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Pesquisa : D12.776.543.750.670 [Categoria DeCS]
Referências encontradas : 352 [refinar]
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[PMID]:28663279
[Au] Autor:Dalwadi DA; Schetz JA
[Ad] Endereço:Department of Pharmacology and Neuroscience (D.A.D., J.A.S.), Graduate School of Biomedical Sciences, Institute for Healthy Aging, Center for Neuroscience Discovery, and Department of Medical Education (J.A.S.), Texas College of Osteopathic Medicine, University of North Texas Health Science Cen-ter, Fort Worth, Texas.
[Ti] Título:Comparative Exploration of the Structure-Activity Space of Cloned -Like Octopamine Receptors from a Marine and a Terrestrial Arthropod.
[So] Source:Mol Pharmacol;92(3):297-309, 2017 Sep.
[Is] ISSN:1521-0111
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The -like octopamine receptors (OctR) are believed to be the evolutionary precursor to the vertebrate -adrenergic receptors ( -ARs) based upon sequence similarity and the ability to interact with norepinephrine and a number of compounds that bind with high affinity to -ARs. Barnacles and fruit flies are two prominent model marine and terrestrial representatives of the Arthropoda phylum, and although -like OctRs have been cloned from (BiOctR) and (DmOctR), little is known about the structure-activity space for these important species. A diverse panel of 22 probes spanning different structural classes were employed to interrogate the structure-activity of the BiOctR and DmOctR. While BiOctR and DmOctR exhibited similar functional profiles for mammalian biogenic amine G protein-coupled receptor agonists and antagonists, some ligands had dramatically different mechanisms of action. For instance, significant differences in the efficacy for some agonists were observed, including that vertebrate biogenic amines structurally related to octopamine acted as superagonists at the DmOctR but partial agonists at the BiOctR, and the two species diverged in their sensitivities to the -AR antagonist [ H]rauwolscine. Furthermore, sodium enhanced [ H]rauwolscine's interactions with the BiOctR, but not at a vertebrate -AR. Molecular mechanistic studies indicate that rauwolscine interacts with the BiOctR, DmOctR, and -adrenergic receptor at an allosteric site. In addition, compounds that acted as agonists at a cloned -like BiOctR also induced a hyperactivity response in cyprids mediated by the -like OctR, suggesting that the receptor may serve as a higher throughput proxy for discovering compounds with potential cyprid deterrent properties.
[Mh] Termos MeSH primário: Receptores de Amina Biogênica/química
Receptores de Amina Biogênica/fisiologia
Thoracica/química
[Mh] Termos MeSH secundário: Agonistas de Receptores Adrenérgicos alfa 2/farmacologia
Animais
Drosophila melanogaster
Células HEK293
Seres Humanos
Isoquinolinas/metabolismo
Naftiridinas/metabolismo
Filogenia
Receptores de Amina Biogênica/agonistas
Sódio/farmacologia
Relação Estrutura-Atividade
Thoracica/genética
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic alpha-2 Receptor Agonists); 0 (Isoquinolines); 0 (Naphthyridines); 0 (RS 79948-197); 0 (Receptors, Biogenic Amine); 0 (norsynephrine receptor); 9NEZ333N27 (Sodium)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170830
[Lr] Data última revisão:
170830
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170701
[St] Status:MEDLINE
[do] DOI:10.1124/mol.117.108456


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[PMID]:28542163
[Au] Autor:Wallberg A; Schöning C; Webster MT; Hasselmann M
[Ad] Endereço:Department of Medical Biochemistry and Microbiology, Science for Life Laboratory, Uppsala University, Uppsala, Sweden.
[Ti] Título:Two extended haplotype blocks are associated with adaptation to high altitude habitats in East African honey bees.
[So] Source:PLoS Genet;13(5):e1006792, 2017 May.
