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  1 / 2051 MEDLINE  
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[PMID]:28460160
[Au] Autor:Huot P; Sgambato-Faure V; Fox SH; McCreary AC
[Ad] Endereço:Centre de Recherche du Centre Hospitalier de l'Université de Montréal , Montreal, QC H2X 0A9, Canada.
[Ti] Título:Serotonergic Approaches in Parkinson's Disease: Translational Perspectives, an Update.
[So] Source:ACS Chem Neurosci;8(5):973-986, 2017 05 17.
[Is] ISSN:1948-7193
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Parkinson's disease (PD) has long been seen as a disorder caused by degeneration of the dopaminergic system, leading to the classic motor manifestations of the disease. However, there is now overwhelming evidence that PD is more than a disease merely caused by dopamine depletion. It is well-known that a myriad of other neurotransmitters are affected by the disease process. One such neurotransmitter is serotonin (5-HT). 5-HT has been shown to play a role in several motor and nonmotor manifestations of PD, including tremor, cognition, depression and psychosis. 5-HT also seems to play a critical role in L-3,4-dihydroxyphenylalanine (L-DOPA)-induced dyskinesia. A breadth of preclinical studies and clinical trials have been conducted that aimed at modulating the 5-HT system in order to alleviate depression, cognitive deficits, psychosis, and dyskinesia. In this Review, we summarize recent advances in the 5-HT field in PD, but with a translational emphasis. We start by presenting a novel nonhuman primate model of PD that presents with dual dopamine and 5-HT lesions. We then present preclinical and clinical data that introduce new concepts, such as the use of biased and partial agonists, as well as molecules recently introduced to the field of PD, such as eltoprazine, pimavanserin, nelotanserin, and SYN-120, to enhance therapeutic benefit while minimizing adverse events, notably on parkinsonian disability.
[Mh] Termos MeSH primário: Antiparkinsonianos/uso terapêutico
Doença de Parkinson/metabolismo
Serotoninérgicos/uso terapêutico
Serotonina/metabolismo
[Mh] Termos MeSH secundário: Animais
Antiparkinsonianos/farmacologia
Modelos Animais de Doenças
Seres Humanos
Atividade Motora/efeitos dos fármacos
Doença de Parkinson/tratamento farmacológico
Serotoninérgicos/farmacologia
Pesquisa Médica Translacional
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Antiparkinson Agents); 0 (Serotonin Agents); 333DO1RDJY (Serotonin)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180223
[Lr] Data última revisão:
180223
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170502
[St] Status:MEDLINE
[do] DOI:10.1021/acschemneuro.6b00440


  2 / 2051 MEDLINE  
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[PMID]:29303006
[Au] Autor:Papaseit E; Torrens M; Pérez-Mañá C; Muga R; Farré M
[Ad] Endereço:a Departments of Clinical Pharmacology and Internal Medicine , Hospital Universitari Germans Trias I Pujol-IGTP , Badalona , Spain.
[Ti] Título:Key interindividual determinants in MDMA pharmacodynamics.
[So] Source:Expert Opin Drug Metab Toxicol;14(2):183-195, 2018 Feb.
[Is] ISSN:1744-7607
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: MDMA, 3,4-methylenedioxymethamphetamine, is a synthetic phenethylamine derivative with structural and pharmacological similarities to both amphetamines and mescaline. MDMA produces characteristic amphetamine-like actions (euphoria, well-being), increases empathy, and induces pro-social effects that seem to motivate its recreational consumption and provide a basis for its potential therapeutic use. Areas covered: The aim of this review is to present the main interindividual determinants in MDMA pharmacodynamics. The principal sources of pharmacodynamic variability are reviewed, with special emphasis on sex-gender, race-ethnicity, genetic differences, interactions, and MDMA acute toxicity, as well as possible therapeutic use. Expert opinion: Acute MDMA effects are more pronounced in women than they are in men. Very limited data on the relationship between race-ethnicity and MDMA effects are available. MDMA metabolism includes some polymorphic enzymes that can slightly modify plasma concentrations and effects. Although a considerable number of studies exist about the acute effects of MDMA, the small number of subjects in each trial limits evaluation of the different interindividual factors and does not permit a clear conclusion about their influence. These issues should be considered when studying possible MDMA therapeutic use.
