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[PMID]: 29308855 [Au] Autor: Maslov LN; Karpov RS [Ti] Título: Prospects for the Use of Cannabinoid Receptor Ligands for the Treatment of Metabolic Syndrome and Atherosclerosis: Analysis of Experimental and Clinical Data. [So] Source: Vestn Ross Akad Med Nauk;72(1):59-65, 2017. [Is] ISSN: 0869-6047 [Cp] País de publicação: Russia (Federation) [La] Idioma: eng [Ab] Resumo: An antagonist of central cannabinoid CB1 receptors rimonabant causes weight loss in patients with obesity and metabolic syndrome, improves blood lipid parameters, increases the adiponectin level, decreases the rate of glucose and glycosylated hemoglobin in patients with diabetes mellitus type-2. However, rimonabant adverse effects include depression, anxiety, nausea, and dizziness which are apparently due to the blockade of central CB1 receptors. In mice with a high-calorie diet, we defined that the blockade of peripheral CB1 receptors prevents obesity, steatosis of the liver, improves lipid and carbohydrate metabolism. Experimental studies suggest that peripheral CB2 receptor agonists have antiatherogenic effect. To validate the expediency of clinical research of CB2 receptor agonists in patients with atherosclerosis the comparative analysis of antiatherogenic properties of cannabinoids should be performed. In addition, experiments are needed on the combination use of cannabinoids with well-known antiatherogenic agents, such as statins. [Mh] Termos MeSH primário: Aterosclerose/tratamento farmacológico Antagonistas de Receptores de Canabinoides/farmacologia Síndrome Metabólica/tratamento farmacológico Receptor CB1 de Canabinoide Receptor CB2 de Canabinoide [Mh] Termos MeSH secundário: Animais Aterosclerose/metabolismo Seres Humanos Ligantes Síndrome Metabólica/metabolismo Receptor CB1 de Canabinoide/antagonistas & inibidores Receptor CB1 de Canabinoide/metabolismo Receptor CB2 de Canabinoide/antagonistas & inibidores Receptor CB2 de Canabinoide/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE; REVIEW [Nm] Nome de substância: 0 (Cannabinoid Receptor Antagonists); 0 (Ligands); 0 (Receptor, Cannabinoid, CB1); 0 (Receptor, Cannabinoid, CB2) [Em] Mês de entrada: 1802 [Cu] Atualização por classe: 180220 [Lr] Data última revisão: 180220 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 180109 [St] Status: MEDLINE [do] DOI: 10.15690/vramn779

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[PMID]: 28934264 [Au] Autor: Asahi H; Inoue SI; Niikura M; Kunigo K; Suzuki Y; Kobayashi F; Sendo F [Ad] Endereço: Department of Infectious Diseases, Division of Tropical Diseases and Parasitology, Kyorin University School of Medicine, Tokyo, Japan. [Ti] Título: Profiling molecular factors associated with pyknosis and developmental arrest induced by an opioid receptor antagonist and dihydroartemisinin in Plasmodium falciparum. [So] Source: PLoS One;12(9):e0184874, 2017. [Is] ISSN: 1932-6203 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Malaria continues to be a devastating disease, largely caused by Plasmodium falciparum infection. We investigated the effects of opioid and cannabinoid receptor antagonists on the growth of intraerythrocytic P. falciparum. The delta opioid receptor antagonist 7-benzylidenenaltrexone (BNTX) and the cannabinoid receptor antagonists rimonaband and SR144528 caused growth arrest of the parasite. Notably BNTX and the established antimalarial drug dihydroartemisinin induced prominent pyknosis in parasite cells after a short period of incubation. We compared genome-wide transcriptome profiles in P. falciparum with different degrees of pyknosis in response to drug treatment, and identified 11 transcripts potentially associated with the evoking of pyknosis, of which three, including glutathione reductase (PfGR), triose phosphate transporter (PfoTPT), and a conserved Plasmodium membrane protein, showed markedly different gene expression levels in accordance with the degree of pyknosis. Furthermore, the use of specific inhibitors confirmed PfGR but not PfoTPT as a possible factor contributing to the development of pyknosis. A reduction in total glutathione levels was also detected