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| Ujian Kebolehtelapan Sel Caco-2× | Elektrofisiologi Patch-Clamp× | Pemodelan Farmakodinamik Populasi× | |
|---|---|---|---|
| Bidang | Farmakologi | Farmakologi | Farmakologi |
| Keluarga | Process / pipeline | Process / pipeline | Process / pipeline |
| Tahun asal≠ | 1989 | 1976 | 1992 |
| Pengasas≠ | Ingrid Hidalgo | Erwin Neher and Bert Sakmann | Lewis Sheiner and Stephen Roush |
| Jenis≠ | absorption screening | ion channel screening | dose-response modeling |
| Sumber perintis≠ | Hidalgo, I. J., Raub, T. J., & Borchardt, R. T. (1989). Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability. Gastroenterology, 96(3), 736-749. DOI ↗ | Neher, E., & Sakmann, B. (1976). Single-channel currents recorded from membrane of denervated frog muscle fibres. Nature, 260(5554), 799-802. DOI ↗ | Dahlström, B., & Nyberg, L. (1993). Population pharmacokinetics and pharmacodynamics. Clinical Pharmacokinetics, 24(1), 45-57. link ↗ |
| Alias | Caco-2 assay, intestinal permeability, ADME screening | patch clamp, whole-cell recording, ion channel assay | PopPD, population PD, hierarchical PD modeling |
| Berkaitan | 3 | 3 | 3 |
| Ringkasan≠ | The Caco-2 assay is an in vitro model system using human colon carcinoma cell monolayers to screen drug intestinal permeability. Developed by Hidalgo and colleagues in 1989, Caco-2 cells differentiate into an epithelial barrier resembling intestinal mucosa, enabling rapid assessment of drug absorption potential and identification of transporter-mediated transport. | Patch-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. | 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. |
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