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[PMID]: 28456841 [Au] Autor: Blanco-Gandía MC; Aracil-Fernández A; Montagud-Romero S; Aguilar MA; Manzanares J; Miñarro J; Rodríguez-Arias M [Ad] Endereço: Departamento de Psicobiología, Facultad de Psicología, Unidad de Investigación Psicobiología de las Drogodependencias, , Universitat de València, Avda. Blasco Ibáñez, 21, 46010, Valencia, Spain. [Ti] Título: Changes in gene expression and sensitivity of cocaine reward produced by a continuous fat diet. [So] Source: Psychopharmacology (Berl);234(15):2337-2352, 2017 Aug. [Is] ISSN: 1432-2072 [Cp] País de publicação: Germany [La] Idioma: eng [Ab] Resumo: RATIONALE: Preclinical studies report that free access to a high-fat diet (HFD) alters the response to psychostimulants. OBJECTIVES: The aim of the present study was to examine how HFD exposure during adolescence modifies cocaine effects. Gene expression of CB1 and mu-opioid receptors (MOr) in the nucleus accumbens (N Acc) and prefrontal cortex (PFC) and ghrelin receptor (GHSR) in the ventral tegmental area (VTA) were assessed. METHODS: Mice were allowed continuous access to fat from PND 29, and the locomotor (10 mg/kg) and reinforcing effects of cocaine (1 and 6 mg/kg) on conditioned place preference (CPP) were evaluated on PND 69. Another group of mice was exposed to a standard diet until the day of post-conditioning, on which free access to the HFD began. RESULTS: HFD induced an increase of MOr gene expression in the N Acc, but decreased CB1 receptor in the N Acc and PFC. After fat withdrawal, the reduction of CB1 receptor in the N Acc was maintained. Gene expression of GHSR in the VTA decreased during the HFD and increased after withdrawal. Following fat discontinuation, mice exhibited increased anxiety, augmented locomotor response to cocaine, and developed CPP for 1 mg/kg cocaine. HFD reduced the number of sessions required to extinguish the preference and decreased sensitivity to drug priming-induced reinstatement. CONCLUSION: Our results suggest that consumption of a HFD during adolescence induces neurobiochemical changes that increased sensitivity to cocaine when fat is withdrawn, acting as an alternative reward. [Mh] Termos MeSH primário: Cocaína/farmacologia Dieta Hiperlipídica/psicologia Dieta Hiperlipídica/tendências Receptor CB1 de Canabinoide/biossíntese Receptor CB1 de Canabinoide/genética Recompensa [Mh] Termos MeSH secundário: Animais Condicionamento Clássico/efeitos dos fármacos Condicionamento Clássico/fisiologia Expressão Gênica Masculino Camundongos Núcleo Accumbens/efeitos dos fármacos Núcleo Accumbens/metabolismo Córtex Pré-Frontal/efeitos dos fármacos Córtex Pré-Frontal/metabolismo Receptores de Grelina/metabolismo Receptores Opioides mu/metabolismo Reforço (Psicologia) Área Tegmentar Ventral/efeitos dos fármacos Área Tegmentar Ventral/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Receptor, Cannabinoid, CB1); 0 (Receptors, Ghrelin); 0 (Receptors, Opioid, mu); I5Y540LHVR (Cocaine) [Em] Mês de entrada: 1803 [Cu] Atualização por classe: 180306 [Lr] Data última revisão: 180306 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170501 [St] Status: MEDLINE [do] DOI: 10.1007/s00213-017-4630-9

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[PMID]: 29265141 [Au] Autor: Sader S; Anant K; Wu C [Ad] Endereço: College of Science and Mathematics, Rowan University, Glassboro, NJ 08028, USA. wuc@rowan.edu. [Ti] Título: To probe interaction of morphine and IBNtxA with 7TM and 6TM variants of the human µ-opioid receptor using all-atom molecular dynamics simulations with an explicit membrane. [So] Source: Phys Chem Chem Phys;20(3):1724-1741, 2018 Jan 17. [Is] ISSN: 1463-9084 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: IBNtxA, a morphine derivative, is 10-fold more potent and has a better safety profile than morphine. Animal studies indicate that the analgesic effect of IBNtxA appears to be mediated by the activation of truncated splice variants (6TM) of the