in association with increased pyknosis. These results further our understanding of the mechanisms responsible for P. falciparum development and the antimalarial activity of dihydroartemisinin, and provide useful information for the development of novel antimalarial agents. [Mh] Termos MeSH primário: Antimaláricos/farmacologia Artemisininas/farmacologia Antagonistas de Receptores de Canabinoides/farmacologia Antagonistas de Entorpecentes/farmacologia Plasmodium falciparum/efeitos dos fármacos Plasmodium falciparum/metabolismo [Mh] Termos MeSH secundário: Compostos de Benzilideno/farmacologia Bornanos/farmacologia Morte Celular/efeitos dos fármacos Morte Celular/fisiologia Cromatina/efeitos dos fármacos Cromatina/metabolismo Relação Dose-Resposta a Droga Perfilação da Expressão Gênica Glutationa/metabolismo Naltrexona/análogos & derivados Naltrexona/farmacologia Oxirredução Piperidinas/farmacologia Plasmodium falciparum/crescimento & desenvolvimento Pirazóis/farmacologia Transcriptoma/efeitos dos fármacos [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antimalarials); 0 (Artemisinins); 0 (Benzylidene Compounds); 0 (Bornanes); 0 (Cannabinoid Receptor Antagonists); 0 (Chromatin); 0 (Narcotic Antagonists); 0 (Piperidines); 0 (Pyrazoles); 0 (SR 144528); 129468-28-6 (7-benzylidenenaltrexone); 5S6W795CQM (Naltrexone); 6A9O50735X (dihydroartemisinin); GAN16C9B8O (Glutathione); RML78EN3XE (rimonabant) [Em] Mês de entrada: 1710 [Cu] Atualização por classe: 171024 [Lr] Data última revisão: 171024 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170922 [St] Status: MEDLINE [do] DOI: 10.1371/journal.pone.0184874

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[PMID]: 28726401 [Au] Autor: Shi Y; Duan YH; Ji YY; Wang ZL; Wu YR; Gunosewoyo H; Xie XY; Chen JZ; Yang F; Li J; Tang J; Xie X; Yu LF [Ad] Endereço: Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University , 3663 North Zhongshan Road, Shanghai 200062, China. [Ti] Título: Amidoalkylindoles as Potent and Selective Cannabinoid Type 2 Receptor Agonists with in Vivo Efficacy in a Mouse Model of Multiple Sclerosis. [So] Source: J Med Chem;60(16):7067-7083, 2017 Aug 24. [Is] ISSN: 1520-4804 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Selective CB agonists represent an attractive therapeutic strategy for the treatment of a variety of diseases without psychiatric side effects mediated by the CB receptor. We carried out a rational optimization of a black market designer drug SDB-001 that led to the identification of potent and selective CB agonists. A 7-methoxy or 7-methylthio substitution at the 3-amidoalkylindoles resulted in potent CB antagonists (27 or 28, IC = 16-28 nM). Replacement of the amidoalkyls from 3-position to the 2-position of the indole ring dramatically increased the agonist selectivity on the CB over CB receptor. Particularly, compound 57 displayed a potent agonist activity on the CB receptor (EC = 114-142 nM) without observable agonist or antagonist activity on the CB receptor. Furthermore, 57 significantly alleviated the clinical symptoms and protected the murine central nervous system from immune damage in an experimental autoimmune encephalomyelitis (EAE) mouse model of multiple sclerosis. [Mh] Termos MeSH primário: Adamantano/análogos & derivados Agonistas de Receptores de Canabinoides/uso terapêutico Indóis/uso terapêutico Esclerose Múltipla/tratamento farmacológico Receptor CB2 de Canabinoide/agonistas [Mh] Termos MeSH secundário: Adamantano/síntese química Adamantano/farmacocinética Adamantano/uso terapêutico Animais Células CHO Agonistas de Receptores de Canabinoides/síntese química Agonistas de Receptores de Canabinoides/farmacocinética Antagonistas de Receptores de Canabinoides/síntese química Antagonistas de Receptores de Canabinoides/farmacologia Cricetulus Feminino Indóis/síntese química Indóis/farmacocinética Ligantes Camundongos Endogâmicos C57BL Simulação de Acoplamento Molecular Receptor CB1 de Canabinoide/agonistas Receptor CB1 de Canabinoide/antagonistas & inibidores Receptor CB2 de Canabinoide/antagonistas & inibidores Relação Estrutura-Atividade [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Cannabinoid Receptor Agonists); 0 (Cannabinoid Receptor Antagonists); 0 (Cnr2 protein, mouse); 0 (Indoles); 0 (Ligands); 0 (N-(adamantan-1-yl)-1-(4-hydroxybutyl)-1H-indole-2-carboxamide); 0 (Receptor, Cannabinoid, CB1); 0 (Receptor, Cannabinoid, CB2); PJY633525U (Adamantane) [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: 170721 [St] Status: MEDLINE [do] DOI: 10.1021/acs.jmedchem.7b00724

