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[PMID]:28475363
[Au] Autor:Srivedavyasasri R; White MB; Kustova TS; Gemejiyeva NG; Cantrell CL; Ross SA
[Ad] Endereço:a National Center for Natural Product Research , University of Mississippi , University , MS , USA.
[Ti] Título:New tetranorlabdanoic acid from aerial parts of Salvia aethiopis.
[So] Source:Nat Prod Res;32(1):14-17, 2018 Jan.
[Is] ISSN:1478-6427
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Salvia aethiopis is a perennial plant native to Eurasia and known by the common names Mediterranean sage or African sage. This plant has been used in Iranian medicine as a carminative and tonic. The ethanolic extract of aerial part of S. aethiopis exhibited moderate to weak activity towards delta and kappa opioid receptors (46.3 and 45.3% displacement, respectively). Chromatographic purification of the ethanolic extract on silica gel column led to isolation of one new: 3α-hydroxy-8α-acetoxy-13,14,15,16-tetranorlabdan-12-oic acid (I) and three known compounds: sesquiterpene spathulenol (II), ß-sitosterol (III) and ß-sitosterol-3-O-glucoside (IV). The structures of all isolated compounds were elucidated by their NMR (1D and 2D) and MS spectral data. All the fractions and isolated compounds were tested for cannabinoid and opioid receptor binding assays.
[Mh] Termos MeSH primário: Componentes Aéreos da Planta/química
Receptores de Canabinoides/metabolismo
Salvia/química
[Mh] Termos MeSH secundário: Avaliação Pré-Clínica de Medicamentos/métodos
Irã (Geográfico)
Espectroscopia de Ressonância Magnética
Estrutura Molecular
Extratos Vegetais/química
Extratos Vegetais/farmacologia
Plantas Medicinais/química
Receptores Opioides delta/metabolismo
Receptores Opioides kappa/metabolismo
Sesquiterpenos/química
Sesquiterpenos/metabolismo
Sesquiterpenos/farmacologia
Sitosteroides/química
Sitosteroides/metabolismo
Sitosteroides/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Plant Extracts); 0 (Receptors, Cannabinoid); 0 (Receptors, Opioid, delta); 0 (Receptors, Opioid, kappa); 0 (Sesquiterpenes); 0 (Sitosterols); 5LI01C78DD (gamma-sitosterol); 7XV9L96SJJ (spathulenol); U45VN859W3 (lyoniside)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180301
[Lr] Data última revisão:
180301
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170506
[St] Status:MEDLINE
[do] DOI:10.1080/14786419.2017.1324961


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[PMID]:28462718
[Au] Autor:Perlikowska R; Janecka A
[Ad] Endereço:Department of Biomolecular Chemistry, Faculty of Medicine, Medical University of Lodz, 92-215 Lodz. Poland.
[Ti] Título:Rubiscolins - Highly Potent Peptides Derived from Plant Proteins.
[So] Source:Mini Rev Med Chem;18(2):104-112, 2018.
[Is] ISSN:1875-5607
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Rubiscolins are two naturally occurring, linear peptides, isolated from the pepsin digests of D-ribulose-1,5-bisphosphate carboxylase/oxygenase (RuBisCo) from spinach leaves. Their sequences are as follows: Tyr-Pro-Leu-Asp-Leu (YPLDL, rubiscolin-5) and Tyr-Pro-Leu-Asp-Leu-Phe (YPLDLF, rubiscolin-6, also known as rubixyl). Though their structure does not resemble typical opioid peptides, rubiscolins were found to exhibit high affinity and selectivity for the delta opioid receptor and an antinociceptive effect in mice after oral administration. Moreover, orally administered rubiscolin-6 was shown to possess orexigenic, anxiolytic-like, and memory-enhancing activities in mice. This review summarizes various biological activities of rubiscolins in mammalian organism and recent developments on the structure-activity relationship of rubiscolin analogs, aimed at improving their pharmacological properties. Naturally occurring substances, such as rubiscolins, may provide a rational and powerful approach in the design of new therapeutics or functional foods.
