Search results for "Harm"

showing 10 items of 13866 documents

Singular Location and Signaling Profile of Adenosine A2A-Cannabinoid CB1 Receptor Heteromers in the Dorsal Striatum

2018

The dorsal striatum is a key node for many neurobiological processes such as motor activity, cognitive functions, and affective processes. The proper functioning of striatal neurons relies critically on metabotropic receptors. Specifically, the main adenosine and endocannabinoid receptors present in the striatum, ie, adenosine A(2A) receptor (A(2A)R) and cannabinoid CB1 receptor (CB1R), are of pivotal importance in the control of neuronal excitability. Facilitatory and inhibitory functional interactions between striatal A(2A)R and CB1R have been reported, and evidence supports that this cross-talk may rely, at least in part, on the formation of A(2A)R-CB1R heteromeric complexes. However, th…

0301 basic medicineCannabinoid receptorAdenosineReceptor Adenosine A2Amedicine.medical_treatmentAdenosinaAdenosine A2A receptormediated inhibitionStriatumBiologyhuntingtons-disease micecannabinoid CB1Mice03 medical and health sciencesglutamatergic neurotransmission0302 clinical medicineReceptor Cannabinoid CB1NeurobiologyNeural PathwaysBasal gangliamedicineAnimalsHumansendocannabinoid systemGenetically modified animalProtein Structure QuaternaryA(2A) receptorsPharmacologyEndocannabinoid systemCorpus Striatumprotein-coupled receptorsProtein SubunitsPsychiatry and Mental healthtransgenic mouse modelHuntington Disease030104 developmental biologyMetabotropic receptornervous systembasal gangliaCannabinoidallosteric interactionsNeuroscience030217 neurology & neurosurgeryNeurobiologiaSignal Transduction
researchProduct

Quantification of the Cannabinoid Type 1 Receptor Availability in the Mouse Brain

2020

Introduction: The endocannabinoid system is involved in several diseases such as addictive disorders, schizophrenia, post-traumatic stress disorder, and eating disorders. As often mice are used as the preferred animal model in translational research, in particular when using genetically modified mice, this study aimed to provide a systematic analysis of in vivo cannabinoid type 1 (CB1) receptor ligand-binding capacity using positron emission tomography (PET) using the ligand [18F]MK-9470. We then compared the PET results with literature data from immunohistochemistry (IHC) to review the consistency between ex vivo protein expression and in vivo ligand binding.Methods: Six male C57BL/6J (6–9…

0301 basic medicineCannabinoid receptormedicine.medical_treatmentNeuroscience (miscellaneous)PharmacologyBiologylcsh:RC321-571lcsh:QM1-69503 medical and health sciencesCellular and Molecular Neuroscience0302 clinical medicineIn vivoRadioligandmedicine[18F]MK-9470 ; cannabinoid type 1 receptor ; immunohistochemistry ; microPET ; mouseReceptorlcsh:Neurosciences. Biological psychiatry. NeuropsychiatrymouseOriginal ResearchCerebrumlcsh:Human anatomyLigand (biochemistry)microPETEndocannabinoid system[18F]MK-9470030104 developmental biologymedicine.anatomical_structurenervous systemcannabinoid type 1 receptorimmunohistochemistryCannabinoidAnatomy030217 neurology & neurosurgeryNeuroscienceFrontiers in Neuroanatomy
researchProduct

Determination of meropenem in endotracheal tubes by in-tube solid phase microextraction coupled to capillary liquid chromatography with diode array d…

2017

Meropenem is a widely used antimicrobial for the treatment of infections associated with the use of invasive medical devices in intensive care unit patients. These treatments are not always effective, in fact, in-vitro studies have demonstrated the difficulty of antimicrobials to penetrate into the biofilm, however in-vivo studies of the effect of these compounds is a trend, mostly because of the complexity of pulmonary samples extracted from ETTs. Therefore, the objective of this study was to evaluate in-tube solid phase microextraction (in-tube SPME) coupled to capillary liquid chromatography (CapLC) with DAD to determine meropenem in Errs in order to estimate the penetration capability i…

