Search results for "pine"

showing 10 items of 2022 documents

Insight on pyrimido[5,4-g]indolizine and pyrimido[4,5-c]pyrrolo[1,2-a]azepine systems as promising photosensitizers on malignant cells

2022

Searching for new small molecules as photosensitizing agents, we have developed a class of twenty-five pyrimido[5,4-g]indolizine and pyrimido[4,5-c]pyrrolo[1,2-a]azepines with a good substitution pattern defining a versatile synthetic pathway to approach the title ring system. All compounds were evaluated for their photocytotoxicity on a triple negative human breast cancer cell line (MDA-MB-231) in the dark and under UVA light (2.0 J/cm2). The most effective compounds exhibited a photoantiproliferative activity with IC50 values up to nanomolar ranges. Interestingly, these new developed compounds showed high selectivity towards cancerous cells with respect to non-cancerous ones. Moreover, fo…

PharmacologyMDA-MB-231Triple negative human breast cancerOrganic ChemistryPhototoxic activityIndolizinesAntineoplastic AgentsApoptosisTriple Negative Breast Neoplasms4-g]indolizinespyrimido[4General MedicineAzepinespyrimido[54-g]indolizinespyrimido[45-c]pyrrolo[12-a]azepinesTriple negative human breast cancerMDA-MB-231Photosensitizing agentsPhototoxic activitypyrimido[5Photosensitizing agents5-c]pyrrolo[1pyrimido[45-c]pyrrolo[12-a]azepinesCell Line Tumor2-a]azepinesTriple negative human breast cancerMDA-MB-231Photosensitizing agentsPhototoxic activityDrug DiscoveryHumanspyrimido[54-g]indolizines
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Barnidipine block of L-type Ca2+ channel currents in rat ventricular cardiomyocytes

2000

The effects of barnidipine and nifedipine on L-type Ca2+ current (ICa(L)) were investigated in ventricular cardiomyocytes from rats. Both barnidipine and nifedipine reduced ICa(L) in a concentration and voltage dependent manner; the EC50 were 80 and 130 nM at a holding potential of −80 mV, respectively, and 18 and 6 nM at −40 mV, respectively. Both drugs induced a leftward shift of the steady-state inactivation curve of ICa(L). Using a twin pulse protocol, the relationships between the amount of block of ICa(L) by either drug, seen during the second pulse, and the length of the first pulse were described by monoexponential functions reflecting onset of block, dependent on drug concentration…

PharmacologyMembrane potentialBarnidipinePulse (signal processing)ChemistryDihydropyridineCardiac musclePharmacologyElectrophysiologymedicine.anatomical_structureNifedipinemedicinePatch clampmedicine.drugBritish Journal of Pharmacology
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DMPP and the adrenergic nerve terminal: mechanisms of noradrenaline release from vesicular and extravesicular compartments.

1977

DMPP (1,1-dimethyl-4-phenylpiperazine) in various concentrations between 1.6×10−6 M and 6.2×10−5 M was infused into isolated rabbit hearts to study the neuronal release and uptake of noradrenaline.

PharmacologyNeuronsmedicine.medical_specialtySympathetic Nervous SystemChemistryMyocardiumPharmacology toxicologyAdrenergicMyocardium metabolismHeartGeneral MedicinePharmacologyIn Vitro TechniquesPiperazinesNorepinephrineEndocrinologyInternal medicinemedicineAnimalsNorepinephrine metabolismRabbitsDimethylphenylpiperazinium IodideNaunyn-Schmiedeberg's archives of pharmacology
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Die Wirkung von Pharmaka auf die Elimination von Noradrenalin aus der Perfusionsfl�ssigkeit und die Noradrenalinaufnahme in das isolierte Herz

1964

PharmacologyNorepinephrine (medication)Isolation perfusionChemistryPharmacology toxicologymedicineGeneral MedicinePharmacologyGuanethidinemedicine.drugNaunyn-Schmiedebergs Archiv f�r Experimentelle Pathologie und Pharmakologie
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Therapeutic monitoring of new antipsychotic drugs.