[Mh] Termos MeSH primário: Alucinógenos/administração & dosagem
N-Metil-3,4-Metilenodioxianfetamina/administração & dosagem
Serotoninérgicos/administração & dosagem
[Mh] Termos MeSH secundário: Animais
Grupos de Populações Continentais
Interações Medicamentosas
Grupos Étnicos
Feminino
Alucinógenos/efeitos adversos
Alucinógenos/farmacologia
Seres Humanos
Masculino
N-Metil-3,4-Metilenodioxianfetamina/efeitos adversos
N-Metil-3,4-Metilenodioxianfetamina/farmacologia
Serotoninérgicos/efeitos adversos
Serotoninérgicos/farmacologia
Fatores Sexuais
Transtornos Relacionados ao Uso de Substâncias/psicologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Hallucinogens); 0 (Serotonin Agents); KE1SEN21RM (N-Methyl-3,4-methylenedioxyamphetamine)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180222
[Lr] Data última revisão:
180222
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180106
[St] Status:MEDLINE
[do] DOI:10.1080/17425255.2018.1424832


  3 / 2051 MEDLINE  
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[PMID]:28413824
[Au] Autor:Pratelli M; Migliarini S; Pelosi B; Napolitano F; Usiello A; Pasqualetti M
[Ad] Endereço:Department of Biology Unit of Cell and Developmental Biology, University of Pisa, Pisa 56127, Italy.
[Ti] Título:Perturbation of Serotonin Homeostasis during Adulthood Affects Serotonergic Neuronal Circuitry.
[So] Source:eNeuro;4(2), 2017 Mar-Apr.
[Is] ISSN:2373-2822
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Growing evidence shows that the neurotransmitter serotonin (5-HT) modulates the fine-tuning of neuron development and the establishment of wiring patterns in the brain. However, whether serotonin is involved in the maintenance of neuronal circuitry in the adult brain remains elusive. Here, we use a conditional knockout (cKO) mouse line to assess the impact of serotonin depletion during adulthood on serotonergic system organization. Data show that the density of serotonergic fibers is increased in the hippocampus and decreased in the thalamic paraventricular nucleus (PVN) as a consequence of brain serotonin depletion. Strikingly, these defects are rescued following reestablishment of brain 5-HT signaling via administration of the serotonin precursor 5-hydroxytryptophan (5-HTP). Finally, 3D reconstruction of serotonergic fibers reveals that changes in serotonin homeostasis affect axonal branching complexity. These data demonstrate that maintaining proper serotonin homeostasis in the adult brain is crucial to preserve the correct serotonergic axonal wiring.
[Mh] Termos MeSH primário: Núcleos da Linha Média do Tálamo/citologia
Rede Nervosa/fisiologia
Neurônios Serotoninérgicos/fisiologia
Serotonina/metabolismo
[Mh] Termos MeSH secundário: 5-Hidroxitriptofano/farmacologia
Animais
Fator Neurotrófico Derivado do Encéfalo/genética
Fator Neurotrófico Derivado do Encéfalo/metabolismo
Regulação da Expressão Gênica/efeitos dos fármacos
Regulação da Expressão Gênica/genética
Proteínas de Fluorescência Verde/genética
Proteínas de Fluorescência Verde/metabolismo
Homeostase/efeitos dos fármacos
Homeostase/genética
Camundongos
Camundongos Endogâmicos C57BL
Camundongos Transgênicos
Vias Neurais/efeitos dos fármacos
Vias Neurais/fisiologia
RNA Mensageiro/metabolismo
Neurônios Serotoninérgicos/efeitos dos fármacos
Serotoninérgicos/farmacologia
Proteínas da Membrana Plasmática de Transporte de Serotonina/genética
Proteínas da Membrana Plasmática de Transporte de Serotonina/metabolismo
Transdução de Sinais/efeitos dos fármacos
Transdução de Sinais/genética
Triptofano Hidroxilase/genética
Triptofano Hidroxilase/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Brain-Derived Neurotrophic Factor); 0 (RNA, Messenger); 0 (Serotonin Agents); 0 (Serotonin Plasma Membrane Transport Proteins); 147336-22-9 (Green Fluorescent Proteins); 333DO1RDJY (Serotonin); C1LJO185Q9 (5-Hydroxytryptophan); EC 1.14.16.4 (Tph2 protein, mouse); EC 1.14.16.4 (Tryptophan Hydroxylase)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170424
[Lr] Data última revisão:
170424
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170418
[St] Status:MEDLINE


  4 / 2051 MEDLINE  
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[PMID]:28337771
[Au] Autor:Marin P; Dityatev A
[Ad] Endereço:Institut de Génomique Fonctionnelle, CNRS UMR 5203, INSERM U1191, Université de Montpellier, Montpellier Cedex 5, France.