0301 basic medicineCapillary action030106 microbiologyClinical BiochemistryPharmaceutical ScienceEndotracheal tubesengineering.materialSolid-phase microextraction01 natural sciencesMeropenemAnalytical Chemistry03 medical and health sciencesCapillary columnCoatingCapillary ElectrochromatographyLimit of DetectionCapillary-LC-DADDrug DiscoverymedicineIntubation IntratrachealHumansSpectroscopySolid Phase MicroextractionChromatographyChemistryBiofilm010401 analytical chemistryIn-tube SPMEPenetration (firestop)MeropenemDiode array0104 chemical sciencesAnti-Bacterial AgentsCapillary lengthengineeringThienamycinsmedicine.drugChromatography LiquidJournal of pharmaceutical and biomedical analysis
researchProduct

Ceftazidime-Avibactam Combination Therapy Compared to Ceftazidime-Avibactam Monotherapy for the Treatment of Severe Infections Due to Carbapenem-Resi…

2020

Ceftazidime-avibactam (CZA) is a novel beta-lactam beta-lactamase inhibitor combination approved for the treatment of complicated urinary tract infections, complicated intra-abdominal infections, and for hospital-acquired/ventilator-associated pneumonia. The aim of this systematic review (PROSPERO registration number: CRD42019128927) was to evaluate the effectiveness of CZA combination therapy versus CZA monotherapy in the treatment of severe infections. The databases included in the search, until February 12th, 2020, were MEDLINE by PubMed, EMBASE, and The Cochrane Central Register of Controlled Trials. We included both randomized controlled trials (RCTs) and non-randomized studies publish…

0301 basic medicineCarbapenem-resistant enterobacteriaceaeBiochemistrylaw.inventionsepsisCeftazidime‐avibactam0302 clinical medicineRandomized controlled trialsystematic reviewlawPharmacology (medical)030212 general & internal medicineGeneral Pharmacology Toxicology and Pharmaceuticsnetwork meta-analysisceftazidime-avibactamAnti‐infective agentnetwork meta-analysiInfectious Diseasescarbapenem-resistant EnterobacteriaceaeMeta-analysisβ-lactamase inhibitors.sepsimedicine.drugMicrobiology (medical)medicine.medical_specialtyCombination therapyβ-lactamase inhibitors030106 microbiologyMEDLINEβ‐lactamase inhibitorsMicrobiologyArticle03 medical and health sciencesCarbapenem‐resistant Enterobacteriaceaemultidrug resistanceInternal medicinemedicineanti-infective agentbacteremiabusiness.industrylcsh:RM1-950Retrospective cohort studyCeftazidime/avibactammedicine.diseaseinfectionlcsh:Therapeutics. PharmacologyBacteremiaanti-infective agentsbusinessNetwork meta‐analysi
researchProduct

Guanxin Danshen Formulation Protects against Myocardial Ischemia Reperfusion Injury-Induced Left Ventricular Remodeling by Upregulating Estrogen Rece…

2017

Background: Guanxin Danshen formulation (GXDSF) is a traditional Chinese herbal recipe recorded in the Chinese Pharmacopoeia since 1995 edition, which consists of Salviae miltiorrhizae Radix et Rhizoma, Notoginseng Radix et Rhizoma and Dalbergiae odoriferae Lignum. Our previous research suggested GXDSF had positive effect on cardiovascular disease. Therefore, the aim of this study was to elucidate the effects of GXDSF on myocardial ischemia reperfusion injury-induced left ventricular remodelling (MIRI-LVR). Methods: The effects of GXDSF on cardiac function were detected by haemodynamics and echocardiograms. The effects of GXDSF on biochemical parameters (AST, LDH and CK-MB) were analysed. H…

0301 basic medicineCardiac function curvemedicine.medical_specialtyGuanxin Danshen formulaEstrogen receptor030204 cardiovascular system & hematologyPharmacologyventricular remodeling03 medical and health sciences0302 clinical medicineFibrosisInternal medicinemedicinenetwork pharmacologyPharmacology (medical)Ventricular remodelingOriginal ResearchPharmacologyPI3K/AktEjection fractionbusiness.industryestrogen receptor βlcsh:RM1-950PHTPPmedicine.diseasemyocardial ischemia reperfusion injury030104 developmental biologylcsh:Therapeutics. PharmacologyCardiologyMyocardial fibrosisbusinessReperfusion injuryFrontiers in Pharmacology
researchProduct

Homozygous Resistance to Thyroid Hormone β: Can Combined Antithyroid Drug and Triiodothyroacetic Acid Treatment Prevent Cardiac Failure?

