Search results for "harm"

showing 10 items of 13866 documents

The neglected hepatitis C virus genotypes 4, 5 and 6: an international consensus report

2009

Abstract Hepatitis C virus (HCV) genotypes 4, 5 and 6 represent20% of all HCV cases worldwide. HCV-4 is mainly seen in Egypt, where it represents 90% of all HCV cases. Antischistosomal therapy was the main cause of contamination there, followed by procedures performed by informal providers and traditional healers such as dental care, wound treatment, circumcision, deliveries, excision and scarification. It is also highly prevalent in sub-Saharan Africa and in the Middle East. In Europe, its prevalence has recently increased particularly among intravenous drug users and in immigrants. HCV-5 is mainly found in South Africa, where it represents 40% of all HCV genotypes, but four pockets of HCV…

medicine.medical_specialtyGenotypeHepatitis C virusHepacivirusmedicine.disease_causechemistry.chemical_compoundPharmacotherapyPegylated interferonInternal medicineEpidemiologyPrevalencemedicineHumansHepatologybusiness.industryTransmission (medicine)Ribavirinvirus diseasesHepatitis Cmedicine.diseaseHepatitis CVirologydigestive system diseaseschemistryHCVbusinessViral hepatitismedicine.drugLiver International
researchProduct

Hepatotoxicity caused by mebendazole in a patient with Gilbert's syndrome

2019

What is known and objective Mebendazole (MBZ) is a broad-spectrum antihelminthic agent of the benzimidazole type. Although MBZ has been reported to cause hepatic injury, case reports of severe hepatic injury are very rare. We report a case of severe hepatitis after administration of MBZ in a patient with Gilbert's syndrome affected by pinworms infestation. Case summary Differently from other cases of hepatitis due to MBZ reported in the scientific literature, our patient received standard doses of MBZ for a short period of time. After 18 days from the start of therapy, he developed hepatomegaly, and increases in hepatic enzymes and bilirubin. Hepatic enzymes returned to normal over the foll…

medicine.medical_specialtyGlucuronosyltransferaseSettore MED/17 - Malattie InfettiveBilirubinMebendazoleGlucuronidation030226 pharmacology & pharmacyGastroenterology03 medical and health scienceschemistry.chemical_compound0302 clinical medicineInternal medicineMedicinePharmacology (medical)030212 general & internal medicinePharmacologyHepatitisLiver injurybiologybusiness.industrydrug toxicity Gilbert's syndrome hepatitis mebendazolemedicine.diseaseAntihelminthic AgentGilbert's syndromechemistrySettore BIO/14 - Farmacologiabiology.proteinbusinessmedicine.drugJournal of Clinical Pharmacy and Therapeutics
researchProduct

New Melanocortin 1 Receptor Binding Motif Based on the C-Terminal Sequence of ?-Melanocyte-Stimulating Hormone

2006

The C-terminal tripeptide of the alpha-melanocyte stimulating hormone (alpha-MSH11-13) possesses strong antiinflammatory activity without known cellular target. In order to better understand the structural requirements for function of such motif, we designed, synthesized and tested out Trp- and Tyr-containing analogues of the alpha-MSH11-13. Seven alpha-MSH11-13 analogues were synthesized and characterized for their binding to the melanocortin receptors recombinantly expressed in insect (Sf9) cells, infected with baculovirus carrying corresponding MC receptor DNA. We also tested these analogues on B16-F1 mouse melanoma cells endogenously expressing the MC1 receptor for binding and for abili…

medicine.medical_specialtyGrowth-hormone-releasing hormone receptorProtein ConformationAmino Acid MotifsMelanoma ExperimentalBiologyToxicologyBinding CompetitiveMiceThyrotropin-releasing hormone receptorInternal medicineChlorocebus aethiopsmedicineEnzyme-linked receptorAnimalsHumansACTH receptorMelanocyte-Stimulating HormonesReceptorPharmacologyGeneral MedicineMelanocortin 3 receptorCell biologyEndocrinologyCOS CellsEstrogen-related receptor gammaMelanocortinReceptor Melanocortin Type 1Basic <html_ent glyph="@amp;" ascii="&"/> Clinical Pharmacology <html_ent glyph="@amp;" ascii="&"/> Toxicology
researchProduct

gamma-Aminobutyric acid and cholinergic transmission in the guinea-pig ileum.