2004

Typical antipsychotic drugs qualify for therapeutic drug monitoring (TDM) primarily for the following reasons: control of compliance and avoidance of extrapyramidal side effects by keeping chronic exposure to minimal effective blood levels. For the atypical antipsychotic clozapine, drug safety is another reason to use TDM. With regard to the new antipsychotics risperidone, olanzapine, quetiapine, amisulpride, ziprasidone, and aripiprazole, which have been introduced in the clinic during the last few years, the rationale to use TDM is a matter of debate. Positron emission tomography (PET), which enables measurement of the occupancy of dopamine D2 receptors, revealed that receptor occupancy c…

PharmacologyOlanzapinemedicine.diagnostic_testDose-Response Relationship Drugmedicine.drug_classbusiness.industryReceptors Dopamine D2medicine.medical_treatmentAtypical antipsychoticPharmacologyTypical antipsychoticStructure-Activity RelationshipTherapeutic drug monitoringmedicineQuetiapineHumansPharmacology (medical)ZiprasidoneAmisulprideDrug MonitoringAntipsychoticbusinessmedicine.drugAntipsychotic AgentsTherapeutic drug monitoring
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Low concentration of ziprasidone in human milk: a case report

2009

Although second-generation antipsychotics are established as the first-line treatment for schizophrenia, female patients are often excluded from this efficient treatment for safety reasons in pregnancy or whilst breastfeeding. For this reason, research on this subject mostly relies on case reports, although there is a great need to establish modern guidelines for treatment. Milk-to-plasma (M:P) ratios have been reported for clozapine (2.79–4.32; Winans, 2001), olanzapine (0.10–0.84; Gardiner et al. 2003), risperidone/9-OH risperidone (0.10–0.42/0.24–0.50; Gentile, 2004) and aripiprazole (0.18–0.20; Schlotterbeck et al. 2007). According to one case report, the infant ingests 0.09–0.43% of th…

PharmacologyOlanzapinemedicine.medical_specialtyPediatricsRisperidonebusiness.industryBreastfeedingPsychiatry and Mental healthPsychiatric historymedicinePsychiatric hospitalQuetiapinePharmacology (medical)AripiprazoleZiprasidonebusinessPsychiatrymedicine.drugThe International Journal of Neuropsychopharmacology
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(+)-α-Pinene in the defensive secretion ofNasutitermes princeps (Isoptera, Termitidae)

1990

The frontal secretion ofNasutitermes princeps consists of 89% diterpenes and 11% monoterpenes. In the samples studied, (+)-α-pinene, whose optical purity reaches 99.5%, accounts for more than 80% of the monoterpenic content.

PharmacologyPinenealpha-PineneMonoterpeneCell BiologyBiologyNasutitermes princepsbiology.organism_classificationTerpeneCellular and Molecular Neurosciencechemistry.chemical_compoundTermitidaechemistryBotanyMolecular MedicineSecretionDiterpeneMolecular BiologyExperientia
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Model-independent method of the analysis of distribution of 1,4-benzodiazepine derivatives possessing psychotropic activity after a single administra…

2010

PharmacologySingle administrationBenzodiazepineChemistrymedicine.drug_classStereochemistrymedicineDistribution (pharmacology)General MedicinePharmacological Reports
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Die Aufnahme von ?-Methylnoradrenalin in das isolierte Kaninchenherz und seine Freisetzung durch Reserpin und Guanethidin in vivo

1965

PharmacologySympathetic nervous systemmedicine.anatomical_structureChemistryPharmacology toxicologymedicineGeneral MedicineMethyldopaPharmacologyReserpinePargylineGuanethidinemedicine.drugNaunyn-Schmiedebergs Archiv f�r Experimentelle Pathologie und Pharmakologie
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Die Noradrenalin-Abgabe aus dem isolierten Kaninchenherzen bei sympathischer Nervenreizung und ihre pharmakologische Beeinflussung

1962

PharmacologyTetracaineChemistrychemistry.chemical_elementSympathetic nerveGeneral MedicineReserpinePharmacologyCalciummedicine.disease_causeNorepinephrine (medication)Hexamethonium compoundmedicineIrritationGuanethidinemedicine.drugNaunyn-Schmiedeberg's Archiv für Experimentelle Pathologie und Pharmakologie
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