[Is] ISSN:1553-7404
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Understanding the genetic basis of adaption is a central task in biology. Populations of the honey bee Apis mellifera that inhabit the mountain forests of East Africa differ in behavior and morphology from those inhabiting the surrounding lowland savannahs, which likely reflects adaptation to these habitats. We performed whole genome sequencing on 39 samples of highland and lowland bees from two pairs of populations to determine their evolutionary affinities and identify the genetic basis of these putative adaptations. We find that in general, levels of genetic differentiation between highland and lowland populations are very low, consistent with them being a single panmictic population. However, we identify two loci on chromosomes 7 and 9, each several hundred kilobases in length, which exhibit near fixation for different haplotypes between highland and lowland populations. The highland haplotypes at these loci are extremely rare in samples from the rest of the world. Patterns of segregation of genetic variants suggest that recombination between haplotypes at each locus is suppressed, indicating that they comprise independent structural variants. The haplotype on chromosome 7 harbors nearly all octopamine receptor genes in the honey bee genome. These have a role in learning and foraging behavior in honey bees and are strong candidates for adaptation to highland habitats. Molecular analysis of a putative breakpoint indicates that it may disrupt the coding sequence of one of these genes. Divergence between the highland and lowland haplotypes at both loci is extremely high suggesting that they are ancient balanced polymorphisms that greatly predate divergence between the extant honey bee subspecies.
[Mh] Termos MeSH primário: Adaptação Fisiológica/genética
Abelhas/genética
Haplótipos/genética
Receptores de Amina Biogênica/genética
[Mh] Termos MeSH secundário: Altitude
Animais
Abelhas/fisiologia
Genoma de Inseto
Sequenciamento de Nucleotídeos em Larga Escala
Anotação de Sequência Molecular
Polimorfismo Genético
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Receptors, Biogenic Amine); 0 (norsynephrine receptor)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170614
[Lr] Data última revisão:
170614
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170526
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pgen.1006792


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[PMID]:28167800
[Au] Autor:Scheiner R; Reim T; Søvik E; Entler BV; Barron AB; Thamm M
[Ad] Endereço:University of Würzburg, Behavioral Physiology & Sociobiology, Biocenter, Am Hubland, Würzburg 97074, Germany ricarda.scheiner@uni-wuerzburg.de.
[Ti] Título:Learning, gustatory responsiveness and tyramine differences across nurse and forager honeybees.
[So] Source:J Exp Biol;220(Pt 8):1443-1450, 2017 Apr 15.
[Is] ISSN:1477-9145
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Honeybees are well known for their complex division of labor. Each bee sequentially performs a series of social tasks during its life. The changes in social task performance are linked to gross differences in behavior and physiology. We tested whether honeybees performing different social tasks (nursing versus foraging) would differ in their gustatory responsiveness and associative learning behavior in addition to their daily tasks in the colony. Further, we investigated the role of the biogenic amine tyramine and its receptors in the behavior of nurse bees and foragers. Tyramine is an important insect neurotransmitter, which has long been neglected in behavioral studies as it was believed to only act as the metabolic precursor of the better-known amine octopamine. With the increasing number of characterized tyramine receptors in diverse insects, we need to understand the functions of tyramine on its own account. Our findings suggest an important role for tyramine and its two receptors in regulating honeybee gustatory responsiveness, social organization and learning behavior. Foragers, which were more responsive to gustatory stimuli than nurse bees and performed better in appetitive learning, also differed from nurse bees in their tyramine brain titers and in the mRNA expression of a tyramine receptor in the brain. Pharmacological activation of tyramine receptors increased gustatory responsiveness of nurse bees and foragers and improved appetitive learning in nurse bees. These data suggest that a large part of the behavioral differences between honeybees may be directly linked to tyramine signaling in the brain.