1983

1. The effects of GABA on release of acetylcholine and on contractility of the smooth muscle were studied in the myenteric plexus-longitudinal muscle preparation of the guinea pig. Acetylcholine was determined as radiolabelled transmitter from strips preloaded with 3H-choline. 2. GABA (1–300 μM) caused an increase in resting tension of smooth muscle as well as an increase in release of acetylcholine that was considerably reduced by tetrodotoxin. The facilitation by GABA of acetylcholine release exhibited a marked tachyphylaxis. The increase in muscle tension was clearly related to the increase in acetylcholine release. Muscimol (0.1–10 μM) also enhanced the release of acetylcholine. The eff…

medicine.medical_specialtyGuinea PigsIn Vitro TechniquesBicucullineTritiumSynaptic Transmissiongamma-Aminobutyric acidchemistry.chemical_compoundIleumInternal medicineMuscle tensionMuscarinic acetylcholine receptormedicineAnimalsPicrotoxingamma-Aminobutyric AcidPharmacologyMuscimolMuscle SmoothGeneral MedicineBicucullineAcetylcholineElectric StimulationEndocrinologynervous systemchemistryMuscimolCholinergicAcetylcholinemedicine.drugPicrotoxinMuscle ContractionNaunyn-Schmiedeberg's archives of pharmacology
researchProduct

Characterization of prejunctional muscarinic autoreceptors in the guinea-pig trachea

1991

1. The effects of ten muscarinic antagonists on electrically evoked [3H]-acetylcholine release and muscle contraction were compared in an epithelium-free preparation of the guinea-pig trachea that had been preincubated with [3H]-choline. 2. The M3-selective antagonists UH-AH 37, 4-diphenyl-acetoxy-N-piperidine methobromide and para-fluorohexahydrosiladiphenidol were more potent in reducing the contractile response than in facilitating the evoked [3H]-acetylcholine release. Hexahydrosiladiphenidol did not discriminate between pre- and postjunctional effects. The rank order of the postjunctional potencies of the ten antagonists as well as the postjunctional pA2 values obtained for hexahydrosi…

medicine.medical_specialtyGuinea PigsIn Vitro TechniquesBiologyCholinechemistry.chemical_compoundInternal medicineMuscarinic acetylcholine receptormedicineMethoctramineAnimalsReceptorPharmacologyParasympatholyticsMuscarinic acetylcholine receptor M3Muscle SmoothMuscarinic acetylcholine receptor M2Receptors MuscarinicAcetylcholineElectric StimulationTracheaEndocrinologychemistryAutoreceptormedicine.symptomAcetylcholineMuscle ContractionResearch Articlemedicine.drugMuscle contractionBritish Journal of Pharmacology
researchProduct

Inhibitory and excitatory muscarinic receptors modulating the release of acetylcholine from the postganglionic parasympathetic neuron of the chicken …

1992

The effects of muscarinic receptor antagonists on ACh release were studied in the absence or presence of cholinesterase (ChE) inhibition using the isolated perfused chicken heart. Presynaptic inhibitory muscarinic autoreceptor were characterized by determining the potency of various antagonists to enhance [3H]-ACh release evoked by field stimulation (3 Hz, 1 min). The order of potencies was: (±)-telenzepine > atropine > 4-DAMP > silahexocyclium > pirenzepine > hexahydro-siladifenidol > AF-DX 116. The comparison with known pA2 values for M1-, M2- and M3-receptors revealed that the presynaptic autoreceptor meets the criteria of an M1-receptor. Basal, not electrically evoked overflow of unlabe…

medicine.medical_specialtyGuinea PigsMuscarinic AntagonistsInhibitory postsynaptic potentialchemistry.chemical_compoundHeart RateInternal medicineMuscarinic acetylcholine receptormedicineMuscarinic acetylcholine receptor M4AnimalsPharmacologyChemistryMyocardiumHeartMuscle SmoothGeneral MedicinePirenzepineMyocardial ContractionAcetylcholineElectric StimulationAtropineEndocrinologyTelenzepineAutoreceptorCholinesterase InhibitorsChickensAcetylcholinemedicine.drugNaunyn-Schmiedeberg's archives of pharmacology
researchProduct

Increase by NO synthase inhibitors of acetylcholine release from guinea-pig myenteric plexus

1994

The effects of nitric oxide (NO) synthase inhibitors on the electrically evoked release of [3H]acetylcholine were studied in guinea-pig myenteric plexus preparations preincubated with [3H]choline. NG-monomethyl-L-arginine (EC50 5.3 mumol l-1) and NG-nitro-L-arginine (EC50 1.3 mumol l-1) concentration-dependently increased the evoked release of [3H]acetylcholine without affecting the basal outflow. The facilitatory effect of NG-mono-methyl-L-arginine was prevented by L-arginine but not by D-arginine. The results suggest that endogenous NO inhibits the depolarisation-evoked release of acetylcholine.

