0000000000796148

AUTHOR

Anna-kaisa Rimpelä

0000-0003-4093-3465

showing 2 related works from this author

Interpretation of Ocular Melanin Drug Binding Assays. Alternatives to the Model of Multiple Classes of Independent Sites

2016

Melanin has a high binding affinity for a wide range of drugs. The determination of the melanin binding capacity and its binding affinity are important, e.g., in the determination of the ocular drug distribution, the prediction of drug effects in the eye, and the trans-scleral drug delivery. The binding parameters estimated from a given data set vary significantly when using different isotherms or different nonlinear fitting methods. In this work, the commonly used bi-Langmuir isotherm, which assumes two classes of independent sites, is confronted with the Sips isotherm. Direct, log-log, and Scatchard plots are used, and the interpretation of the binding curves in the latter is critically a…

Drugmedia_common.quotation_subjectBinding energyPharmaceutical Science02 engineering and technology010402 general chemistryBioinformatics01 natural sciencesInterpretation (model theory)MelaninGoodness of fitMelanin bindingFitting methodsDrug Discoverymedia_commonMelaninsScatchard plotChemistrytechnology industry and agricultureChloroquineModels Theoretical021001 nanoscience & nanotechnology0104 chemical sciencesKineticsBiophysicsMolecular Medicine0210 nano-technologyMetoprololMolecular Pharmaceutics
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Drug Distribution to Retinal Pigment Epithelium: Studies on Melanin Binding, Cellular Kinetics, and Single Photon Emission Computed Tomography/Comput…

2016

Melanin binding is known to affect the distribution and elimination of ocular drugs. The purpose of this study was to evaluate if the extent of drug uptake to primary retinal pigment epithelial (RPE) cells could be estimated based on in vitro binding studies with isolated melanin and evaluate the suitability of single photon emission computed tomography/computed tomography (SPECT/CT) in studying pigment binding in vivo with pigmented and albino rats. Binding of five compounds, basic molecules timolol, chloroquine, and nadolol and acidic molecules methotrexate and 5(6)-carboxy-2',7'-dichlorofluorescein (CDCF), was studied using isolated melanin from porcine choroid-RPE at pH 5.0 and 7.4. The…

0301 basic medicinePathologymedicine.medical_specialtySingle Photon Emission Computed Tomography Computed TomographySwinePigment bindingPharmaceutical ScienceTimololRetinal Pigment EpitheliumBiologySingle-photon emission computed tomographyEye030226 pharmacology & pharmacyIodine RadioisotopesMelanin03 medical and health scienceschemistry.chemical_compound0302 clinical medicineIn vivoDrug DiscoverymedicineAnimalsDistribution (pharmacology)Cells CulturedMelaninsRetinal pigment epitheliummedicine.diagnostic_testChloroquineRetinalHydrogen-Ion Concentrationeye diseasesRats3. Good healthKineticsNadololMethotrexate030104 developmental biologymedicine.anatomical_structurechemistryTimololBiophysicsMolecular Medicinesense organsProtein Bindingmedicine.drugMolecular Pharmaceutics
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