2017

Resistance to thyroid hormone β (RTHβ) due to homozygous THRB defects is exceptionally rare, with only five kindreds reported worldwide. Cardiac dysfunction, which can be life-threatening, is recognized in the disorder. Here we describe the clinical, metabolic, ophthalmic, and cardiac findings in a 9-year-old boy harboring a biallelic THRB mutation (R243Q), along with biochemical, physiologic, and cardiac responses to carbimazole and triiodothyroacetic acid (TRIAC) therapy. The patient exhibits recognized features (goiter, nonsuppressed thyroid-stimulating hormone levels, upper respiratory tract infections, hyperactivity, low body mass index) of heterozygous RTHβ, with additional characteri…

0301 basic medicineCardiac function curvemedicine.medical_specialtyendocrine systemGoiterendocrine system diseasesEndocrinology Diabetes and Metabolism030209 endocrinology & metabolismCase ReportsCardiovascularthyroidresistance to thyroid hormonehomozygous THRB mutation03 medical and health sciences0302 clinical medicineClinical ResearchInternal medicinemedicine2.1 Biological and endogenous factorsDecompensation2. Zero hungercardiac thyrotoxicosisbusiness.industryThyroidDilated cardiomyopathymedicine.disease3. Good health030104 developmental biologyEndocrinologymedicine.anatomical_structureCarbimazoleHeart Disease6.1 PharmaceuticalsBasal metabolic ratebusinessHormonemedicine.drug
researchProduct

Gene therapy for chondral and osteochondral regeneration: is the future now?

2017

Gene therapy might represent a promising strategy for chondral and osteochondral defects repair by balancing the management of temporary joint mechanical incompetence with altered metabolic and inflammatory homeostasis. This review analysed preclinical and clinical studies on gene therapy for the repair of articular cartilage defects performed over the last 10 years, focussing on expression vectors (non-viral and viral), type of genes delivered and gene therapy procedures (direct or indirect). Plasmids (non-viral expression vectors) and adenovirus (viral vectors) were the most employed vectors in preclinical studies. Genes delivered encoded mainly for growth factors, followed by transcripti…

0301 basic medicineCartilage ArticularExpression vectorPathologymedicine.medical_specialtyCell signalingCartilage repair; Expression vectors; Gene therapy procedures; Osteoarthritis; Regenerative medicine; Molecular Medicine; Molecular Biology; Pharmacology; Cellular and Molecular Neuroscience; Cell BiologyBone RegenerationInflammatory arthritisGenetic enhancementGene therapy procedureOsteoarthritisViral vector03 medical and health sciencesCellular and Molecular NeuroscienceCartilage repairChondrocytesInterferonSettore BIO/13 - Biologia ApplicataOsteoarthritismedicineAnimalsHumansRegenerationMolecular BiologyPharmacologyExpression vectorbusiness.industryRegeneration (biology)Cell BiologyGenetic Therapymedicine.disease030104 developmental biologyRegenerative medicineCancer researchMolecular MedicineOsteoarthritibusinessmedicine.drugCellular and molecular life sciences : CMLS
researchProduct

Chondroprotective effects of the combination chondroitin sulfate-glucosamine in a model of osteoarthritis induced by anterior cruciate ligament trans…

2016

[EN] Context: The efficacy of the combination chondroitin sulfate-glucosamine (CS-GlcN) in the treatment of knee osteoarthritis (OA) has been suggested in recent clinical studies. In vitro reports have also suggested anti-inflammatory and anti-resorptive effects of this combination. Objective: The aim of this study was to characterize the effects of CS-GlcN on joint degradation in vivo including the assessment of inflammation and bone metabolism in a model of OA. Materials and methods: We have used the OA model induced by anterior cruciate ligament transection (ACLT) in ovariectomised rats. CS-GlcN was administered daily (oral gavage) from week 0 until week 12 after ovariectomy at the dose …