Mu opioid receptor (MOR-1) where transmembrane helix 1 (TM1) is removed. Interestingly, morphine is unable to activate 6TM variants. To date, a high resolution structure of 6TM variants is missing, and the interaction of 6TM variants with IBNtxA and morphine remains elusive. In this study we used homology modeling, docking and molecular dynamics (MD) simulations to study a representative 6TM variant (G1) and a full-length 7TM variant of human MOR-1 in complex with IBNtxA and morphine respectively. The structural models of human G1 and 7TM were obtained by homology modeling using the X-ray solved crystal structure of the active mouse 7TM bound to an agonist BU72 (PDB id: ) as the template. Our 6000 ns MD data show that either TM1 truncation (i.e. from 7TM to 6TM) or ligand modification (i.e. from morphine to IBNtxA) alone causes the loss of key morphine-7TM interactions that are well-known to be required for MOR-1 activation. Receptor disruptions are mainly located at TMs 2, 3, 6 and 7 in comparison with the active crystal complex. However, when both perturbations occur in the 6TM-IBNtxA complex, the key ligand-receptor interactions and the receptor conformation are recovered to resemble those in the active 7TM-morphine complex. Our molecular switch analysis further explains well why morphine is not able to activate 6TM variants. The close resemblance between 6TM-IBTtxA and 7TM in complex with PZM21, a G-protein biased 7TM agonist, suggests the possible biased agonism of IBNtxA on G1, which is consistent with its reduced side effects. [Mh] Termos MeSH primário: Simulação de Dinâmica Molecular Morfina/metabolismo Naltrexona/análogos & derivados Receptores Opioides mu/metabolismo [Mh] Termos MeSH secundário: Sequência de Aminoácidos Animais Sítios de Ligação Seres Humanos Ligantes Camundongos Morfina/química Mutagênese Naltrexona/química Naltrexona/metabolismo Domínios Proteicos Receptores Opioides mu/química Receptores Opioides mu/genética Alinhamento de Sequência [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Ligands); 0 (Receptors, Opioid, mu); 0 (iodobenzoylnaltrexamide); 5S6W795CQM (Naltrexone); 76I7G6D29C (Morphine) [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: 171222 [St] Status: MEDLINE [do] DOI: 10.1039/c7cp06745c

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[PMID]: 28743600 [Au] Autor: Lee JR; Muckerman JE; Wright AM; Davis DJ; Childs TE; Gillespie CE; Vieira-Potter VJ; Booth FW; Ericsson AC; Will MJ [Ad] Endereço: Interdisciplinary Neuroscience Program, University of Missouri, Columbia, MO, USA; Christopher Bond Life Sciences Center, University of Missouri, Columbia, MO, USA. Electronic address: jrl5d5@mail.missouri.edu. [Ti] Título: Sex determines effect of physical activity on diet preference: Association of striatal opioids and gut microbiota composition. [So] Source: Behav Brain Res;334:16-25, 2017 09 15. [Is] ISSN: 1872-7549 [Cp] País de publicação: Netherlands [La] Idioma: eng [Ab] Resumo: Previous studies suggest an interaction between the level of physical activity and diet preference. However, this relationship has not been well characterized for sex differences that may exist. The present study examined the influence of sex on diet preference in male and female Wistar rats that were housed under either sedentary (no wheel access) (SED) or voluntary wheel running access (RUN) conditions. Following a 1 week acclimation period to these conditions, standard chow was replaced with concurrent ad libitum access to a choice of 3 pelleted diets (high-fat, high-sucrose, and high-corn starch) in the home cage. SED and RUN conditions remained throughout the next 4 week diet preference assessment period. Body weight, running distance, and intake of each diet were measured daily. At the conclusion of the 4 week diet preference test, animals were sacrificed and brains were collected for mRNA analysis. Fecal samples were also collected before and after the 4 week diet preference phase to characterize microbiota