[Mh] Termos MeSH primário: Analgésicos/farmacologia
Produtos Biológicos/farmacologia
Dor/tratamento farmacológico
Peptídeos/farmacologia
Proteínas de Plantas/química
Spinacia oleracea/química
[Mh] Termos MeSH secundário: Analgésicos/administração & dosagem
Analgésicos/química
Animais
Produtos Biológicos/administração & dosagem
Produtos Biológicos/química
Seres Humanos
Peptídeos/administração & dosagem
Peptídeos/química
Receptores Opioides delta/antagonistas & inibidores
Receptores Opioides delta/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Analgesics); 0 (Biological Products); 0 (Peptides); 0 (Plant Proteins); 0 (Receptors, Opioid, delta)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180208
[Lr] Data última revisão:
180208
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170503
[St] Status:MEDLINE
[do] DOI:10.2174/1389557517666170426160703


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[PMID]:29191644
[Au] Autor:Yadlapalli JSK; Dogra N; Walbaum AW; Prather PL; Crooks PA; Dobretsov M
[Ad] Endereço:Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock 72205, USA.
[Ti] Título:Preclinical assessment of utility of M6S for multimodal acute and chronic pain treatment in diabetic neuropathy.
[So] Source:Life Sci;192:151-159, 2018 Jan 01.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:AIMS: Previous reports from our laboratory have established that morphine-6-O-sulfate (M6S) is a mixed µ/δ opioid receptor (OR) agonist and a potential improved alternative to morphine for treatment of chronic multimodal pain in non-diabetic rats. This study extends the antinociceptive effects of M6S and morphine in STZ-induced diabetic rats. MATERIALS AND METHODS: Effects of morphine and M6S were studied across a range of pain modalities, using hot plate threshold (HPT), pinprick sensitivity threshold (PST) and paw pressure threshold (PPT) tests. KEY FINDINGS: Acutely, M6S was 3- to 5-fold more potent and 2- to 3-fold more efficacious than morphine in HPT and PST tests. No differences in analgesic drug potency/efficacy were detected in the PPT test. After 7-9days of chronic treatment, tolerance developed to the antinociceptive effects of morphine, but not to M6S, in all three pain tests. Furthermore, morphine-tolerant rats were not cross-tolerant to M6S. The selective δ-OR antagonist, naltrindole, blocked M6S-induced antinociception by 62±3% in the HPT test, 93±5% in the PST test, and 30±17% in the PPT test when examined acutely. SIGNIFICANCE: These studies provide additional confirmation for the mixed µ/δ activity of M6S and demonstrate potential improved clinical utility for dual µ/δ agonists relative to morphine in treatment of diabetic neuropathy across multiple pain domains.
[Mh] Termos MeSH primário: Analgésicos Opioides/uso terapêutico
Dor Crônica/tratamento farmacológico
Nefropatias Diabéticas/tratamento farmacológico
Derivados da Morfina/uso terapêutico
Dor/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Dor Crônica/etiologia
Diabetes Mellitus Experimental/complicações
Nefropatias Diabéticas/complicações
Masculino
Morfina/uso terapêutico
Dor/etiologia
Manejo da Dor
Medição da Dor/efeitos dos fármacos
Limiar da Dor/efeitos dos fármacos
Ratos
Ratos Sprague-Dawley
Receptores Opioides delta/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Analgesics, Opioid); 0 (Morphine Derivatives); 0 (Receptors, Opioid, delta); 0 (morphine-6-O-sulfate); 76I7G6D29C (Morphine)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180108
[Lr] Data última revisão:
180108
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171202
[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


  5 / 4337 MEDLINE  
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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]:28877966
[Au] Autor:Rosen SF; Ham B; Drouin S; Boachie N; Chabot-Dore AJ; Austin JS; Diatchenko L; Mogil JS
[Ad] Endereço:Department of Psychology and Alan Edwards Centre for Research on Pain, McGill University, Montreal, Quebec H3A 1B1, Canada, and.
[Ti] Título:T-Cell Mediation of Pregnancy Analgesia Affecting Chronic Pain in Mice.
