30 research outputs found
4-Hydroxy-1,2,5-oxadiazol-3-yl Moiety as Bioisoster of the Carboxy Function. Synthesis, Ionization Constants, and Molecular Pharmacological Characterization at Ionotropic Glutamate Receptors of Compounds Related to Glutamate and Its Homologues
Get PDFMonitoring and Control of a Continuous Grignard Reaction for the Synthesis of an Active Pharmaceutical Ingredient Intermediate Using Inline NIR spectroscopy
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Stereostructure-activity studies on agonists at the AMPA and kainate subtypes of ionotropic glutamate receptors
No full textStructures of the ligand-binding core of iGluR2 in complex with the agonists (R)- and (S)-2-amino-3-(4-hydroxy-1,2,5-thiadiazol-3-yl)propionic acid explain their unusual equipotency
No full textAMPA type ionotropic glutamate receptors generally display high stereoselectivity in agonist binding. However, the stereoisomers of 2 amino 3 4 hydroxy 1,2,5 thiadiazol 3 yl propionic acid TDPA have similar enantiopharmacology. To understand this observation, we have determined the X ray structures of R TDPA and S TDPA in complex with the ligand binding core of iGluR2 and investigated the binding pharmacology at AMPA and kainate receptors. Both enantiomers induce full domain closure in iGluR2 but adopt different conformations when binding to the receptor, which may explain the similar enantiopharmacolog
Bioactivation of diclofenac in vitro and in vivo: correlation to electrochemical studies
No full textSynthesis and Pharmacology of the Baclofen Homologues 5-Amino-4-(4-chlorophenyl)pentanoic Acid and the R
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