composition. Results indicate sex dependent interactions between physical activity and both behavioral and physiological measures. Females in both RUN and SED conditions preferred the high-fat diet, consuming significantly more high-fat diet than either of the other two diets. While male SED rats also preferred the high-fat diet, male RUN rats consumed significantly less high-fat diet than the other groups, instead preferring all three diets equally. There was also a sex dependent influence of physical activity on both reward related opioid mRNA expression in the ventral striatum and the characterization of gut microbiota. The significant sex differences in response to physical activity observed through both behavioral and physiological measures suggest potential motivational or metabolic difference between males and females. The findings highlight the necessity for further exploration between male and female response to physical activity and feeding behavior. [Mh] Termos MeSH primário: Dieta/psicologia Preferências Alimentares/fisiologia Microbioma Gastrointestinal/fisiologia Corrida/fisiologia Caracteres Sexuais Estriado Ventral/metabolismo [Mh] Termos MeSH secundário: Animais Gorduras na Dieta Sacarose na Dieta Ingestão de Alimentos/fisiologia Ingestão de Alimentos/psicologia Fezes/microbiologia Feminino Preferências Alimentares/psicologia Masculino Motivação/fisiologia RNA Mensageiro/metabolismo Ratos Wistar Receptores de Dopamina D2/metabolismo Receptores Opioides mu/metabolismo Recompensa Corrida/psicologia Amido [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (DRD2 protein, rat); 0 (Dietary Fats); 0 (Dietary Sucrose); 0 (Oprm1 protein, rat); 0 (RNA, Messenger); 0 (Receptors, Dopamine D2); 0 (Receptors, Opioid, mu); 9005-25-8 (Starch) [Em] Mês de entrada: 1712 [Cu] Atualização por classe: 180104 [Lr] Data última revisão: 180104 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170727 [St] Status: MEDLINE

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[PMID]: 29211767 [Au] Autor: Leong C; Neumann C; Ramasamy S; Rout B; Yi Wee L; Bigliardi-Qi M; Bigliardi PL [Ad] Endereço: Institute of Medical Biology, Agency for Science Technology & Research (A*STAR), Singapore, Singapore. [Ti] Título: Investigating endogenous µ-opioid receptors in human keratinocytes as pharmacological targets using novel fluorescent ligand. [So] Source: PLoS One;12(12):e0188607, 2017. [Is] ISSN: 1932-6203 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Opioids in skin function during stress response, regeneration, ageing and, particularly in regulating sensation. In chronic pruritus, topical treatment with Naltrexone changes µ-opioid receptor (µ-OR) localization to relieve itch. The molecular mechanisms behind the effects of Naltrexone on µ-OR function in reduction of itching behavior has not been studied. There is an immediate need to understand the endogenous complexity of µ-OR dynamics in normal and pathological skin conditions. Here we evaluate real-time behavior of µ-OR-Endomorphine complexes in the presence of agonist and antagonists. The µ-OR ligand Endomorphine-1 (EM) was conjugated to the fluorescent dye Tetramethylrhodamine (TAMRA) to investigate the effects of agonist and antagonists in N/TERT-1 keratinocytes. The cellular localization of the EM-TAMRA was followed through time resolved confocal microscopy and population analysis was performed by flow cytometry. The in vitro analyses demonstrate fast internalization and trafficking of the endogenous EM-TAMRA-µ-OR interactions in a qualitative manner. Competition with Endomorphine-1, Naltrexone and CTOP show both canonical and non-canonical effects in basal and differentiated keratinocytes. Acute and chronic treatment with Naltrexone and Endomorphine-1 increases EM-TAMRA binding to skin cells. Although Naltrexone is clinically effective in relieving itch, the mechanisms behind re-distribution of µ-ORs during clinical treatments are not known. Our study has given insight into cellular