[So] Source:J Neurosci;37(41):9819-9827, 2017 Oct 11.
[Is] ISSN:1529-2401
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:It has been reported consistently that many female chronic pain sufferers have an attenuation of symptoms during pregnancy. Rats display increased pain tolerance during pregnancy due to an increase in opioid receptors in the spinal cord. Past studies did not consider the role of non-neuronal cells, which are now known to play an important role in chronic pain processing. Using an inflammatory (complete Freund's adjuvant) or neuropathic (spared nerve injury) model of persistent pain, we observed that young adult female mice in early pregnancy switch from a microglia-independent to a microglia-dependent pain hypersensitivity mechanism. During late pregnancy, female mice show no evidence of chronic pain whatsoever. This pregnancy-related analgesia is reversible by intrathecal administration of naloxone, suggesting an opioid-mediated mechanism; pharmacological and genetic data suggest the importance of δ-opioid receptors. We also observe that T-cell-deficient ( and -null mutant) pregnant mice do not exhibit pregnancy analgesia, which can be rescued with the adoptive transfer of CD4 or CD8 T cells from late-pregnant wild-type mice. These results suggest that T cells are a mediator of the opioid analgesia exhibited during pregnancy. Chronic pain symptoms often subside during pregnancy. This pregnancy-related analgesia has been demonstrated for acute pain in rats. Here, we show that pregnancy analgesia can produce a complete cessation of chronic pain behaviors in mice. We show that the phenomenon is dependent on pregnancy hormones (estrogen and progesterone), δ-opioid receptors, and T cells of the adaptive immune system. These findings add to the recent but growing evidence of sex-specific T-cell involvement in chronic pain processing.
[Mh] Termos MeSH primário: Analgesia
Dor Crônica/fisiopatologia
Prenhez/fisiologia
Linfócitos T
[Mh] Termos MeSH secundário: Transferência Adotiva
Animais
Dor Crônica/induzido quimicamente
Feminino
Hiperalgesia/fisiopatologia
Camundongos
Camundongos Endogâmicos ICR
Camundongos Nus
Microglia/imunologia
Naloxona/farmacologia
Antagonistas de Entorpecentes/farmacologia
Neuralgia/fisiopatologia
Ovariectomia
Gravidez
Receptores Opioides delta/efeitos dos fármacos
Linfócitos T/imunologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Narcotic Antagonists); 0 (Receptors, Opioid, delta); 36B82AMQ7N (Naloxone)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171023
[Lr] Data última revisão:
171023
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170908
[St] Status:MEDLINE
[do] DOI:10.1523/JNEUROSCI.2053-17.2017


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[PMID]:28823730
[Au] Autor:Leroy F; Brann DH; Meira T; Siegelbaum SA
[Ad] Endereço:Department of Neuroscience, Kavli Institute of Brain Science, Columbia University Medical Center, 1051 Riverside Drive, New York, NY, USA. Electronic address: felxfel@aol.com.
[Ti] Título:Input-Timing-Dependent Plasticity in the Hippocampal CA2 Region and Its Potential Role in Social Memory.
[So] Source:Neuron;95(5):1089-1102.e5, 2017 Aug 30.
[Is] ISSN:1097-4199
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Input-timing-dependent plasticity (ITDP) is a circuit-based synaptic learning rule by which paired activation of entorhinal cortical (EC) and Schaffer collateral (SC) inputs to hippocampal CA1 pyramidal neurons (PNs) produces a long-term enhancement of SC excitation. We now find that paired stimulation of EC and SC inputs also induces ITDP of SC excitation of CA2 PNs. However, whereas CA1 ITDP results from long-term depression of feedforward inhibition (iLTD) as a result of activation of CB1 endocannabinoid receptors on cholecystokinin-expressing interneurons, CA2 ITDP results from iLTD through activation of δ-opioid receptors on parvalbumin-expressing interneurons. Furthermore, whereas CA1 ITDP has been previously linked to enhanced specificity of contextual memory, we find that CA2 ITDP is associated with enhanced social memory. Thus, ITDP may provide a general synaptic learning rule for distinct forms of hippocampal-dependent memory mediated by distinct hippocampal regions.
