Intact Cell Binding for In Vitro Prediction of Sedative and Non-sedative Histamine H1–Receptor Antagonists Based on Receptor Internalization

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Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization.

We evaluated changes in the binding properties of sedative and non-sedative histamine H1-receptor antagonists induced by internalization of H1 receptors in intact human U373 MG astrocytoma cells. Internalization of H1 receptors was induced without their degradation by treatment with 0.1 mM histamine for 30 min at 37 degrees C, and then the intact cell binding assay was performed at 4 degrees C....

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Comparison of Different 2D and 3D-QSAR Methods on Activity Prediction of Histamine H3 Receptor Antagonists

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Comparison of Different 2D and 3D-QSAR Methods on Activity Prediction of Histamine H3 Receptor Antagonists

     Histamine H3 receptor subtype has been the target of several recent drug development programs. Quantitative structure-activity relationship (QSAR) methods are used to predict the pharmaceutically relevant properties of drug candidates whenever it is applicable. The aim of this study was to compare the predictive powers of three different QSAR techniques, namely, multiple linear regression ...

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Sedative-Hypnotic and Receptor Binding Studies of Fermented Marine Organisms

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comparison of different 2d and 3d-qsar methods on activity prediction of histamine h3 receptor antagonists

histamine h3 receptor subtype has been the target of several recent drug development programs. quantitative structure-activity relationship (qsar) methods are used to predict the pharmaceutically relevant properties of drug candidates whenever it is applicable. the aim of this study was to compare the predictive powers of three different qsar techniques, namely, multiple linear regression (mlr)...

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ژورنال

عنوان ژورنال: Journal of Pharmacological Sciences

سال: 2008

ISSN: 1347-8613,1347-8648

DOI: 10.1254/jphs.fp0071865