mechanisms of µ-OR ligand-receptor interactions after opioid agonist and antagonist treatments in vitro. These findings potentially offer opportunities in using novel treatment strategies for skin and peripheral sensory disorders. [Mh] Termos MeSH primário: Corantes Fluorescentes/metabolismo Queratinócitos/metabolismo Receptores Opioides mu/metabolismo [Mh] Termos MeSH secundário: Células Cultivadas Seres Humanos Ligantes Espectrometria de Fluorescência [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Fluorescent Dyes); 0 (Ligands); 0 (Receptors, Opioid, mu) [Em] Mês de entrada: 1712 [Cu] Atualização por classe: 171229 [Lr] Data última revisão: 171229 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 171207 [St] Status: MEDLINE [do] DOI: 10.1371/journal.pone.0188607

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[PMID]: 27778501 [Au] Autor: Schneider S; Provasi D; Filizola M [Ad] Endereço: Department of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai , New York, New York 10029, United States. [Ti] Título: How Oliceridine (TRV-130) Binds and Stabilizes a µ-Opioid Receptor Conformational State That Selectively Triggers G Protein Signaling Pathways. [So] Source: Biochemistry;55(46):6456-6466, 2016 Nov 22. [Is] ISSN: 1520-4995 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Substantial attention has recently been devoted to G protein-biased agonism of the µ-opioid receptor (MOR) as an ideal new mechanism for the design of analgesics devoid of serious side effects. However, designing opioids with appropriate efficacy and bias is challenging because it requires an understanding of the ligand binding process and of the allosteric modulation of the receptor. Here, we investigated these phenomena for TRV-130, a G protein-biased MOR small-molecule agonist that has been shown to exert analgesia with less respiratory depression and constipation than morphine and that is currently being evaluated in human clinical trials for acute pain management. Specifically, we carried out multimicrosecond, all-atom molecular dynamics (MD) simulations of the binding of this ligand to the activated MOR crystal structure. Analysis of >50 µs of these MD simulations provides insights into the energetically preferred binding pathway of TRV-130 and its stable pose at the orthosteric binding site of MOR. Information transfer from the TRV-130 binding pocket to the intracellular region of the receptor was also analyzed, and was compared to a similar analysis carried out on the receptor bound to the classical unbiased agonist morphine. Taken together, these studies lead to a series of testable hypotheses of ligand-receptor interactions that are expected to inform the structure-based design of improved opioid analgesics. [Mh] Termos MeSH primário: Conformação Proteica Receptores Opioides mu/química Transdução de Sinais Compostos de Espiro/química Tiofenos/química [Mh] Termos MeSH secundário: Aminoácidos/genética Sítios de Ligação/genética Ligação Competitiva Cristalização Seres Humanos Cinética Ligantes Modelos Moleculares Simulação de Dinâmica Molecular Estrutura Molecular Domínios Proteicos Estabilidade Proteica Receptores Opioides mu/genética Receptores Opioides mu/metabolismo Compostos de Espiro/metabolismo Tiofenos/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (((3-methoxythiophen-2-yl)methyl)((2-(9-(pyridin-2-yl)-6-oxaspiro(4.5)decan-9-yl)ethyl))amine); 0 (Amino Acids); 0 (Ligands); 0 (OPRM1 protein, human); 0 (Receptors, Opioid, mu); 0 (Spiro Compounds); 0 (Thiophenes) [Em] Mês de entrada: 1705 [Cu] Atualização por classe: 171229 [Lr] Data última revisão: 171229 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161026 [St] Status: MEDLINE