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[PMID]: 28606623 [Au] Autor: Donvito G; Bagdas D; Toma W; Rahimpour E; Jackson A; Meade JA; AlSharari S; Kulkarni AR; Ivy Carroll F; Lichtman AH; Papke RL; Thakur GA; Imad Damaj M [Ad] Endereço: Department of Pharmacology and Toxicology, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, VA, USA. Electronic address: giulia.donvito@vcuhealth.org. [Ti] Título: The interaction between alpha 7 nicotinic acetylcholine receptor and nuclear peroxisome proliferator-activated receptor-α represents a new antinociceptive signaling pathway in mice. [So] Source: Exp Neurol;295:194-201, 2017 Sep. [Is] ISSN: 1090-2430 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Recently, α7 nicotinic acetylcholine receptors (nAChRs), primarily activated by binding of orthosteric agonists, represent a target for anti-inflammatory and analgesic drug development. These receptors may also be modulated by positive allosteric modulators (PAMs), ago-allosteric ligands (ago-PAMs), and α7-silent agonists. Activation of α7 nAChRs has been reported to increase the brain levels of endogenous ligands for nuclear peroxisome proliferator-activated receptors type-α (PPAR-α), palmitoylethanolamide (PEA) and oleoylethanolamide (OEA), in a Ca -dependent manner. Here, we investigated potential crosstalk between α7 nAChR and PPAR-α, using the formalin test, a mouse model of tonic pain. Using pharmacological and genetic approaches, we found that PNU282987, a full α7 agonist, attenuated formalin-induced nociceptive behavior in α7-dependent manner. Interestingly, the selective PPAR-α antagonist GW6471 blocked the antinociceptive effects of PNU282987, but did not alter the antinociceptive responses evoked by the α7 nAChR PAM PNU120596, ago-PAM GAT107, and silent agonist NS6740. Moreover, GW6471 administered systemically or spinally, but not via the intraplantar surface of the formalin-injected paw blocked PNU282987-induced antinociception. Conversely, exogenous administration of the naturally occurring PPAR-α agonist PEA potentiated the antinociceptive effects of PNU282987. In contrast, the cannabinoid CB antagonist rimonabant and the CB antagonist SR144528 failed to reverse the antinociceptive effects of PNU282987. These findings suggest that PPAR-α plays a key role in a putative antinociceptive α7 nicotinic signaling pathway. [Mh] Termos MeSH primário: Nociceptividade/efeitos dos fármacos PPAR alfa/efeitos dos fármacos Transdução de Sinais/efeitos dos fármacos Receptor Nicotínico de Acetilcolina alfa7/efeitos dos fármacos [Mh] Termos MeSH secundário: Animais Compostos Azabicíclicos/farmacologia Benzamidas/farmacologia Compostos Bicíclicos com Pontes/farmacologia Antagonistas de Receptores de Canabinoides/farmacologia Etanolaminas/farmacologia Furanos/farmacologia Masculino Camundongos Camundongos Endogâmicos ICR Antagonistas Nicotínicos/farmacologia Oxazóis/farmacologia PPAR alfa/antagonistas & inibidores Medição da Dor/efeitos dos fármacos Ácidos Palmíticos/farmacologia Receptor Cross-Talk Tirosina/análogos & derivados Tirosina/farmacologia Receptor Nicotínico de Acetilcolina alfa7/antagonistas & inibidores [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (1,4-diazabicyclo(3.2.2)nonan-4-yl(5-(3-(trifluoromethyl)phenyl)furan-2-yl)methanone); 0 (Azabicyclo Compounds); 0 (Benzamides); 0 (Bridged Bicyclo Compounds); 0 (Cannabinoid Receptor Antagonists); 0 (Ethanolamines); 0 (Furans); 0 (GW 6471); 0 (Nicotinic Antagonists); 0 (Oxazoles); 0 (PNU-282987); 0 (PPAR alpha); 0 (Palmitic Acids); 0 (alpha7 Nicotinic Acetylcholine Receptor); 42HK56048U (Tyrosine); 6R8T1UDM3V (palmidrol) [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: 170614 [St] Status: MEDLINE