[Ti] Título:5-HT7 receptor shapes spinogenesis in cortical and striatal neurons: An Editorial Highlight for 'Serotonin 5-HT7 receptor increases the density of dendritic spines and facilitates synaptogenesis in forebrain neurons'.
[So] Source:J Neurochem;141(5):644-646, 2017 Jun.
[Is] ISSN:1471-4159
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Read the highlighted article 'Serotonin 5-HT7 receptor increases the density of dendritic spines and facilitates synaptogenesis in forebrain neurons' on page 647.
[Mh] Termos MeSH primário: Espinhas Dendríticas/fisiologia
Neurônios/citologia
Prosencéfalo/citologia
Receptores de Serotonina/fisiologia
Sinapses/fisiologia
[Mh] Termos MeSH secundário: Animais
Espinhas Dendríticas/efeitos dos fármacos
Neurônios/efeitos dos fármacos
Serotoninérgicos/farmacologia
Sinapses/efeitos dos fármacos
[Pt] Tipo de publicação:EDITORIAL
[Nm] Nome de substância:
0 (Receptors, Serotonin); 0 (Serotonin Agents); 0 (serotonin 7 receptor)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170325
[St] Status:MEDLINE
[do] DOI:10.1111/jnc.13981


  5 / 2051 MEDLINE  
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[PMID]:28326933
[Au] Autor:Wang CT; Mao CJ; Zhang XQ; Zhang CY; Lv DJ; Yang YP; Xia KL; Liu JY; Wang F; Hu LF; Xu GY; Liu CF
[Ad] Endereço:1 Department of Neurology and Suzhou Clinical Research Center of Neurological Disease, The Second Affiliated Hospital of Soochow University, Suzhou, China.
[Ti] Título:Attenuation of hyperalgesia responses via the modulation of 5-hydroxytryptamine signalings in the rostral ventromedial medulla and spinal cord in a 6-hydroxydopamine-induced rat model of Parkinson's disease.
[So] Source:Mol Pain;13:1744806917691525, 2017 Jan.
[Is] ISSN:1744-8069
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Background Although pain is one of the most distressing non-motor symptoms among patients with Parkinson's disease, the underlying mechanisms of pain in Parkinson's disease remain elusive. The aim of the present study was to investigate the role of serotonin (5-hydroxytryptamine) in the rostral ventromedial medulla (RVM) and spinal cord in pain sensory abnormalities in a 6-hydroxydopamine-treated rat model of Parkinson's disease. Methods The rotarod test was used to evaluate motor function. The radiant heat test and von Frey test were conducted to evaluate thermal and mechanical pain thresholds, respectively. Immunofluorescence was used to examine 5-hydroxytryptamine neurons and fibers in the rostral ventromedial medulla and spinal cord. High-performance liquid chromatography was used to determine 5-hydroxytryptamine and 5-hydroxyindoleacetic acid levels. Results The duration of running time on the rotarod test was significantly reduced in 6-hydroxydopamine-treated rats. Nociceptive thresholds of both mechanical and heat pain were reduced compared to sham-treated rats. In addition to the degeneration of cell bodies and fibers in the substantia nigra pars compacta, the number of rostral ventromedial medulla 5-hydroxytryptamine neurons and 5-hydroxytryptamine fibers in the spinal dorsal horn was dramatically decreased. 5-Hydroxytryptamine concentrations in both the rostral ventromedial medulla and spinal cord were reduced. Furthermore, the administration of citalopram significantly attenuated pain hypersensitivity. Interestingly, Intra-rostral ventromedial medulla (intra-RVM) microinjection of 5,7-dihydroxytryptamine partially reversed pain hypersensitivity of 6-hydroxydopamine-treated rats. Conclusions These results suggest that the decreased 5-hydroxytryptamine contents in the rostral ventromedial medulla and spinal dorsal horn may be involved in hyperalgesia in the 6-hydroxydopamine-induced rat model of Parkinson's disease.