[Mh] Termos MeSH primário: Região CA2 Hipocampal/fisiologia
Memória/fisiologia
Plasticidade Neuronal/fisiologia
[Mh] Termos MeSH secundário: Animais
Região CA2 Hipocampal/citologia
Córtex Entorrinal/fisiologia
Interneurônios/metabolismo
Depressão Sináptica de Longo Prazo/fisiologia
Masculino
Camundongos
Camundongos Transgênicos
Inibição Neural/fisiologia
Parvalbuminas/metabolismo
Células Piramidais/fisiologia
Receptores Opioides delta/metabolismo
Comportamento Social
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Parvalbumins); 0 (Receptors, Opioid, delta)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170929
[Lr] Data última revisão:
170929
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170822
[St] Status:MEDLINE


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[PMID]:28778917
[Au] Autor:Trujillo AN; Katnik C; Cuevas J; Cha BJ; Taylor-Clark TE; Breslin JW
[Ad] Endereço:Department of Molecular Pharmacology and Physiology, Morsani College of Medicine, University of South Florida, Tampa, Florida.
[Ti] Título:Modulation of mesenteric collecting lymphatic contractions by σ -receptor activation and nitric oxide production.
[So] Source:Am J Physiol Heart Circ Physiol;313(4):H839-H853, 2017 Oct 01.
[Is] ISSN:1522-1539
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Recently, it has been reported that a σ-receptor antagonist could reduce inflammation-induced edema. Lymphatic vessels play an essential role in removing excess interstitial fluid. We tested the hypothesis that activation of σ-receptors would reduce or weaken collecting lymphatic contractions. We used isolated, cannulated rat mesenteric collecting lymphatic vessels to study contractions in response to the σ-receptor agonist afobazole in the absence and presence of different σ-receptor antagonists. We used RT-PCR and Western blot analysis to investigate whether these vessels express the σ -receptor and immunofluorescence confocal microscopy to examine localization of the σ -receptor in the collecting lymphatic wall. Using -nitro-l-arginine methyl ester (l-NAME) pretreatment before afobazole in isolated lymphatics, we tested the role of nitric oxide (NO) signaling. Finally, we used 4-amino-5-methylamino-2',7'-difluorofluorescein diacetate fluorescence as an indicator to test whether afobazole increases NO release in cultured lymphatic endothelial cells. Our results show that afobazole (50-150 µM) elevated end-systolic diameter and generally reduced pump efficiency and that this response could be partially blocked by the σ -receptor antagonists BD 1047 and BD 1063 but not by the σ -receptor antagonist SM-21. σ -Receptor mRNA and protein were detected in lysates from isolated rat mesenteric collecting lymphatics. Confocal images with anti-σ -receptor antibody labeling suggested localization in the lymphatic endothelium. Blockade of NO synthases with l-NAME inhibited the effects of afobazole. Finally, afobazole elicited increases in NO production from cultured lymphatic endothelial cells. Our findings suggest that the σ -receptor limits collecting lymphatic pumping through a NO-dependent mechanism. Relatively little is known about the mechanisms that govern contractions of lymphatic vessels. σ -Receptor activation has been shown to reduce the fractional pump flow of isolated rat mesenteric collecting lymphatics. The σ -receptor was localized mainly in the endothelium, and blockade of nitric oxide synthase inhibited the effects of afobazole.