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[PMID]: 28533288 [Au] Autor: Hruba L; McMahon LR [Ad] Endereço: Department of Pharmacology, University of Texas Health Science Center at San Antonio, San Antonio, Texas. [Ti] Título: Apparent Affinity Estimates and Reversal of the Effects of Synthetic Cannabinoids AM-2201, CP-47,497, JWH-122, and JWH-250 by Rimonabant in Rhesus Monkeys. [So] Source: J Pharmacol Exp Ther;362(2):278-286, 2017 Aug. [Is] ISSN: 1521-0103 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Synthetic cannabinoids have been prohibited due to abuse liability and toxicity. Four such synthetic cannabinoids, AM-2201 ([1-(5-fluoropentyl)indol-3-yl]-naphthalen-1-ylmethanone), CP-47,497 (2-[(1R,3S)-3-hydroxycyclohexyl]-5-(2-methyloctan-2-yl)phenol), JWH-122 [(4-methylnaphthalen-1-yl)-(1-pentylindol-3-yl)methanone], and JWH-250 [2-(2-methoxyphenyl)-1-(1-pentylindol-3-yl)ethanone], were tested for their capacity to produce CB receptor-mediated discriminative stimulus effects in two groups of rhesus monkeys. One group ( = 4) discriminated Δ -tetrahydrocannabinol (∆ -THC; 0.1 mg/kg i.v.), and a second group ( = 4) discriminated the cannabinoid antagonist rimonabant (1 mg/kg i.v.) while receiving 1 mg/kg/12 hours of ∆ -THC. AM-2201, JWH-122, CP-47,497, JWH-250, and ∆ -THC increased ∆ -THC lever responding. Duration of action was 1-2 hours for AM-2201, JWH-122, and JWH-250 and 4-5 hours for CP-47,497 and ∆ -THC. Rimonabant (1 mg/kg) surmountably antagonized the discriminative stimulus effects of all cannabinoid agonists; the magnitude of rightward shift was 10.6-fold for AM-2201, 10.7-fold for JWH-122, 11.0-fold for CP-47,497, and 15.7-fold for JWH-250. The respective pK values were not significantly different: 6.61, 6.65, 6.66, and 6.83. In ∆ -THC-treated monkeys discriminating rimonabant, AM-2201 (0.1 and 0.32 mg/kg), JWH-122 (0.32 and 1 mg/kg), JWH-250 (1 and 3.2 mg/kg), and CP-47,497 (0.32, 1, and 3.2 mg/kg) produced not only rate-decreasing effects that were reversed by rimonabant, but also dose-dependent, rightward shifts in the rimonabant discrimination dose-effect function. These results show striking similarity in the CB receptor mechanism mediating the subjective effects of AM-2201, JWH-122, JWH-250, and CP-47,497. For products containing AM-2201 and JWH-122, a short duration of action could lead to more frequent use; moreover, inattention to differences in potency among synthetic cannabinoids could underlie unexpected toxicity. Rapid reversal of effects by intravenous rimonabant has potential value in emergency situations. [Mh] Termos MeSH primário: Antagonistas de Receptores de Canabinoides/metabolismo Canabinoides/metabolismo Cicloexanóis/metabolismo Indóis/metabolismo Naftalenos/metabolismo Piperidinas/metabolismo Pirazóis/metabolismo [Mh] Termos MeSH secundário: Animais Antagonistas de Receptores de Canabinoides/farmacologia Canabinoides/farmacologia Cicloexanóis/farmacologia Aprendizagem por Discriminação/efeitos dos fármacos Aprendizagem por Discriminação/fisiologia Relação Dose-Resposta a Droga Feminino Indóis/farmacologia Macaca mulatta Masculino Naftalenos/farmacologia Piperidinas/farmacologia Pirazóis/farmacologia Receptor CB1 de Canabinoide/agonistas Receptor CB1 de Canabinoide/antagonistas & inibidores Receptor CB1 de Canabinoide/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 ((4-methyl-1-naphthyl)-(1-pentylindol-3-yl)methanone); 0 (1-((5-fluoropentyl)-1H-indol-3-yl)-(naphthalen-1-yl)methanone); 0 (Cannabinoid Receptor Antagonists); 0 (Cannabinoids); 0 (Cyclohexanols); 0 (Indoles); 0 (Naphthalenes); 0 (Piperidines); 0 (Pyrazoles); 0 (Receptor, Cannabinoid, CB1); 70434-82-1 (CP 47497); RML78EN3XE (rimonabant) [Em] Mês de entrada: 1708 [Cu] Atualização por classe: 170802 [Lr] Data última revisão: 170802 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170524 [St] Status: MEDLINE [do] DOI: 10.1124/jpet.117.240572