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[PMID]: 27777132 [Au] Autor: Tao PL [Ad] Endereço: Center for Neuropsychiatric Research, National Health Research Institutes, Miaoli, Taiwan, ROC. Electronic address: pltao@nhri.org.tw. [Ti] Título: Reply to: Agonism at delta-opioid receptor contributes to the antinociceptive effect of oxycodone in mice. [So] Source: Pharmacol Res;114:293, 2016 Dec. [Is] ISSN: 1096-1186 [Cp] País de publicação: Netherlands [La] Idioma: eng [Mh] Termos MeSH primário: Oxicodona Receptores Opioides delta [Mh] Termos MeSH secundário: Analgésicos Opioides Animais Camundongos Camundongos Endogâmicos ICR Morfina Antagonistas de Entorpecentes Medição da Dor/efeitos dos fármacos Receptores Opioides mu [Pt] Tipo de publicação: LETTER; COMMENT [Nm] Nome de substância: 0 (Analgesics, Opioid); 0 (Narcotic Antagonists); 0 (Receptors, Opioid, delta); 0 (Receptors, Opioid, mu); 76I7G6D29C (Morphine); CD35PMG570 (Oxycodone) [Em] Mês de entrada: 1711 [Cu] Atualização por classe: 171128 [Lr] Data última revisão: 171128 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161030 [St] Status: MEDLINE

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[PMID]: 29070014 [Au] Autor: Kong X; Deng H; Gong S; Alston T; Kong Y; Wang J [Ad] Endereço: Department of Neurosurgery, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences, No. 1 Shuaifuyuan Hutong, Dongcheng District, Beijing, 100730, People's Republic of China. [Ti] Título: Lack of associations of the opioid receptor mu 1 (OPRM1) A118G polymorphism (rs1799971) with alcohol dependence: review and meta-analysis of retrospective controlled studies. [So] Source: BMC Med Genet;18(1):120, 2017 Oct 26. [Is] ISSN: 1471-2350 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: BACKGROUND: Studies have sought associations of the opioid receptor mu 1 (OPRM1) A118G polymorphism (rs1799971) with alcohol-dependence, but findings are inconsistent. We summarize the information as to associations of rs1799971 (A > G) and the alcohol-dependence. METHODS: Systematically, we reviewed related literatures using the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) guideline. Embase, PubMed, Web of Knowledge, and Chinese National Knowledge Infrastructure (CNKI) databases were searched using select medical subject heading (MeSH) terms to identify all researches focusing on the present topic up to September 2016. Odds ratios (ORs) along with the 95% confidence interval (95% CI) were estimated in allele model, homozygote model, heterozygote model, dominant model and recessive model. Ethnicity-specific subgroup-analysis, sensitivity analysis, heterogeneity description, and publication-bias assessment were also analyzed. RESULTS: There were 17 studies, including 9613 patients in the present meta-analysis. The ORs in the 5 genetic-models were 1.037 (95% CI: 0.890, 1.210; p = 0.64), 1.074 (95% CI: 0.831, 1.387; p = 0.586), 1.155 (95% CI: 0.935, 1.427; p = 0.181), 1.261 (95% CI: 1.008, 1.578; p = 0.042), 0.968 (95% CI: 0.758, 1.236; p = 0.793), respectively. An association is significant in the dominant model, but there is no statistical significance upon ethnicity-specific subgroup analysis. CONCLUSION: The rs1799971 (A > G) is not strongly associated with alcohol-dependence. However, there are study heterogeneities and limited sample sizes. [Mh] Termos MeSH primário: Alcoolismo/genética Modelos Genéticos Polimorfismo de Nucleotídeo Único Receptores Opioides mu/genética [Mh] Termos MeSH secundário: Alcoolismo/fisiopatologia Alelos Estudos de Casos e Controles Expressão Gênica Frequência do Gene Heterozigoto Homozigoto Seres Humanos Razão de Chances Estudos Retrospectivos [Pt] Tipo de publicação: JOURNAL ARTICLE; META-ANALYSIS; REVIEW [Nm] Nome de substância: 0 (OPRM1 protein, human); 0 (Receptors, Opioid, mu) [Em] Mês de entrada: 1711 [Cu] Atualização por classe: 171102 [Lr] Data última revisão: 171102 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 171027 [St] Status: MEDLINE [do] DOI: 10.1186/s12881-017-0478-4

