|
|||||
|
|
Fluorescent Benzofurazan–Cholic Acid Conjugates for in vitro Assessment of Bile Acid Uptake and Its Modulation by Drugs |
|
| Authors: | Jana Rohacova M. Luisa Marín Dr. Alicia Martinez‐Romero Dr. Laura Diaz José‐Enrique O'Connor Dr. M. Jose Gomez‐Lechon Dr. M. Teresa Donato Dr. José V. Castell Prof. Dr. Miguel A. Miranda Prof. Dr. |
| Affiliation: | 1. Instituto de Tecnología Química, Departamento de Química (UPV‐CSIC), Avda. de los Naranjos s/n, 46022 Valencia (Spain), Fax: (+34)?963877809;2. Laboratorio de Citómica, Unidad Mixta CIPF‐UVEG, Centro de Investigación Príncipe Felipe, Avda. Autopista del Saler 16‐3, 46013 Valencia (Spain);3. Unidad de Hepatología Experimental, Centro de Investigación Hospital Universitario “La?Fe”, Avda. Campanar, 46009 Valencia (Spain);4. CIBERHEPAD, FIS (Spain);5. Departamento de Bioquímica y Biología Molecular, Facultad de Medicina, Universidad de Valencia, Avda. Blasco Ibá?ez, 46020 Valencia (Spain) |
| Abstract: | Fluorescent synthetic 7‐nitrobenzo‐2‐oxa‐1,3‐diazole (NBD) conjugates of cholic acid were prepared and characterized. Their photophysical properties make them suitable for monitoring uptake in freshly isolated rat hepatocytes using flow cytometry. This technique makes it possible to screen drug candidates for cholestatic (and thus hepatotoxic) liability.  |
| Keywords: | chlorpromazine cholestasis flow cytometry hepatocytes troglitazone |