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[PMID]: 28492810 [Au] Autor: Chen B; Hu N [Ad] Endereço: Department of Orthopedics, Zhongnan Hospital, Wuhan University, Wuhan, Hubei Province, China. [Ti] Título: Rimonabant improves metabolic parameters partially attributed to restoration of high voltage-activated Ca2+ channels in skeletal muscle in HFD-fed mice. [So] Source: Braz J Med Biol Res;50(6):e6141, 2017 May 04. [Is] ISSN: 1414-431X [Cp] País de publicação: Brazil [La] Idioma: eng [Ab] Resumo: Cannabinoid type 1 receptor (CB1R) inhibition tends to be one of the promising strategies for the treatment of obesity and other related metabolic disorders. Although CB1R inhibition may cause adverse psychiatric effects including depression and anxiety, the investigation of the role of peripheral CB1R on weight loss and related metabolic parameters are urgently needed. We first explored the effect of rimonabant, a selective CB1R antagonist/inverse agonist, on some metabolic parameters in high fat-diet (HFD)-induced obesity in mice. Then, real-time PCR and electrophysiology were used to explore the contribution of high voltage-activated Ca2+ channels (HVACCs), especially Cav1.1, on rimonabant's effect in skeletal muscle (SM) in HFD-induced obesity. Five-week HFD feeding caused body weight gain, and decreased glucose/insulin tolerance in mice compared to those in the regular diet group (P<0.05), which was restored by rimonabant treatment compared to the HFD group (P<0.05). Interestingly, HVACCs and Cav1.1 were decreased in soleus muscle cells in the HFD group compared to the control group. Daily treatment with rimonabant for 5 weeks was shown to counter such decrease (P<0.05). Collectively, our findings provided a novel understanding for peripheral CB1R's role in the modulation of body weight and glucose homeostasis and highlight peripheral CB1R as well as Cav1.1 in the SM as potential targets for obesity treatment. [Mh] Termos MeSH primário: Glicemia/efeitos dos fármacos Canais de Cálcio/efeitos dos fármacos Antagonistas de Receptores de Canabinoides/farmacologia Músculo Esquelético/efeitos dos fármacos Piperidinas/farmacologia Pirazóis/farmacologia Receptor CB1 de Canabinoide/antagonistas & inibidores [Mh] Termos MeSH secundário: Animais Peso Corporal/efeitos dos fármacos Canais de Cálcio/metabolismo Canais de Cálcio Tipo L/efeitos dos fármacos Canais de Cálcio Tipo L/metabolismo Dieta Hiperlipídica/efeitos adversos Intolerância à Glucose/etiologia Resistência à Insulina Masculino Camundongos Endogâmicos C57BL Modelos Animais Músculo Esquelético/metabolismo Obesidade/etiologia Receptor CB1 de Canabinoide/fisiologia [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Blood Glucose); 0 (Calcium Channels); 0 (Calcium Channels, L-Type); 0 (Cannabinoid Receptor Antagonists); 0 (Piperidines); 0 (Pyrazoles); 0 (Receptor, Cannabinoid, CB1); RML78EN3XE (rimonabant) [Em] Mês de entrada: 1709 [Cu] Atualização por classe: 170925 [Lr] Data última revisão: 170925 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170512 [St] Status: MEDLINE

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[PMID]: 28442584 [Au] Autor: Grim TW; Morales AJ; Thomas BF; Wiley JL; Endres GW; Negus SS; Lichtman AH [Ad] Endereço: Department of Pharmacology, Virginia Commonwealth University, Richmond, Virginia (T.W.G., A.J.M., S.S.N., A.H.L.); RTI International, Research Triangle Park, North Carolina (B.F.T., J.L.W.); and PinPoint Testing, LLC, AR (G.W.E.) tgrim@scripps.edu. [Ti] Título: Apparent CB Receptor Rimonabant Affinity Estimates: Combination with THC and Synthetic Cannabinoids in the Mouse In Vivo Triad Model. [So] Source: J Pharmacol Exp Ther;362(1):210-218, 2017 Jul. [Is] ISSN: 1521-0103 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Synthetic cannabinoids (SCs) represent an emerging class of abused drugs associated with psychiatric complications and other substantial health risks. These ligands are largely sold over the internet for human consumption, presumably because of their high cannabinoid 1 receptor (CB R) affinity and their potency in eliciting pharmacological effects similar to Δ -tetrahydrocannabinol (THC), as well as circumventing laws illegalizing this plant. Factors potentially contributing to the increased prevalence of SC abuse and related hospitalizations, such as increased CB R efficacy and non-CB R targets, highlight the need for quantitative pharmacological analyses to determine receptor mediation of the pharmacological effects of cannabinoids. Accordingly, the