0301 basic medicineCartilage Articularmedicine.medical_specialtyAnterior cruciate ligamentOvariectomyType II collagenOsteoarthritisProtective AgentsBone and BonesBone remodeling03 medical and health scienceschemistry.chemical_compound0302 clinical medicineOsteoprotegerinGlucosamineInternal medicineOsteoarthritisMedicineAnimalsChondroitin sulfateAnterior cruciate ligament transectionAnterior Cruciate LigamentRats Wistar030203 arthritis & rheumatologyPharmacologyGlucosaminebusiness.industryCartilageAnterior Cruciate Ligament InjuriesChondroitin SulfatesGeneral MedicineX-Ray MicrotomographyOsteoarthritis Kneemedicine.diseaseChondroitin sulfate-glucosamine Ovariectomised ratscarbohydrates (lipids)Disease Models Animal030104 developmental biologymedicine.anatomical_structureEndocrinologychemistryDrug Therapy CombinationFemaleJointsInflammation MediatorsbusinessBiomarkersModel
researchProduct

Inhibitory Effect of Kurarinone on Growth of Human Non-small Cell Lung Cancer: An Experimental Study Both in Vitro and in Vivo Studies

2018

Kurarinone, a flavonoid isolated from Sophora flavescens Aiton, has been reported to have significant antitumor activity. However, the cytotoxic activity of kurarinone against non-small cell lung cancer (NSCLC) cells is still under explored. In our study, we have evaluated the inhibitory effects of kurarinone on the growth of NSCLC both in vivo and in vitro as well as the molecular mechanisms underlying kurarinone-induced A549 cell apoptosis. The results showed that kurarinone effectively inhibited the proliferation of A549 cells with little toxic effects on human bronchial epithelial cell line BEAS-2B. FASC examination and Hoechst 33258 staining assay showed that kurarinone dose-dependentl…

0301 basic medicineCaspase 303 medical and health sciences0302 clinical medicineIn vivoCytotoxic T cellPharmacology (medical)Protein kinase BPharmacologyA549 cellCaspase-9biologyChemistrymulti-targetlcsh:RM1-950apoptosiskurarinoneIn vitrorespiratory tract diseases030104 developmental biologyanticancer activitylcsh:Therapeutics. PharmacologyApoptosis030220 oncology & carcinogenesisCancer researchbiology.proteinlung carcinomaFrontiers in Pharmacology
researchProduct

Development of Novel Peptide-Based Michael Acceptors Targeting Rhodesain and Falcipain-2 for the Treatment of Neglected Tropical Diseases (NTDs)

2017

This paper describes the development of a class of peptide-based inhibitors as novel antitrypanosomal and antimalarial agents. The inhibitors are based on a characteristic peptide sequence for the inhibition of the cysteine proteases rhodesain of Trypanosoma brucei rhodesiense and falcipain-2 of Plasmodium falciparum. We exploited the reactivity of novel unsaturated electrophilic functions such as vinyl-sulfones, -ketones, -esters, and -nitriles. The Michael acceptors inhibited both rhodesain and falcipain-2, at nanomolar and micromolar levels, respectively. In particular, the vinyl ketone 3b has emerged as a potent rhodesain inhibitor (k2nd = 67 × 106 M-1 min-1), endowed with a picomolar b…

0301 basic medicineCathepsin LAntimalarialPeptideHeLa Cell01 natural sciencesCysteine Proteinase InhibitorDipeptideDrug DiscoveryPeptide sequencechemistry.chemical_classificationTrypanocidal AgentbiologyNeglected DiseasesStereoisomerismDipeptidesTrypanocidal AgentsMAJOR CYSTEINE PROTEASE PLASMODIUM-FALCIPARUM TRYPANOSOMA-BRUCEI CONFORMATIONAL-ANALYSIS BIOLOGICAL EVALUATION HIGHLY POTENT VINYL-ESTER INHIBITORS PEPTIDOMIMETICS SUBSTRATEMolecular Docking SimulationCysteine EndopeptidasesBiochemistryMolecular MedicineHumanProteasesNeglected DiseaseStereochemistryPhenylalaninePlasmodium falciparumTrypanosoma brucei bruceiCysteine Proteinase InhibitorsMolecular Dynamics SimulationTrypanosoma bruceiAntimalarialsStructure-Activity Relationship03 medical and health sciencesparasitic diseasesHumansStructure–activity relationship010405 organic chemistryDrug Discovery3003 Pharmaceutical ScienceHydrogen BondingTrypanosoma brucei rhodesiensePlasmodium falciparumbiology.organism_classificationMalaria0104 chemical sciencesTrypanosomiasis African030104 developmental biologychemistryCarbamateCarbamatesCysteine EndopeptidaseHeLa CellsCysteineJournal of Medicinal Chemistry
researchProduct