[Mh] Termos MeSH primário: Hiperalgesia/tratamento farmacológico
Hiperalgesia/etiologia
Bulbo/metabolismo
Doença de Parkinson/complicações
Serotonina/metabolismo
Transdução de Sinais/fisiologia
Medula Espinal/metabolismo
[Mh] Termos MeSH secundário: 5,7-Di-Hidroxitriptamina/uso terapêutico
Animais
Modelos Animais de Doenças
Indóis/metabolismo
Masculino
Bulbo/efeitos dos fármacos
Oxidopamina/toxicidade
Doença de Parkinson/etiologia
Doença de Parkinson/patologia
Ratos
Ratos Sprague-Dawley
Receptores Opioides mu/metabolismo
Serotoninérgicos/farmacologia
Inibidores da Captação de Serotonina/farmacologia
Medula Espinal/efeitos dos fármacos
Simpatolíticos/toxicidade
Tirosina 3-Mono-Oxigenase/metabolismo
Ácido gama-Aminobutírico/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Indoles); 0 (Receptors, Opioid, mu); 0 (Serotonin Agents); 0 (Serotonin Uptake Inhibitors); 0 (Sympatholytics); 31363-74-3 (5,7-Dihydroxytryptamine); 333DO1RDJY (Serotonin); 56-12-2 (gamma-Aminobutyric Acid); 5SW11R7M7M (indole-3-lactic acid); 8HW4YBZ748 (Oxidopamine); EC 1.14.16.2 (Tyrosine 3-Monooxygenase)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170323
[St] Status:MEDLINE
[do] DOI:10.1177/1744806917691525


  6 / 2051 MEDLINE  
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[PMID]:28233634
[Au] Autor:Sasaki-Hamada S; Suzuki A; Ueda Y; Matsumoto K; Oka JI
[Ad] Endereço:Laboratory of Pharmacology, Faculty of Pharmaceutical Sciences, Tokyo University of Science, Japan.
[Ti] Título:Serotonergic and dopaminergic systems are implicated in antidepressant-like effects of chotosan, a Kampo formula, in mice.
[So] Source:J Pharmacol Sci;133(2):110-113, 2017 Feb.
[Is] ISSN:1347-8648
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:We previously demonstrated that chotosan (CTS), a traditional herbal formula called Kampo medicine, improves diabetes-induced cognitive deficits. In the present study, we investigated the antidepressant-like effects of CTS in mice. The administration of CTS (1.0 g/kg, for 3 days) decreased the immobility time in the forced-swim test, and this decrease was prevented by the prior administration of sulpiride (an antagonist of D receptors) and WAY100635 (an antagonist of 5-HT receptors). None of the treatments tested altered the locomotor activity of mice. These results suggest that CTS exerts antidepressant-like effects through changes in the serotonergic and dopaminergic systems.