[Mh] Termos MeSH primário: Abelhas/fisiologia
Proteínas de Insetos/metabolismo
Receptores de Amina Biogênica/metabolismo
Tiramina/metabolismo
[Mh] Termos MeSH secundário: Animais
Comportamento Apetitivo
Comportamento Animal
Condicionamento Clássico
Proteínas de Insetos/genética
Octopamina/análise
Octopamina/metabolismo
RNA Mensageiro/genética
Receptores de Amina Biogênica/genética
Transdução de Sinais
Olfato
Comportamento Social
Paladar
Tiramina/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Insect Proteins); 0 (RNA, Messenger); 0 (Receptors, Biogenic Amine); 0 (tyramine receptor); 14O50WS8JD (Octopamine); X8ZC7V0OX3 (Tyramine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170616
[Lr] Data última revisão:
170616
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170208
[St] Status:MEDLINE
[do] DOI:10.1242/jeb.152496


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[PMID]:27986436
[Au] Autor:Gross AD; Temeyer KB; Day TA; Pérez de León AA; Kimber MJ; Coats JR
[Ad] Endereço:Pesticide Toxicology Laboratory, Department of Entomology, Iowa State University of Science and Technology, Ames, IA, 50011, USA; Department of Biomedical Science, Iowa State University of Science and Technology, Ames, IA, 50011, USA.
[Ti] Título:Interaction of plant essential oil terpenoids with the southern cattle tick tyramine receptor: A potential biopesticide target.
[So] Source:Chem Biol Interact;263:1-6, 2017 Feb 01.
[Is] ISSN:1872-7786
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:An outbreak of the southern cattle tick, Rhipicephalus (Boophilus) microplus, (Canestrini), in the United States would have devastating consequences on the cattle industry. Tick populations have developed resistance to current acaricides, highlighting the need to identify new biochemical targets along with new chemistry. Furthermore, acaricide resistance could further hamper control of tick populations during an outbreak. Botanically-based compounds may provide a safe alternative for efficacious control of the southern cattle tick. We have developed a heterologous expression system that stably expresses the cattle tick's tyramine receptor with a G-protein chimera, producing a system that is amenable to high-throughput screening. Screening an in-house terpenoid library, at two screening concentrations (10 µM and 100 µM), has identified four terpenoids (piperonyl alcohol, 1,4-cineole, carvacrol and isoeugenol) that we believe are positive modulators of the southern cattle tick's tyramine receptor.
[Mh] Termos MeSH primário: Acaricidas/metabolismo
Óleos Voláteis/química
Receptores de Amina Biogênica/metabolismo
Terpenos/metabolismo
Carrapatos/enzimologia
[Mh] Termos MeSH secundário: Acaricidas/química
Acaricidas/toxicidade
Animais
Células CHO
Bovinos
Cricetinae
Cricetulus
Plasmídeos/genética
Plasmídeos/metabolismo
Ligação Proteica
Receptores de Amina Biogênica/antagonistas & inibidores
Receptores de Amina Biogênica/genética
Terpenos/química
Terpenos/toxicidade
Carrapatos/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Acaricides); 0 (Oils, Volatile); 0 (Receptors, Biogenic Amine); 0 (Terpenes); 0 (tyramine receptor)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170201
[Lr] Data última revisão:
170201
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161218
[St] Status:MEDLINE


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[PMID]:27939988
[Au] Autor:Reim T; Balfanz S; Baumann A; Blenau W; Thamm M; Scheiner R
[Ad] Endereço:Institute of Biochemistry and Biology, University of Potsdam, Potsdam, Germany.
[Ti] Título:AmTAR2: Functional characterization of a honeybee tyramine receptor stimulating adenylyl cyclase activity.
[So] Source:Insect Biochem Mol Biol;80:91-100, 2017 Jan.