present study used pA and pK analyses for quantitative determination of CB R mediation in which we utilized the CB R-selective inverse agonist/antagonist rimonabant to elicit rightward shifts in the dose-response curves of five SCs (i.e., A-834,735D; WIN55,212-2; CP55,950; JWH-073; and CP47,497) and THC in producing common cannabimimetic effects (i.e., catalepsy, antinociception, and hypothermia). The results revealed overall similarity of pA and pK values for these compounds and suggest that CB Rs, and not other pharmacological targets, largely mediated the central pharmacological effects of SCs. More generally, affinity estimation offers a powerful pharmacological approach to assess potential receptor heterogeneity subserving in vivo pharmacological effects of SCs. [Mh] Termos MeSH primário: Agonistas de Receptores de Canabinoides/metabolismo Antagonistas de Receptores de Canabinoides/metabolismo Canabinoides/metabolismo Dronabinol/metabolismo Piperidinas/metabolismo Pirazóis/metabolismo Receptor CB1 de Canabinoide/metabolismo [Mh] Termos MeSH secundário: Animais Agonistas de Receptores de Canabinoides/administração & dosagem Antagonistas de Receptores de Canabinoides/administração & dosagem Canabinoides/administração & dosagem Relação Dose-Resposta a Droga Dronabinol/administração & dosagem Combinação de Medicamentos Feminino Masculino Camundongos Camundongos Endogâmicos C57BL Camundongos Transgênicos Piperidinas/administração & dosagem Pirazóis/administração & dosagem Receptor CB1 de Canabinoide/agonistas Receptor CB1 de Canabinoide/antagonistas & inibidores [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Cannabinoid Receptor Agonists); 0 (Cannabinoid Receptor Antagonists); 0 (Cannabinoids); 0 (Drug Combinations); 0 (Piperidines); 0 (Pyrazoles); 0 (Receptor, Cannabinoid, CB1); 7J8897W37S (Dronabinol); RML78EN3XE (rimonabant) [Em] Mês de entrada: 1708 [Cu] Atualização por classe: 170929 [Lr] Data última revisão: 170929 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170427 [St] Status: MEDLINE [do] DOI: 10.1124/jpet.117.240192

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[PMID]: 28421836 [Au] Autor: Abouchedid R; Hudson S; Thurtle N; Yamamoto T; Ho JH; Bailey G; Wood M; Sadones N; Stove CP; Dines A; Archer JRH; Wood DM; Dargan PI [Ad] Endereço: a Clinical Toxicology , Guy's and St Thomas' NHS Foundation Trust , London , UK. [Ti] Título: Analytical confirmation of synthetic cannabinoids in a cohort of 179 presentations with acute recreational drug toxicity to an Emergency Department in London, UK in the first half of 2015. [So] Source: Clin Toxicol (Phila);55(5):338-345, 2017 Jun. [Is] ISSN: 1556-9519 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: CONTEXT: Synthetic cannabinoid receptor agonists are the largest group of new psychoactive substances reported in the last decade; in this study we investigated how commonly these drugs are found in patients presenting to the Emergency Department with acute recreational drug toxicity. METHODS: We conducted an observational cohort study enrolling consecutive adult patients presenting to an Emergency Department (ED) in London (UK) January-July 2015 (6 months) with acute recreational drug toxicity. Residual serum obtained from a serum sample taken as part of routine clinical care was analyzed using high-resolution accurate mass-spectrometry with liquid-chromatography (HRAM-LCMSMS). Minimum clinical data were obtained from ED medical records. RESULTS: 18 (10%) of the 179 patient samples were positive for synthetic cannabinoid receptor agonists. The most common was 5F AKB-48 (13 samples, concentration 50-7600 pg/ml), followed by 5F PB-22 (7, 30-400 pg/mL), MDMB-CHMICA (7, 80-8000 pg/mL), AB-CHMINACA (3, 50-1800 pg/mL), Cumyl 5F-PINACA (1, 800 pg/mL) and BB-22 (1, 60 pg/mL). Only 9/18 (50%) in whom synthetic cannabinoid receptor agonists were detected self-reported synthetic cannabinoid receptor agonist use. The most common clinical features were seizures and agitation, both recorded in four (22%) individuals. Fourteen patients (78%) were discharged from the ED, one of the four admitted to hospital was admitted to critical care. CONCLUSIONS: Synthetic cannabinoid receptor agonists were found in 10% of this cohort with acute recreational drug toxicity but self-reported in only half of these. This suggests that presentations to the ED with acute synthetic cannabinoid receptor agonist toxicity may be more common than reported. [Mh] Termos MeSH primário: Antagonistas de Receptores de Canabinoides/efeitos adversos Antagonistas de Receptores de Canabinoides/sangue Overdose de Drogas/sangue Serviço Hospitalar de Emergência [Mh] Termos MeSH secundário: Adamantano/administração & dosagem Adamantano/análogos & derivados Adamantano/sangue Adolescente Adulto Idoso Estudos de Coortes Overdose de Drogas/diagnóstico Feminino Seres Humanos Indazóis/administração & dosagem Indazóis/sangue Indóis/sangue Londres Masculino Meia-Idade Estudos Prospectivos Drogas Ilícitas/efeitos adversos Drogas Ilícitas/sangue Detecção do Abuso de Substâncias Espectrometria de Massas em Tandem Valina/análogos & derivados Valina/sangue Adulto Jovem [Pt] Tipo de publicação: JOURNAL ARTICLE; OBSERVATIONAL STUDY [Nm] Nome de substância: 0 (Cannabinoid Receptor Antagonists); 0 (Indazoles); 0 (Indoles); 0 (N-(1-(aminocarbonyl)-2-methylpropyl)-1-(cyclohexylmethyl)-1H-indazole-3-carboxamide); 0 (N-(1-adamantyl)-1-(5-fluoropentyl)-1H-indazole-3-carboxamide); 0 (Street Drugs); 0 (methyl 2-(1-(cyclohexylmethyl)-1H-indole-3-carboxamido)-3,3-dimethylbutanoate); HG18B9YRS7 (Valine); PJY633525U (Adamantane) [Em] Mês de entrada: 1704 [Cu] Atualização por classe: 170425 [Lr] Data última revisão: 170425 [Sb] Subgrupo de revista: AIM; IM [Da] Data de entrada para processamento: 170420 [St] Status: MEDLINE [do] DOI: 10.1080/15563650.2017.1287373

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[PMID]: 28400256 [Au] Autor: Sergeeva OA; De Luca R; Mazur K; Chepkova AN; Haas HL; Bauer A [Ad] Endereço: Institute of Clinical Neurosciences and Medical Psychology, Medical Faculty of Heinrich-Heine University, D 40225 Düsseldorf, Germany; Institute of Neural and Sensory Physiology, Medical Faculty of Heinrich-Heine University, D 40225 Düsseldorf, Germany. Electronic address: olga.sergeeva@uni-duesseld [Ti] Título: N-oleoyldopamine modulates activity of midbrain dopaminergic neurons through multiple mechanisms. [So] Source: Neuropharmacology;119:111-122, 2017 Jun. [Is] ISSN: 1873-7064 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: N-oleoyl-dopamine (OLDA) is an amide of dopamine and oleic acid, synthesized in catecholaminergic neurons. The present study investigates OLDA targets in midbrain dopaminergic (DA) neurons. Substantia Nigra compacta (SNc) DA neurons recorded in brain slices were excited by OLDA in wild type mice. In transient receptor potential vanilloid 1 (TRPV1) knockout (KO) mice, however, SNc DA neurons displayed sustained inhibition of firing. In the presence of the dopamine type 2 receptor (D2R) antagonist sulpiride or the dopamine transporter blocker nomifensine no such inhibition was observed. Under sulpiride OLDA slightly excited SNc DA neurons, an action abolished upon combined application of the cannabinoid1 and 2 receptor antagonists AM251 and AM630. In ventral tegmental area (VTA) DA neurons from TRPV1 KO mice a transient inhibition of firing by OLDA was observed. Thus OLDA modulates the firing of nigrostriatal DA neurons through interactions with TRPV1, cannabinoid receptors and dopamine uptake. These findings suggest further development of OLDA-like tandem molecules for the treatment of movement disorders including Parkinson's disease. [Mh] Termos MeSH primário: Dopaminérgicos/farmacologia Dopamina/análogos & derivados Neurônios Dopaminérgicos/efeitos dos fármacos Mesencéfalo/citologia Canais de Cátion TRPV/metabolismo [Mh] Termos MeSH secundário: Acrilamidas/farmacologia Potenciais de Ação/efeitos dos fármacos Fatores Etários Animais Animais Recém-Nascidos Compostos Bicíclicos Heterocíclicos com Pontes/farmacologia Antagonistas de Receptores de Canabinoides/farmacologia Dopamina/farmacologia Proteínas da Membrana Plasmática de Transporte de Dopamina/genética Proteínas da Membrana Plasmática de Transporte de Dopamina/metabolismo Proteínas Luminescentes/genética Proteínas