[Mh] Termos MeSH primário: Antidepressivos/farmacologia
Dopaminérgicos/farmacologia
Medicamentos de Ervas Chinesas/farmacologia
Medicina Kampo
Serotoninérgicos/farmacologia
[Mh] Termos MeSH secundário: Animais
Modelos Animais de Doenças
Fenclonina/química
Imipramina/química
Imipramina/farmacologia
Ketanserina/química
Ketanserina/farmacologia
Locomoção
Masculino
Metergolina/química
Camundongos
Piperazinas/química
Piperazinas/farmacologia
Piridinas/química
Piridinas/farmacologia
Sulpirida/química
Sulpirida/farmacologia
Natação
Ioimbina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antidepressive Agents); 0 (Dopamine Agents); 0 (Drugs, Chinese Herbal); 0 (Piperazines); 0 (Pyridines); 0 (Serotonin Agents); 0 (choto-san); 1501393LY5 (Metergoline); 2Y49VWD90Q (Yohimbine); 71IH826FEG (N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide); 7MNE9M8287 (Sulpiride); 97F9DE4CT4 (Ketanserin); OGG85SX4E4 (Imipramine); R5J7E3L9SP (Fenclonine)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170504
[Lr] Data última revisão:
170504
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170225
[St] Status:MEDLINE


  7 / 2051 MEDLINE  
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[PMID]:28035530
[Au] Autor:Terry N; Margolis KG
[Ad] Endereço:Division of Pediatric Gastroenterology, Children's Hospital of Philadelphia, Perelman School of Medicine at the University of Pennsylvania, Philadelphia, PA, USA.
[Ti] Título:Serotonergic Mechanisms Regulating the GI Tract: Experimental Evidence and Therapeutic Relevance.
[So] Source:Handb Exp Pharmacol;239:319-342, 2017.
[Is] ISSN:0171-2004
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Serotonin (5-hydroxytryptamine; 5-HT) is best known as a neurotransmitter critical for central nervous system (CNS) development and function. 95% of the body's serotonin, however, is produced in the intestine where it has been increasingly recognized for its hormonal, autocrine, paracrine, and endocrine actions. This chapter provides the most current knowledge of the critical autocrine and paracrine roles of 5-HT in intestinal motility and inflammation as well as its function as a hormone in osteocyte homeostasis. Therapeutic applications in each of these areas are also discussed.
[Mh] Termos MeSH primário: Sistema Nervoso Entérico/metabolismo
Trato Gastrointestinal/inervação
Doenças Inflamatórias Intestinais/metabolismo
Neurônios Serotoninérgicos/metabolismo
Serotonina/metabolismo
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios/uso terapêutico
Remodelação Óssea
Sistema Nervoso Entérico/efeitos dos fármacos
Sistema Nervoso Entérico/fisiopatologia
Fármacos Gastrointestinais/uso terapêutico
Motilidade Gastrointestinal
Trato Gastrointestinal/efeitos dos fármacos
Seres Humanos
Doenças Inflamatórias Intestinais/tratamento farmacológico
Doenças Inflamatórias Intestinais/fisiopatologia
Neurogênese
Osteócitos/metabolismo
Osteoporose/metabolismo
Osteoporose/fisiopatologia
Receptores de Serotonina/metabolismo
Serotoninérgicos/uso terapêutico
Transdução de Sinais
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Gastrointestinal Agents); 0 (Receptors, Serotonin); 0 (Serotonin Agents); 333DO1RDJY (Serotonin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171016
[Lr] Data última revisão:
171016
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161231
[St] Status:MEDLINE
[do] DOI:10.1007/164_2016_103


  8 / 2051 MEDLINE  
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[PMID]:27981607
[Au] Autor:Pessoa-Mahana H; Silva-Matus P; Pessoa-Mahana CD; Chung H; Iturriaga-Vásquez P; Quiroz G; Möller-Acuña P; Zapata-Torres G; Saitz-Barría C; Araya-Maturana R; Reyes-Parada M
[Ad] Endereço:Departamento de Química Orgánica y Fisicoquímica, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Santiago, Chile.
[Ti] Título:Synthesis and Docking of Novel 3-Indolylpropyl Derivatives as New Polypharmacological Agents Displaying Affinity for 5-HT R/SERT.
[So] Source:Arch Pharm (Weinheim);350(1), 2017 Jan.
[Is] ISSN:1521-4184
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:A series of novel 3-indolylpropyl derivatives was synthesized and evaluated for their binding affinities at the serotonin-1A receptor subtype (5-HT R) and the 5-HT transporter (SERT). Compounds 11b and 14b exhibited the highest affinities at the 5-HT R (K = 43 and 56 nM), whereas compounds 11c and 14a were the most potent analogs at the SERT (K = 34 and 17 nM). On the other hand, compounds 14b and 11d showed potent activity at both targets, displaying a profile that makes them promising leads for the search for novel potent ligands with a dual mechanism of action. Molecular docking studies in all the compounds unveiled relevant drug-target interactions, which allowed rationalizing the observed affinities.