[Is] ISSN:1879-0240
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The biogenic monoamines norepinephrine and epinephrine regulate important physiological functions in vertebrates. Insects such as honeybees do not synthesize these neuroactive substances. Instead, they employ octopamine and tyramine for comparable physiological functions. These biogenic amines activate specific guanine nucleotide-binding (G) protein-coupled receptors (GPCRs). Based on pharmacological data obtained on heterologously expressed receptors, α- and ß-adrenergic-like octopamine receptors are better activated by octopamine than by tyramine. Conversely, GPCRs forming the type 1 tyramine receptor clade (synonymous to octopamine/tyramine receptors) are better activated by tyramine than by octopamine. More recently, receptors were characterized which are almost exclusively activated by tyramine, thus forming an independent type 2 tyramine receptor clade. Functionally, type 1 tyramine receptors inhibit adenylyl cyclase activity, leading to a decrease in intracellular cAMP concentration ([cAMP] ). Type 2 tyramine receptors can mediate Ca signals or both Ca signals and effects on [cAMP] . We here provide evidence that the honeybee tyramine receptor 2 (AmTAR2), when heterologously expressed in flpTM cells, exclusively causes an increase in [cAMP] . The receptor displays a pronounced preference for tyramine over octopamine. Its activity can be blocked by a series of established antagonists, of which mianserin and yohimbine are most efficient. The functional characterization of two tyramine receptors from the honeybee, AmTAR1 (previously named AmTYR1) and AmTAR2, which respond to tyramine by changing cAMP levels in opposite direction, is an important step towards understanding the actions of tyramine in honeybee behavior and physiology, particularly in comparison to the effects of octopamine.
[Mh] Termos MeSH primário: Adenilil Ciclases/genética
Abelhas/genética
Proteínas de Insetos/genética
Receptores de Amina Biogênica/genética
Transdução de Sinais
[Mh] Termos MeSH secundário: Adenilil Ciclases/metabolismo
Animais
Abelhas/metabolismo
Proteínas de Insetos/metabolismo
Octopamina/metabolismo
Filogenia
Receptores de Amina Biogênica/metabolismo
Análise de Sequência de DNA
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Insect Proteins); 0 (Receptors, Biogenic Amine); 0 (tyramine receptor); 14O50WS8JD (Octopamine); EC 4.6.1.1 (Adenylyl Cyclases)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170901
[Lr] Data última revisão:
170901
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161213
[St] Status:MEDLINE


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[PMID]:27749013
[Au] Autor:Saul MC; Majdak P; Perez S; Reilly M; Garland T; Rhodes JS
[Ad] Endereço:Carl R. Woese Institute for Genomic Biology, Urbana, IL.
[Ti] Título:High motivation for exercise is associated with altered chromatin regulators of monoamine receptor gene expression in the striatum of selectively bred mice.
[So] Source:Genes Brain Behav;16(3):328-341, 2017 Mar.
[Is] ISSN:1601-183X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Although exercise is critical for health, many lack the motivation to exercise, and it is unclear how motivation might be increased. To uncover the molecular underpinnings of increased motivation for exercise, we analyzed the transcriptome of the striatum in four mouse lines selectively bred for high voluntary wheel running and four non-selected control lines. The striatum was dissected and RNA was extracted and sequenced from four individuals of each line. We found multiple genes and gene systems with strong relationships to both selection and running history over the previous 6 days. Among these genes were Htr1b, a serotonin receptor subunit and Slc38a2, a marker for both glutamatergic and γ-aminobutyric acid (GABA)-ergic signaling. System analysis of the raw results found enrichment of transcriptional regulation and kinase genes. Further, we identified a splice variant affecting the Wnt-related Golgi signaling gene Tmed5. Using coexpression network analysis, we found a cluster of interrelated coexpression modules with relationships to running behavior. From these modules, we built a network correlated with running that predicts a mechanistic relationship between transcriptional regulation by nucleosome structure and Htr1b expression. The Library of Integrated Network-Based Cellular Signatures identified the protein kinase C δ inhibitor, rottlerin, the tyrosine kinase inhibitor, Linifanib and the delta-opioid receptor antagonist 7-benzylidenenaltrexone as potential compounds for increasing the motivation to run. Taken together, our findings support a neurobiological framework of exercise motivation where chromatin state leads to differences in dopamine signaling through modulation of both the primary neurotransmitters glutamate and GABA, and by neuromodulators such as serotonin.