medicine.medical_specialtyGuinea PigsMyenteric PlexusArginineNitric OxideNitroarginineNitric oxideGuinea pigchemistry.chemical_compoundInternal medicinemedicineAnimalsCholineEvoked PotentialsMyenteric plexusPharmacologyomega-N-MethylargininebiologyMuscle SmoothGeneral MedicineAcetylcholineElectric StimulationNitric oxide synthaseEndocrinologychemistryEnzyme inhibitorbiology.proteinLiberationAmino Acid OxidoreductasesNitric Oxide SynthaseAcetylcholinemedicine.drugNaunyn-Schmiedeberg's Archives of Pharmacology
researchProduct

Choline inhibits acetylcholine release via presynaptic muscarine receptors

1981

The effect of exogenous choline on the outflow of 3H-acetylcholine evoked by field stimulation was studied on the myenteric plexus-longitudinal muscle preparation of the guinea pig. Choline at concentrations of 100 microM and higher depressed the evoked outflow of 3H-acetylcholine in a concentration-dependent manner. The EC50 for the inhibitory action was 300 microM. Scopolamine (10 nM) antagonized the effect of choline which indicates that the inhibition of 3H-acetylcholine outflow is mediated by muscarine receptors. The findings imply that choline at high concentrations does not improve cholinergic synaptic neurotransmission in tissues that are endowed with presynaptic muscarine receptors…

medicine.medical_specialtyGuinea PigsScopolamineMyenteric PlexusIn Vitro TechniquesTritiumInhibitory postsynaptic potentialCholinechemistry.chemical_compoundHemicholinium-3Internal medicinemedicineAnimalsCholineReceptors CholinergicMyenteric plexusPharmacologyMuscarineHemicholinium 3General MedicineReceptors MuscarinicCholine acetyltransferaseAcetylcholineEndocrinologychemistryCholinergicNeuroscienceAcetylcholineMuscle Contractionmedicine.drugNaunyn-Schmiedeberg's Archives of Pharmacology
researchProduct

Two types of neuronal muscarine receptors modulating acetylcholine release from guinea-pig myenteric plexus

1985

Longitudinal muscle strips of the guinea-pig ileum were incubated with [3H]choline and the effects of muscarinic agonists on smooth muscle contraction and on spontaneous and electrically-evoked outflow of tritium were studied. Muscarine and pilocarpine concentration-dependently increased both muscle contraction and spontaneous outflow of [3H]ACh, and inhibited the electrically-evoked outflow of [3H]ACh. The increase in spontaneous outflow was prevented by tetrodotoxin and scopolamine, but not by hexamethonium. Oxotremorine (1-100 microM) did not increase the spontaneous outflow of tritium. Pirenzepine in concentrations of 10 and 100 nM hardly affected the muscle contractions induced by pilo…

medicine.medical_specialtyGuinea PigsScopolamineMyenteric PlexusIn Vitro Techniqueschemistry.chemical_compoundIleumMuscarineInternal medicineMuscarinic acetylcholine receptormedicineOxotremorineAnimalsPharmacologyBenzodiazepinonesMuscarineOxotremorinePilocarpinePirenzepineGeneral MedicineSmooth muscle contractionReceptors MuscarinicPirenzepineAcetylcholineEndocrinologychemistrycardiovascular systemHexamethoniummedicine.symptomAcetylcholineMuscle ContractionMuscle contractionmedicine.drugNaunyn-Schmiedeberg's Archives of Pharmacology
researchProduct

Release of [3H]acetylcholine from the isolated rat or guinea-pig trachea evoked by preganglionic nerve stimulation; a comparison with transmural stim…

1991

Basal and stimulated outflow of radioactive acetylcholine, phosphorylcholine and choline from rat and guinea-pig isolated tracheae were measured by reverse phase HPLC followed by liquid-scintillation-spectrometry. Tracheae were stimulated either by an electrical field (transmural stimulation) or by a local stimulation of the innervating parasympathetic nerves (preganglionic stimulation). Epithelium was removed in most experiments, as the epithelium inhibits acetylcholine release. The basal tritium efflux (1,600 dpm/3min) from rat isolated tracheae incubated with [3H]choline consisted of 56% [3H]phosphorylcholine and 38% [3H]choline. Preganglionic stimulation (15 Hz, 1,200 pulses) caused a 2…

medicine.medical_specialtyGuinea PigsTubocurarineStimulationHexamethonium CompoundsTetrodotoxinBiologyIn Vitro TechniquesEpitheliumCholineGuinea pigchemistry.chemical_compoundInternal medicineMuscarinic acetylcholine receptorOxotremorinemedicineAnimalsChromatography High Pressure LiquidPharmacologyNeuronsPhosphorylcholineOxotremorineEpithelial CellsGanglia ParasympatheticGeneral MedicineAcetylcholineElectric StimulationRatsTracheaEndocrinologychemistryTetrodotoxinAcetylcholinesteraseHexamethoniumCalciumAcetylcholinemedicine.drugNaunyn-Schmiedeberg's archives of pharmacology
researchProduct