Histamine H3 -receptor agonists and imidazole-based H3 -receptor antagonists can be thermodynamically discriminated
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چکیده
منابع مشابه
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 ...
متن کاملComparison 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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With the very recent market approval of pitolisant (Wakix®), the interest in clinical applications of novel multifunctional histamine H3 receptor antagonists has clearly increased. Since histamine H3 receptor antagonists in clinical development have been tested for a variety of different indications, the combination of pharmacological properties in one molecule for improved pharmacological effe...
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This article has not been copyedited and formatted. The final version may differ from this version. Abbreviations Imetit, 2-(1H-imidazol-5-yl)ethyl imidothiocarbamate, iodoproxyfan, 3-(1H-imidazol-4-yl)propyl-(4-iodophenyl)-methyl ether, proxyfan, 4-[3-(benzyloxy)propyl]-1H-imidazole, NαMH, N-α-methylhistamine dihydrochloride, pERK, phosphorylated extracellular signal-regulated kinase, RαMH, (R...
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Phenytoin (PHT), valproic acid, and modern antiepileptic drugs (AEDs), eg, remacemide, loreclezole, and safinamide, are only effective within a maximum of 70%-80% of epileptic patients, and in many cases the clinical use of AEDs is restricted by their side effects. Therefore, a continuous need remains to discover innovative chemical entities for the development of active and safer AEDs. Ligands...
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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 2007
ISSN: 0007-1188
DOI: 10.1038/sj.bjp.0707243