[Mh] Termos MeSH primário: Cromatina/genética
Corpo Estriado/fisiologia
Motivação/genética
Atividade Motora/genética
Esforço Físico/genética
Receptores de Amina Biogênica/genética
Corrida/fisiologia
[Mh] Termos MeSH secundário: Animais
Monoaminas Biogênicas/metabolismo
Cromatina/metabolismo
Corpo Estriado/metabolismo
Dopamina/genética
Dopamina/metabolismo
Regulação da Expressão Gênica
Masculino
Camundongos
RNA não Traduzido/genética
Receptor 5-HT1B de Serotonina/biossíntese
Receptor 5-HT1B de Serotonina/genética
Receptores de Amina Biogênica/biossíntese
Seleção Genética
Transcriptoma
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biogenic Monoamines); 0 (Chromatin); 0 (HTR1B protein, mouse); 0 (RNA, Untranslated); 0 (Receptor, Serotonin, 5-HT1B); 0 (Receptors, Biogenic Amine); VTD58H1Z2X (Dopamine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170628
[Lr] Data última revisão:
170628
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161018
[St] Status:MEDLINE
[do] DOI:10.1111/gbb.12347


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[PMID]:27720431
[Au] Autor:Gisquet-Verrier P; Tolédano D; Le Dorze C
[Ad] Endereço:Neuro-PSI, CNRS UMR 9197, université Paris-Sud, université Paris-Saclay, 91400 Orsay, France. Electronic address: pascale.gisquet@u-psud.fr.
[Ti] Título:[Common physiological basis for post-traumatic stress disorder and dependence to drugs of abuse: Implications for new therapeutic approaches].
[Ti] Título:Bases physiologiques communes pour les troubles de stress post-traumatique et la dépendance aux drogues d'abus : conséquences pour de nouvelles approches thérapeutiques..
[So] Source:Therapie;72(3):357-366, 2017 Jun.
[Is] ISSN:0040-5957
[Cp] País de publicação:France
[La] Idioma:fre
[Ab] Resumo:Post-traumatic stress disorder (PTSD) and addiction to drugs of abuse are two common diseases, showing high comorbidity rates. This review presents a number of evidence showing similarities between these two pathologies, especially the hyper-responsiveness to environmental cues inducing a reactivation of the target memory leading either to re-experiencing (PTSD), or drug craving. Accordingly, PTSD and addiction to drug of abuse might by considered as memory pathologies, underlined by the same physiological process. We propose that these two pathologies rely on an uncoupling of the monoaminergic systems. According to this hypothesis, exposure to extreme conditions, either negative (trauma) or positive (drugs) induced a loss of the reciprocal control that one system usually exerts on the other monoaminergic system, resulting to an uncoupling between the noradrenergic and the serotonergic systems. Results obtained in our laboratory, using animal models of these pathologies, demonstrate that after a trauma, such as after repeated drug injections, rats developed both a behavioral sensitization (increases of the locomotion in response to a stimulation of the monoaminergic systems) and a pharmacological sensitization (increases of noradrenergic release within the prefrontal cortex). These results support our hypothesis and led us to propose new and innovative therapeutic approaches consisting either to induce a re-coupling of the monoaminergic systems, or to modify the pathological memories by using an emotional memory remodeling. Extremely encouraging results have already been obtained in rats and in humans, opening new and promising therapeutic avenues.
[Mh] Termos MeSH primário: Receptores de Amina Biogênica/fisiologia
Transtornos de Estresse Pós-Traumáticos/fisiopatologia
Transtornos Relacionados ao Uso de Substâncias/fisiopatologia
[Mh] Termos MeSH secundário: Animais
Seres Humanos
Transtornos de Estresse Pós-Traumáticos/terapia
Transtornos Relacionados ao Uso de Substâncias/terapia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Receptors, Biogenic Amine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170926
[Lr] Data última revisão:
170926
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161011
[St] Status:MEDLINE


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[PMID]:27717101
[Au] Autor:Xu L; Li L; Yang P; Ma Z
[Ad] Endereço:State Key Laboratory of Integrated Management of Pest Insects and Rodents, Institute of Zoology, Chinese Academy of Sciences, Beijing, China.
[Ti] Título:Calmodulin as a downstream gene of octopamine-OAR α1 signalling mediates olfactory attraction in gregarious locusts.