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[PMID]: 29053731 [Au] Autor: Ujcikova H; Hlouskova M; Cechova K; Stolarova K; Roubalova L; Svoboda P [Ad] Endereço: Department of Biomathematics, Institute of Physiology of the Czech Academy of Sciences, Prague, Czech Republic. [Ti] Título: Determination of µ-, δ- and κ-opioid receptors in forebrain cortex of rats exposed to morphine for 10 days: Comparison with animals after 20 days of morphine withdrawal. [So] Source: PLoS One;12(10):e0186797, 2017. [Is] ISSN: 1932-6203 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: BACKGROUND: Chronic exposure of mammalian organism to morphine results in adaption to persistent high opioid tone through homeostatic adjustments. Our previous results indicated that in the frontal brain cortex (FBC) of rats exposed to morphine for 10 days, such a compensatory adjustment was detected as large up-regulation of adenylylcyclases I (8-fold) and II (2.5-fold). The other isoforms of AC (III-IX) were unchanged. Importantly, the increase of ACI and ACII was reversible as it disappeared after 20 days of morphine withdrawal. Changes of down-stream signaling molecules such as G proteins and adenylylcyclases should respond to and be preceded by primary changes proceeding at receptor level. Therefore in our present work, we addressed the problem of reversibility of the long-term morphine effects on µ-, δ- and κ-OR protein levels in FBC. METHODS: Rats were exposed to increasing doses of morphine (10-40 mg/kg) for 10 days and sacrificed either 24 h (group +M10) or 20 days (group +M10/-M20) after the last dose of morphine in parallel with control animals (groups -M10 and -M10/-M20). Post-nuclear supernatant (PNS) fraction was prepared from forebrain cortex, resolved by 1D-SDS-PAGE under non-dissociated (-DTT) and dissociated (+DTT) conditions, and analyzed for the content of µ-, δ- and κ-OR by immunoblotting with C- and N-terminus oriented antibodies. RESULTS: Significant down-regulation of δ-OR form exhibiting Mw ≈ 60 kDa was detected in PNS prepared from both (+M10) and (+M10/-M20) rats. However, the total immunoblot signals of µ-, δ- and κ-OR, respectively, were unchanged. Plasma membrane marker Na, K-ATPase, actin and GAPDH were unaffected by morphine in both types of PNS. Membrane-domain marker caveolin-1 and cholesterol level increased in (+M10) rats and this increase was reversed back to control level in (+M10/-M20) rats. CONCLUSIONS: In FBC, prolonged exposure of rats to morphine results in minor (δ-OR) or no change (µ- and κ-OR) of opioid receptor content. The reversible increases of caveolin-1 and cholesterol levels suggest participation of membrane domains in compensatory responses during opioid withdrawal. GENERAL SIGNIFICANCE: Analysis of reversibility of morphine effect on mammalian brain. [Mh] Termos MeSH primário: Morfina/administração & dosagem Prosencéfalo/metabolismo Receptores Opioides delta/metabolismo Receptores Opioides kappa/metabolismo Receptores Opioides mu/metabolismo Síndrome de Abstinência a Substâncias [Mh] Termos MeSH secundário: Animais Western Blotting Eletroforese em Gel Bidimensional Eletroforese em Gel de Poliacrilamida Masculino Morfina/efeitos adversos Ratos Ratos Wistar [Pt] Tipo de publicação: COMPARATIVE STUDY; JOURNAL ARTICLE [Nm] Nome de substância: 0 (Receptors, Opioid, delta); 0 (Receptors, Opioid, kappa); 0 (Receptors, Opioid, mu); 76I7G6D29C (Morphine) [Em] Mês de entrada: 1711 [Cu] Atualização por classe: 171113 [Lr] Data última revisão: 171113 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 171021 [St] Status: MEDLINE [do] DOI: 10.1371/journal.pone.0186797

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[PMID]: 28990740 [Au] Autor: Drug Enforcement Administration, Department of Justice [Ti] Título: Schedules of Controlled Substances: Removal of Naldemedine From Control. Final rule. [So] Source: Fed Regist;82(188):45436-8, 2017 Sep 29. [Is] ISSN: 0097-6326 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: With the issuance of this final rule, the Drug Enforcement Administration removes the substance naldemedine (4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,7,9-trihydroxy-N-(2-(3-phenyl-1,2,4-oxadiazol-5-yl)propan-2-yl)-2,3,4,4a,5,7a-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamide) including