[Mh] Termos MeSH primário: Vasos Linfáticos/efeitos dos fármacos
Vasos Linfáticos/metabolismo
Mesentério/efeitos dos fármacos
Mesentério/metabolismo
Óxido Nítrico/biossíntese
Receptores Opioides delta/agonistas
[Mh] Termos MeSH secundário: Animais
Benzimidazóis/farmacologia
Células Cultivadas
Células Endoteliais/efeitos dos fármacos
Células Endoteliais/metabolismo
Inibidores Enzimáticos/farmacologia
Masculino
Morfolinas/farmacologia
Contração Muscular/efeitos dos fármacos
Músculo Liso Vascular/efeitos dos fármacos
NG-Nitroarginina Metil Éster/farmacologia
Ratos
Ratos Sprague-Dawley
Receptores Opioides delta/antagonistas & inibidores
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2-((2-morpholino)ethylthio)-5-ethoxybenzimidazole); 0 (Benzimidazoles); 0 (DOR1 protein, rat); 0 (Enzyme Inhibitors); 0 (Morpholines); 0 (Receptors, Opioid, delta); 31C4KY9ESH (Nitric Oxide); V55S2QJN2X (NG-Nitroarginine Methyl Ester)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171108
[Lr] Data última revisão:
171108
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170806
[St] Status:MEDLINE
[do] DOI:10.1152/ajpheart.00702.2016


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[PMID]:28734666
[Au] Autor:Pasquinucci L; Turnaturi R; Prezzavento O; Arena E; Aricò G; Georgoussi Z; Parenti R; Cantarella G; Parenti C
[Ad] Endereço:Department of Drug Sciences, Medicinal Chemistry Section, University of Catania, Viale A. Doria 6, 95125 Catania, Italy.
[Ti] Título:Development of novel LP1-based analogues with enhanced delta opioid receptor profile.
[So] Source:Bioorg Med Chem;25(17):4745-4752, 2017 Sep 01.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Pain relief achieved by co-administration of drugs acting at different targets is more effective than that obtained with conventional MOR selective agonists usually associated to relevant side effects. It has been demonstrated that simultaneously targeting different opioid receptors is a more effective therapeutic strategy. Giving the promising role for DOR in pain management, novel LP1-based analogues with different N-substituents were designed and synthesized with the aim to improve DOR profile. For this purpose, we maintained the phenyl ring in the N-substituent of 6,7-benzomorphan scaffold linked to an ethyl spacer bearing a hydroxyl/methyl or methoxyl group at carbon 2 or including it in a 1,4-benzodioxane ring. LP1 analogues were tested by competition binding assays. Compounds 6 (K =2.47nM, K =9.6nM), 7 (K =0.5nM and K =0.8nM) and 9 (K =1.08nM, K =6.6nM) retained MOR affinity but displayed an improved DOR binding capacity as compared to LP1 (K =0.83nM, K =29.1nM). Moreover, GPI and MVD functional assays indicated that compounds 6 (IC =49.2 and IC =10.8nM), 7 (IC =9.9 and IC =11.8nM) and 9 (IC =21.5 and IC =4.4nM) showed a MOR/DOR agonist profile, unlike LP1 that was a MOR agonist/DOR antagonist (IC =1.9 and IC =1240nM). Measurements of their antinociceptive effect was evaluated by mice radiant tail flick test displaying for compounds 6, 7 and 9 ED values of 1.3, 1.0 and 0.9mg/kg, i.p., respectively. Moreover, the antinociceptive effect of compound 9 was longer lasting with respect to LP1. In conclusion the N-substituent nature of compounds 6, 7 and 9 shifts the DOR profile of LP1 from antagonism to agonism.
[Mh] Termos MeSH primário: Analgésicos/química
Benzomorfanos/química
Receptores Opioides delta/metabolismo
[Mh] Termos MeSH secundário: Analgésicos/metabolismo
Analgésicos/uso terapêutico
Animais
Ligação Competitiva
Concentração Inibidora 50
Cinética
Masculino
Camundongos
Dor/tratamento farmacológico
Ligação Proteica
Receptores Opioides delta/química
Receptores Opioides kappa/química
Receptores Opioides kappa/metabolismo
Receptores Opioides mu/química
Receptores Opioides mu/metabolismo
Relação Estrutura-Atividade
Trítio/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (3-((2R,6R,11R)-8-hydroxy-6,11-dimethyl-1,4,5,6-tetrahydro-2,6-methano-3-benzazocin-3(2H)-yl)-N-phenylpropanamide); 0 (Analgesics); 0 (Benzomorphans); 0 (Receptors, Opioid, delta); 0 (Receptors, Opioid, kappa); 0 (Receptors, Opioid, mu); 10028-17-8 (Tritium)
[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:170724
[St] Status:MEDLINE


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[PMID]:28700700
[Au] Autor:McDonnell C; Leánez S; Pol O
[Ad] Endereço:Grup de Neurofarmacologia Molecular, Institut d'Investigació Biomèdica Sant Pau, Barcelona, Spain.