[So] Source:Insect Mol Biol;26(1):1-12, 2017 Feb.
[Is] ISSN:1365-2583
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The migratory locust (Locusta migratoria) shows aggregative traits in nymph marching bands and swarm formations through mutual olfactory attraction of conspecifics. However, olfactory preference in different nymph stages in gregarious locusts is not sufficiently explored. In this study, we found that the nymph olfactory preference for gregarious volatiles exhibited obvious variations at different developmental stages. The gregarious locusts show attractive response to conspecific volatiles from the third stadium. Transcriptome comparison between third- and fourth-stadium nymphs showed that the G protein-coupled receptor (GPCR) pathways are significantly enriched. Amongst the genes present in GPCR pathways, the expression level of calmodulin in locust brains significantly increased from the third- to the fourth-stadium nymphs. Amongst the four octopamine receptors (OARs) belonging to the GPCR family, only OAR α1 showed similar expression patterns to those of calmodulin, and knockdown of OAR α1 reduced the expression level of calmodulin. RNA interference of calmodulin decreased locomotion and induced the loss of olfactory attraction in gregarious locusts. Moreover, the activation of OAR α1 in calmodulin-knockdown locusts did not induce olfactory attraction of the nymphs to gregarious volatiles. Thus, calmodulin as a downstream gene of octopamine-OAR α1 (OA-OAR α1) signalling mediates olfactory attraction in gregarious locusts. Overall, this study provides novel insights into the mechanism of OA-OAR α1 signalling involved in olfactory attraction of gregarious locusts.
[Mh] Termos MeSH primário: Calmodulina/metabolismo
Locusta migratoria/metabolismo
Feromônios
Receptores de Amina Biogênica/metabolismo
Olfato
[Mh] Termos MeSH secundário: Animais
Encéfalo/metabolismo
Proteínas de Insetos/metabolismo
Locusta migratoria/genética
Locusta migratoria/crescimento & desenvolvimento
Ninfa/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Calmodulin); 0 (Insect Proteins); 0 (Pheromones); 0 (Receptors, Biogenic Amine); 0 (norsynephrine receptor)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170828
[Lr] Data última revisão:
170828
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161008
[St] Status:MEDLINE
[do] DOI:10.1111/imb.12266


  9 / 352 MEDLINE  
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[PMID]:27484898
[Au] Autor:Kita T; Hayashi T; Ohtani T; Takao H; Takasu H; Liu G; Ohta H; Ozoe F; Ozoe Y
[Ad] Endereço:Department of Life Science and Biotechnology, Faculty of Life and Environmental Science, Shimane University, Matsue, Shimane, Japan.
[Ti] Título:Amitraz and its metabolite differentially activate α- and ß-adrenergic-like octopamine receptors.
[So] Source:Pest Manag Sci;73(5):984-990, 2017 May.
[Is] ISSN:1526-4998
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Amitraz is a formamidine acaricide and insecticide used to control ticks, mites and fleas. N -(2,4-Dimethylphenyl)-N -methyformamidine (DPMF), a metabolite of amitraz, is thought to be an active agent that exerts acaricidal and insecticidal effects by acting as an agonist on octopamine receptors. The emergence of cattle ticks resistant to amitraz is a serious problem that requires urgent attention. The objective of this research was to determine which type of octopamine receptor is the primary target of amitraz and thereby understand the molecular mechanisms of action and resistance to amitraz. RESULTS: Amitraz and DPMF potently activated Bombyx mori α- and ß-adrenergic-like octopamine receptors (α- and ß-AL OARs) that were stably expressed in HEK-293 cells. Notably, DPMF elevated intracellular cAMP levels, with an EC of 79.6 pm in ß-AL OARs, the transcripts of which were prevalently and widely localised in B. mori body parts. Furthermore, DPMF elevated the intracellular Ca levels, with an EC of 1.17 nm in α-AL OARs. CONCLUSION: Although both amitraz and DPMF acted as OAR agonists, the metabolite DPMF was more potent than amitraz and differentially activated α- and ß-AL OARs. The present findings provide a basis for studies to examine the mechanism of amitraz resistance and to develop novel acaricides and insecticides. © 2016 Society of Chemical Industry.
