on both agonist and modulator concentrations. It is noteworthy that the potentiated currents exceed the maximum currents achieved by saturating (millimolar) concentrations of agonist. Studies of macroscopic currents elicited by prolonged drug applications (100-300 s) indicate that morantel does not increase alpha3beta2 receptor activity by reducing slow (> or =1 s) desensitization. Instead, using outside-out patch-clamp recordings, we demonstrate that morantel increases the frequency of single-channel openings and alters the bursting characteristics of the openings in a manner consistent with enhanced channel gating; these results quantitatively explain the macroscopic current potentiation. Morantel is a very weak agonist alone, but we show that the classic competitive antagonist dihydro-beta-erythroidine inhibits morantel-evoked currents noncompetitively, indicating that morantel does not bind to the canonical ACh binding sites.
[Mh] Termos MeSH primário: Anti-Helmínticos/farmacologia
Ativação do Canal Iônico/efeitos dos fármacos
Morantel/farmacologia
Neurônios/efeitos dos fármacos
Receptores Nicotínicos/fisiologia
[Mh] Termos MeSH secundário: Regulação Alostérica/efeitos dos fármacos
Regulação Alostérica/fisiologia
Animais
Feminino
Ativação do Canal Iônico/fisiologia
Morantel/química
Neurônios/fisiologia
Ratos
Receptores Nicotínicos/química
Xenopus laevis
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anthelmintics); 0 (Receptors, Nicotinic); 0 (nicotinic receptor alpha3beta2); 7NJ031HAX5 (Morantel)
[Em] Mês de entrada:0808
[Cu] Atualização por classe:161122
[Lr] Data última revisão:
161122
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080507
[St] Status:MEDLINE
[do] DOI:10.1124/mol.107.044388


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[PMID]:18333693
[Au] Autor:Escher BI; Berger C; Bramaz N; Kwon JH; Richter M; Tsinman O; Avdeef A
[Ad] Endereço:Swiss Federal Institute of Aquatic Science and Technology, Eawag, 8600 Dübendorf, Switzerland. escher@eawag.ch
[Ti] Título:Membrane-water partitioning, membrane permeability, and baseline toxicity of the parasiticides ivermectin, albendazole, and morantel.
[So] Source:Environ Toxicol Chem;27(4):909-18, 2008 Apr.
[Is] ISSN:0730-7268
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A comparative hazard assessment of the antiparasitics ivermectin, albendazole, and morantel was performed, with a particular focus on bioavailability and uptake into biological membranes. The experimentally determined liposome-water distribution ratio at pH 7 (D(lipw) (pH 7)) of the positively charged morantel was 100 L/kg lipid. The D(lipw) (pH 7) of albendazole was 3,000 L/kg lipid. The membrane permeability determined with the parallel artificial membrane permeability assay was consistent with predictions from a quantitative structure-activity relationship (QSAR) for morantel but 14-fold lower than predicted for albendazole, which can be rationalized because neutral albendazole is, in fact, zwitterionic and the large dipole moment hinders permeation through hydrophobic membranes. An unusually large molecule, ivermectin was suspected to show decreased bioaccumulation because of its bulkiness, but experimental determination of solubility showed that it was 40-fold less soluble than expected from a QSAR between solubility and the octanol-water partition coefficient. In contrast, its membrane permeability appeared to be typical for a compound of the given hydrophobicity, but it was not possible to determine the membrane-water partition coefficient because of its low solubility and high affinity to the dialysis membrane of the experimental device. The D(lipw) (pH 7) for ivermectin of 2,700 L/kg lipid was calculated with a QSAR model. Morantel and albendazole were baseline toxicants in the bioluminescence inhibition test with Vibrio fischeri and a test for inhibition of photosynthesis in green algae. Only ivermectin exhibited a specific effect toward algae, but the excess toxicity was not very pronounced and might be biased by the uncertainty of the estimated hydrophobicity descriptor. Overall, we did not find any unexpected effect on nontarget endpoints.
[Mh] Termos MeSH primário: Albendazol/toxicidade
Antiparasitários/toxicidade
Permeabilidade da Membrana Celular
Ivermectina/toxicidade
Morantel/toxicidade
[Mh] Termos MeSH secundário: Albendazol/química
Albendazol/farmacocinética
Animais
Antiparasitários/química
Antiparasitários/farmacocinética
Relação Dose-Resposta a Droga
Estabilidade de Medicamentos
Peixes/metabolismo
Ivermectina/química
Ivermectina/farmacocinética
Lipossomos/química
Morantel/química
Morantel/farmacocinética
Relação Quantitativa Estrutura-Atividade
Solubilidade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antiparasitic Agents); 0 (Liposomes); 70288-86-7 (Ivermectin); 7NJ031HAX5 (Morantel); F4216019LN (Albendazole)
[Em] Mês de entrada:0804
[Cu] Atualização por classe:161018
[Lr] Data última revisão:
161018
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080313
[St] Status:MEDLINE
[do] DOI:10.1897/07-427.1



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