its salts from the schedules of the Controlled Substances Act. Prior to the effective date of this rule, naldemedine was a schedule II controlled substance because it can be derived from opium alkaloids. This action removes the regulatory controls and administrative, civil, and criminal sanctions applicable to controlled substances, including those specific to schedule II controlled substances, on persons who handle (manufacture, distribute, reverse distribute, dispense, conduct research, import, export, or conduct chemical analysis) or propose to handle naldemedine. [Mh] Termos MeSH primário: Controle de Medicamentos e Entorpecentes/legislação & jurisprudência Antagonistas de Entorpecentes/classificação Receptores Opioides mu/antagonistas & inibidores Receptores Opioides mu/classificação [Mh] Termos MeSH secundário: Analgésicos Opioides/efeitos adversos Analgésicos Opioides/uso terapêutico Constipação Intestinal/induzido quimicamente Constipação Intestinal/tratamento farmacológico Seres Humanos Estados Unidos [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Analgesics, Opioid); 0 (Narcotic Antagonists); 0 (Receptors, Opioid, mu) [Em] Mês de entrada: 1710 [Cu] Atualização por classe: 171031 [Lr] Data última revisão: 171031 [Sb] Subgrupo de revista: T [Da] Data de entrada para processamento: 171011 [St] Status: MEDLINE

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[PMID]: 28834399 [Au] Autor: Laskowska AK; Puszko AK; Sosnowski P; Rózycki K; Kosson P; Matalinska J; Durlik M; Misicka A [Ad] Endereço: Department of Neuropeptides, Mossakowski Medical Research Centre, Polish Academy of Sciences, Pawinskiego 5, 02-106, Warsaw, Poland. [Ti] Título: Opioid Tripeptides Hybridized with trans-1-Cinnamylpiperazine as Proliferation Inhibitors of Pancreatic Cancer Cells in Two- and Three-Dimensional in vitro Models. [So] Source: ChemMedChem;12(19):1637-1644, 2017 Oct 09. [Is] ISSN: 1860-7187 [Cp] País de publicação: Germany [La] Idioma: eng [Ab] Resumo: According to the World Health Organization, the mortality rate among patients with pancreatic cancer will increase in the upcoming years. Gemcitabine is the first choice for treatment of pancreatic malignancy, but increasing resistance to this drug is decreasing its overall efficacy. Studies on new therapies that target metabolic pathways, growth factor inhibitors, and tumor stroma or tumor stem cells are currently underway in many research groups. Herein we report the bioactive properties (cytotoxicity and hemolytic activity) of synthetic peptidomimetics containing an opioid tripeptide fragment (Tyr-R -R -; where R is d-Ala or d-Thr, and R is Phe or Trp) hybridized with trans-1-cinnamylpiperazine. These compounds are stable in plasma up to 96 h and exhibit low hemotoxicity and good inhibitory effects on cancer cell growth in two- and three-dimensional in vitro models of pancreatic cancer. [Mh] Termos MeSH primário: Analgésicos Opioides/química Analgésicos Opioides/farmacologia Oligopeptídeos/química Oligopeptídeos/farmacologia Piperazinas/química [Mh] Termos MeSH secundário: Sequência de Aminoácidos Analgésicos Opioides/síntese química Analgésicos Opioides/metabolismo Técnicas de Cultura de Células Linhagem Celular Proliferação Celular/efeitos dos fármacos Sobrevivência Celular/efeitos dos fármacos Eritrócitos/citologia Eritrócitos/efeitos dos fármacos Eritrócitos/metabolismo Hemólise/efeitos dos fármacos Seres Humanos Isomerismo Modelos Biológicos Neoplasias Pancreáticas/metabolismo Neoplasias Pancreáticas/patologia Peptidomiméticos Ligação Proteica Receptores Opioides mu/genética Receptores Opioides mu/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Analgesics, Opioid); 0 (Oligopeptides); 0 (Peptidomimetics); 0 (Piperazines); 0 (Receptors, Opioid, mu); 1RTM4PAL0V (piperazine) [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: 170824 [St] Status: MEDLINE [do] DOI: 10.1002/cmdc.201700453

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