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Patch-Clamp Elektrofsioloogia×Michaelis-Menteni kineetika×Population Pharmacodynamics×Schildi analüüs×
ValdkondFarmakoloogiaFarmakoloogiaFarmakoloogiaFarmakoloogia
PerekondProcess / pipelineProcess / pipelineProcess / pipelineProcess / pipeline
Tekkeaasta1976191319921947
LoojaErwin Neher and Bert SakmannLeonor Michaelis and Maud MentenLewis Sheiner and Stephen RoushHenry Schild
Tüüpion channel screeningmechanistic modeldose-response modelingantagonism quantification
AlgallikasNeher, E., & Sakmann, B. (1976). Single-channel currents recorded from membrane of denervated frog muscle fibres. Nature, 260(5554), 799-802. DOI ↗Michaelis, L., & Menten, M. L. (1913). Die Kinetik der Invertinwirkung. Biochemische Zeitschrift, 49, 333-369. link ↗Dahlström, B., & Nyberg, L. (1993). Population pharmacokinetics and pharmacodynamics. Clinical Pharmacokinetics, 24(1), 45-57. link ↗Schild, H. O. (1947). pA, a new scale for the measurement of drug antagonism. Journal of Physiology, 106(3), 337-357. DOI ↗
Rööpnimetusedpatch clamp, whole-cell recording, ion channel assayMM kinetics, Michaelis constant, VmaxPopPD, population PD, hierarchical PD modelingSchild plot, pA2
Seotud3233
KokkuvõtePatch-clamp electrophysiology is a technique for measuring ionic currents through ion channels in cell membranes, developed by Neher and Sakmann in 1976. It enables direct observation of single-channel and whole-cell currents at millisecond resolution, making it essential for characterizing drug effects on ion channels and cardiac safety assessment.Michaelis-Menten kinetics describes the rate of enzyme-catalyzed reactions as a function of substrate concentration. Developed by Leonor Michaelis and Maud Menten in 1913, this foundational framework models enzyme catalysis through the rapid-equilibrium approximation and enables prediction of drug metabolism rates in pharmacokinetics.Population pharmacodynamic (PopPD) modeling integrates pharmacokinetics with individual dose-response relationships across patient populations to characterize drug efficacy and tolerability. Pioneered by Lewis Sheiner and colleagues, PopPD accounts for inter-individual variability in drug effects and enables rational dose optimization and response prediction.Schild analysis is a quantitative method for characterizing competitive receptor antagonism developed by Henry Schild in 1947. It uses dose-response curves in the presence and absence of antagonist to estimate the antagonist affinity constant (pA2), enabling standardized comparison of antagonist potency across drugs and experimental systems.
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ScholarGateVõrdle meetodeid: Patch-Clamp · Michaelis-Menten Kinetics · Population Pharmacodynamics · Schild Analysis. Loetud 2026-06-19 aadressilt https://scholargate.app/et/compare