[Mh] Termos MeSH primário: Acaricidas/metabolismo
Acaricidas/farmacologia
Inseticidas/metabolismo
Inseticidas/farmacologia
Receptores de Amina Biogênica/metabolismo
Toluidinas/metabolismo
Toluidinas/farmacologia
[Mh] Termos MeSH secundário: Animais
Bombyx/efeitos dos fármacos
Bombyx/metabolismo
Células HEK293
Seres Humanos
Larva/efeitos dos fármacos
Larva/metabolismo
RNA Mensageiro/genética
RNA Mensageiro/metabolismo
Receptores de Amina Biogênica/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Acaricides); 0 (Insecticides); 0 (RNA, Messenger); 0 (Receptors, Biogenic Amine); 0 (Toluidines); 0 (norsynephrine receptor); 33IAH5017S (amitraz)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170501
[Lr] Data última revisão:
170501
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160804
[St] Status:MEDLINE
[do] DOI:10.1002/ps.4412


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[PMID]:27306119
[Au] Autor:Bonnafé E; Alayrangues J; Hotier L; Massou I; Renom A; Souesme G; Marty P; Allaoua M; Treilhou M; Armengaud C
[Ad] Endereço:Jean-François Champollion University Center, Albi, France.
[Ti] Título:Monoterpenoid-based preparations in beehives affect learning, memory, and gene expression in the bee brain.
[So] Source:Environ Toxicol Chem;36(2):337-345, 2017 Feb.
[Is] ISSN:1552-8618
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Bees are exposed in their environment to contaminants that can weaken the colony and contribute to bee declines. Monoterpenoid-based preparations can be introduced into hives to control the parasitic mite Varroa destructor. The long-term effects of monoterpenoids are poorly investigated. Olfactory conditioning of the proboscis extension reflex (PER) has been used to evaluate the impact of stressors on cognitive functions of the honeybee such as learning and memory. The authors tested the PER to odorants on bees after exposure to monoterpenoids in hives. Octopamine receptors, transient receptor potential-like (TRPL), and γ-aminobutyric acid channels are thought to play a critical role in the memory of food experience. Gene expression levels of Amoa1, Rdl, and trpl were evaluated in parallel in the bee brain because these genes code for the cellular targets of monoterpenoids and some pesticides and neural circuits of memory require their expression. The miticide impaired the PER to odors in the 3 wk following treatment. Short-term and long-term olfactory memories were improved months after introduction of the monoterpenoids into the beehives. Chronic exposure to the miticide had significant effects on Amoa1, Rdl, and trpl gene expressions and modified seasonal changes in the expression of these genes in the brain. The decrease of expression of these genes in winter could partly explain the improvement of memory. The present study has led to new insights into alternative treatments, especially on their effects on memory and expression of selected genes involved in this cognitive function. Environ Toxicol Chem 2017;36:337-345. © 2016 SETAC.
[Mh] Termos MeSH primário: Antiparasitários/toxicidade
Abelhas/efeitos dos fármacos
Encéfalo/efeitos dos fármacos
Expressão Gênica/efeitos dos fármacos
Memória/efeitos dos fármacos
Monoterpenos/toxicidade
[Mh] Termos MeSH secundário: Animais
Abelhas/fisiologia
Encéfalo/fisiologia
Aprendizagem/efeitos dos fármacos
Percepção Olfatória/efeitos dos fármacos
Receptores de Amina Biogênica/genética
Receptores de GABA/genética
Canais de Receptores Transientes de Potencial/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antiparasitic Agents); 0 (Monoterpenes); 0 (Receptors, Biogenic Amine); 0 (Receptors, GABA); 0 (Transient Receptor Potential Channels); 0 (norsynephrine receptor)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170724
[Lr] Data última revisão:
170724
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160617
[St] Status:MEDLINE
[do] DOI:10.1002/etc.3527



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