[Ti] Título:The induction of the transcription factor Nrf2 enhances the antinociceptive effects of delta-opioid receptors in diabetic mice.
[So] Source:PLoS One;12(7):e0180998, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The involvement of heme oxygenase 1 (HO-1) in the modulation of the antinociceptive effects of opioids in type 1 diabetes has been demonstrated but the role played by the transcription factor Nrf2 in the regulation of painful neuropathy and in the effects and expression of δ-opioid receptors (DOR) in type 2 diabetes, has not been studied. In male BKS.Cg-m+/+Leprdb/J (db/db) mice, the anti-allodynic effects produced by a Nrf2 transcription factor activator, sulforaphane (SFN) administered alone and combined with two DOR agonists, [d-Pen(2),d-Pen(5)]-Enkephalin (DPDPE) and (+)-4-[(αR)-α-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N diethylbenzamide (SNC-80), were evaluated. The effects of SFN on glucose levels and body weight as well as on the proteins levels of Nrf2, HO-1, NAD(P)H: quinone oxidoreductase 1 (NQO1), MAPKs (JNK) and DOR in sciatic nerve from db/db mice were also assessed. This study showed that the administration of SFN dose dependently reversed mechanical allodynia, reduced hyperglycemia and body weight gain associated to type 2 diabetes and significantly increased the anti-allodynic effects of DPDPE and SNC-80 in db/db mice. This treatment normalized the down regulation of Nrf2 and NQO1 and enhanced the protein levels of HO-1 in db/db mice. Moreover, the administration of SFN also inhibited the JNK phosphorylation and DOR down-regulation in the sciatic nerve of diabetic mice. Our data indicated that SFN treatment is effective in reversing mechanical allodynia and enhancing DOR antinociceptive effects in db/db mice which effects might be mediated by activating Nrf2 signaling, reducing hyperglycemia, inhibiting JNK phosphorylation and avoiding DOR down-regulation in the sciatic nerve of these animals. These results propose SFN, alone and/or combined with DOR agonists, as interesting approaches for the treatment of painful diabetic neuropathy associated to type 2 diabetes in mice.
[Mh] Termos MeSH primário: Diabetes Mellitus Experimental/metabolismo
Fator 2 Relacionado a NF-E2/metabolismo
Receptores Opioides delta/metabolismo
[Mh] Termos MeSH secundário: Animais
Benzamidas/farmacologia
Glicemia/efeitos dos fármacos
Glicemia/metabolismo
Western Blotting
Peso Corporal/efeitos dos fármacos
Peso Corporal/genética
Peso Corporal/fisiologia
Diabetes Mellitus Experimental/genética
Diabetes Mellitus Tipo 2/genética
Diabetes Mellitus Tipo 2/metabolismo
Neuropatias Diabéticas/metabolismo
D-Penicilina (2,5)-Encefalina/farmacologia
Hiperalgesia/metabolismo
Isotiocianatos/farmacologia
Masculino
Camundongos
Fator 2 Relacionado a NF-E2/genética
Piperazinas/farmacologia
Receptores Opioides delta/agonistas
Receptores Opioides delta/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzamides); 0 (Blood Glucose); 0 (Isothiocyanates); 0 (NF-E2-Related Factor 2); 0 (Nfe2l2 protein, mouse); 0 (Piperazines); 0 (Receptors, Opioid, delta); 156727-74-1 (4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-N,N-diethylbenzamide); 88373-73-3 (Enkephalin, D-Penicillamine (2,5)-); GA49J4310U (sulforafan)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170927
[Lr] Data última revisão:
170927
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170713
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0180998



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