[Mh] Termos MeSH primário: Indóis/síntese química
Indóis/farmacologia
Simulação de Acoplamento Molecular
Receptor 5-HT1A de Serotonina/metabolismo
Serotoninérgicos/síntese química
Serotoninérgicos/farmacologia
Proteínas da Membrana Plasmática de Transporte de Serotonina/metabolismo
[Mh] Termos MeSH secundário: Antidepressivos/síntese química
Antidepressivos/farmacologia
Relação Dose-Resposta a Droga
Seres Humanos
Indóis/química
Estrutura Molecular
Serotoninérgicos/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antidepressive Agents); 0 (Indoles); 0 (Serotonin Agents); 0 (Serotonin Plasma Membrane Transport Proteins); 112692-38-3 (Receptor, Serotonin, 5-HT1A)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170417
[Lr] Data última revisão:
170417
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161217
[St] Status:MEDLINE
[do] DOI:10.1002/ardp.201600271


  9 / 2051 MEDLINE  
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[PMID]:27941419
[Au] Autor:Yoon S; Jeon SW; Ko YH; Patkar AA; Masand PS; Pae CU; Han C
[Ad] Endereço:From the *Department of Psychiatry, Korea University College of Medicine, Seoul, Korea; †Department of Psychiatry and Behavioural Sciences, Duke University Medical Center, Durham, NC; ‡Academic Medicine Education Institute, Duke-NUS Medical School, Singapore; and §Department of Psychiatry, The Catholic University of Korea College of Medicine, Seoul, Korea.
[Ti] Título:Adjunctive Brexpiprazole as a Novel Effective Strategy for Treating Major Depressive Disorder: A Systematic Review and Meta-Analysis.
[So] Source:J Clin Psychopharmacol;37(1):46-53, 2017 Feb.
[Is] ISSN:1533-712X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:PURPOSE/BACKGROUND: Brexpiprazole was approved for adjunctive treatment of major depressive disorder (MDD) in 2015. Because only a small number of randomized controlled trials have investigated the use of brexpiprazole in MDD, we performed a meta-analysis. METHODS/PROCEDURES: We systematically searched literatures in PubMed, Cochrane Library database, EMBASE, Google Scholar, and clinicaltrials.gov up to January 2016. The primary efficacy measure was the mean change in total Montgomery-Åsberg Depression Rating Scale (MADRS) score from baseline. Secondary efficacy measures were the mean change in total Hamilton Rating Scale for Depression (17 items) score from baseline and the response (≥50% reduction in MADRS total score) and remission (MADRS total score ≤ 10 with ≥50% reduction) rates. FINDINGS/RESULTS: Four studies fulfilled the inclusion criteria and were included in the analysis. Brexpiprazole showed superior efficacy over placebo with effect sizes (mean differences) of -1.76 (95% confidence interval [CI], -2.45 to -1.07) for MADRS and -1.21 (95% CI, -1.71 to -0.72) for the 17-item Hamilton Rating Scale for Depression. The risk ratios for response and remission were 1.57 (95% CI, 1.29-1.91) and 1.55 (95% CI, 1.22-1.96), respectively. The incidences of discontinuation due to adverse events, akathisia, and weight increase were higher in the brexpiprazole group than in the placebo group, with risk ratios of 3.44 (95% CI, 1.52-7.80), 3.39 (95% CI, 2.08-5.51), and 4.36 (95% CI, 2.45-7.77), respectively, and the incidence of akathisia was related to the brexpiprazole dose. IMPLICATIONS/CONCLUSIONS: Although our results suggest that brexpiprazole could be an effective adjunctive agent for MDD, they should be cautiously translated into clinical practice because the meta-analysis was based on only a handful of randomized controlled trials.