Luminescentes/metabolismo Camundongos Camundongos Endogâmicos C57BL Camundongos Transgênicos Inibição Neural/efeitos dos fármacos Técnicas de Patch-Clamp Piperidinas/farmacologia Pirazóis/farmacologia Canais de Cátion TRPV/antagonistas & inibidores Canais de Cátion TRPV/genética Tirosina 3-Mono-Oxigenase/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo(b)(1,4)dioxin-6-yl)acrylamide); 0 (Acrylamides); 0 (Bridged Bicyclo Compounds, Heterocyclic); 0 (Cannabinoid Receptor Antagonists); 0 (Dopamine Agents); 0 (Dopamine Plasma Membrane Transport Proteins); 0 (Luminescent Proteins); 0 (Piperidines); 0 (Pyrazoles); 0 (TRPV Cation Channels); 0 (TRPV1 protein, mouse); 3I4FA44MAI (AM 251); EC 1.14.16.2 (Tyrosine 3-Monooxygenase); T87P7X9XSZ (N-oleoyldopamine); VTD58H1Z2X (Dopamine) [Em] Mês de entrada: 1708 [Cu] Atualização por classe: 171116 [Lr] Data última revisão: 171116 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170413 [St] Status: MEDLINE

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[PMID]: 28366798 [Au] Autor: Marinho EAV; Oliveira-Lima AJ; Yokoyama TS; Santos-Baldaia R; Ribeiro LTC; Baldaia MA; da Silva RW; Hollais AW; Talhati F; Longo BM; Berro LF; Frussa-Filho R [Ad] Endereço: Department of Health Sciences, Universidade Estadual de Santa Cruz, Rod. Ilhéus/Itabuna, Km 16, 45662-0 Ilhéus, BA, Brazil. Electronic address: edumarinho@hotmail.com. [Ti] Título: Post-sensitization treatment with rimonabant blocks the expression of cocaine-induced behavioral sensitization and c-Fos protein in mice. [So] Source: Pharmacol Biochem Behav;156:16-23, 2017 May. [Is] ISSN: 1873-5177 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: CB1 receptor antagonists have been shown to prevent acute and long-term behavioral effects of cocaine. Here we evaluate the effectiveness of the CB1 receptor antagonist rimonabant to modify sensitized responses to cocaine. Mice were treated with saline or cocaine injections in a 15-day intermittent sensitization treatment and subsequently treated with either vehicle, 1 or 10mg/kg rimonabant in the drug-associated environment for 8 consecutive days. Animals were then challenged with saline and cocaine in the open-field apparatus on subsequent days to evaluate the expression of conditioned and sensitized effects to cocaine. c-Fos protein expression was evaluated in the nucleus accumbens (NAcc), ventral tegmental area (VTA), basolateral amygdala (BLA), medial prefrontal cortex (mPFC) and caudate-putamen (CPu) after the last (cocaine) challenge. Previous treatment with 10mg/kg rimonabant blocked the expression of conditioned hyperlocomotion and behavioral sensitization to cocaine, but not acute cocaine-induced hyperlocomotion. These behavioral effects were accompanied by significant changes in c-Fos expression in the brain reward system. Chronic cocaine sensitization blunted a subsequent acute cocaine-induced increase in c-Fos protein in the NAcc, effect that was reversed by previous treatment with rimonabant. Treatment with 10mg/kg rimonabant also attenuated the significant increase in c-Fos expression in the CPu, mPFC and BLA induced by previous chronic sensitization with cocaine. Our findings add to the evidence that drugs targeting CB1 receptors are good candidates for the treatment of cocaine abuse and provide further insights into the mechanisms underlying endocannabinoid signaling within the brain reward system in the context of cocaine abuse. [Mh] Termos MeSH primário: Comportamento Animal/efeitos dos fármacos Antagonistas de Receptores de Canabinoides/farmacologia Cocaína/farmacologia Piperidinas/farmacologia Proteínas Proto-Oncogênicas c-fos/metabolismo Pirazóis/farmacologia [Mh] Termos MeSH secundário: Animais Locomoção/efeitos dos fármacos Masculino Camundongos [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Cannabinoid Receptor Antagonists); 0 (Piperidines); 0 (Proto-Oncogene Proteins c-fos); 0 (Pyrazoles); I5Y540LHVR (Cocaine); RML78EN3XE (rimonabant) [Em] Mês de entrada: 1711 [Cu] Atualização por classe: 171109 [Lr] Data última revisão: 171109 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170404 [St] Status: MEDLINE

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