[Mh] Termos MeSH primário: Transtorno Depressivo Maior/tratamento farmacológico
Quinolonas/farmacologia
Serotoninérgicos/farmacologia
Tiofenos/farmacologia
[Mh] Termos MeSH secundário: Seres Humanos
Quinolonas/administração & dosagem
Serotoninérgicos/administração & dosagem
Tiofenos/administração & dosagem
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS; REVIEW
[Nm] Nome de substância:
0 (Quinolones); 0 (Serotonin Agents); 0 (Thiophenes); 2J3YBM1K8C (brexpiprazole)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170605
[Lr] Data última revisão:
170605
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161213
[St] Status:MEDLINE
[do] DOI:10.1097/JCP.0000000000000622


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[PMID]:27580242
[Au] Autor:Liu Y; Canal CE; Cordova-Sintjago TC; Zhu W; Booth RG
[Ad] Endereço:Center for Drug Discovery, Department of Pharmaceutical Sciences, and Department of Chemistry and Chemical Biology, Northeastern University , Boston, Massachusetts 02115, United States.
[Ti] Título:Mutagenesis Analysis Reveals Distinct Amino Acids of the Human Serotonin 5-HT Receptor Underlying the Pharmacology of Distinct Ligands.
[So] Source:ACS Chem Neurosci;8(1):28-39, 2017 Jan 18.
[Is] ISSN:1948-7193
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:While exploring the structure-activity relationship of 4-phenyl-2-dimethylaminotetralins (PATs) at serotonin 5-HT receptors, we discovered that relatively minor modification of PAT chemistry impacts function at 5-HT receptors. In HEK293 cells expressing human 5-HT receptors, for example, (-)-trans-3'-Br-PAT and (-)-trans-3'-Cl-PAT are agonists regarding Gα -inositol phosphate signaling, whereas (-)-trans-3'-CF -PAT is an inverse agonist. To investigate the ligand-receptor interactions that govern this change in function, we performed site-directed mutagenesis of 14 amino acids of the 5-HT receptor based on molecular modeling and reported G protein-coupled receptor crystal structures, followed by molecular pharmacology studies. We found that S3.36, T3.37, and F5.47 in the orthosteric binding pocket are critical for affinity (K ) of all PATs tested, we also found that F6.44, M6.47, C7.45, and S7.46 are primarily involved in regulating EC/IC functional potencies of PATs. We discovered that when residue S5.43, N6.55, or both are mutated to alanine, (-)-trans-3'-CF -PAT switches from inverse agonist to agonist function, and when N6.55 is mutated to leucine, (-)-trans-3'-Br-PAT switches from agonist to inverse agonist function. Notably, most point-mutations that affected PAT pharmacology did not significantly alter affinity (K ) of the antagonist radioligand [ H]mesulergine, but every mutation tested negatively impacted serotonin binding. Also, amino acid mutations differentially affected the pharmacology of other commercially available 5-HT ligands tested. Collectively, the data show that functional outcomes shared by different ligands are mediated by different amino acids and that some 5-HT receptor residues important for pharmacology of one ligand are not necessarily important for another ligand.
[Mh] Termos MeSH primário: Aminoácidos/genética
Mutagênese Sítio-Dirigida/métodos
Mutagênese/genética
Receptor 5-HT2C de Serotonina/genética
Receptor 5-HT2C de Serotonina/metabolismo
[Mh] Termos MeSH secundário: Análise de Variância
Sítios de Ligação/efeitos dos fármacos
Sítios de Ligação/genética
Glicolatos/síntese química
Glicolatos/química
Glicolatos/farmacocinética
Células HEK293
Seres Humanos
Fosfatos de Inositol/metabolismo
Ligantes
Modelos Moleculares
Ensaio Radioligante
Serotoninérgicos/farmacologia
Relação Estrutura-Atividade
Transfecção
Trítio/farmacocinética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amino Acids); 0 (Glycolates); 0 (Inositol Phosphates); 0 (Ligands); 0 (N-(2-(3,5-di-tert-butyl-4-hydroxyphenyl)-4-oxothiazolidin-3-yl-(4-chlorophenoxy))acetamide); 0 (Receptor, Serotonin, 5-HT2C); 0 (Serotonin Agents); 10028-17-8 (Tritium); 55780-80-8 (inositol-1-pyrophosphate)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160901
[St] Status:MEDLINE
[do] DOI:10.1021/acschemneuro.6b00124



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