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10.1021/acs.jmedchem.0c01912 http://scihub22266oqcxt.onion/10.1021/acs.jmedchem.0c01912 33426889!ä!33426889 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       J+Med+Chem 2021 ; 64 (2): 1170-1179 Nephropedia Template TP {{tp|p=33426889|t=2021. Ifenprodil Stereoisomers: Synthesis, Absolute Configuration, and Correlation with Biological Activity |pdf=|usr=}}{{33426889}} gab.com Text Ifenprodil Stereoisomers: Synthesis, Absolute Configuration, and Correlation with Biological Activity JO: J Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=33426889 #FOAvip Ifenprodil (1) is a potent GluN2B-selective N-methyl-d-aspartate (NMDA) receptor antagonist that is used as a cerebral vasodilator and has been examined in clinical trials for the treatment of drug addiction, idiopathic pulmonary fibrosis, and COVID-19. To correlate biological data with configuration, all four ifenprodil stereoisomers were prepared by diastereoselective reduction and subsequent separation of enantiomers by chiral HPLC. The absolute configuration of ifenprodil stereoisomers was determined by X-ray crystal structure analysis of (1R,2S)-1a and (1S,2S)-1d. GluN2B affinity, ion channel inhibitory activity, and selectivity over alpha, sigma, and 5-HT receptors were evaluated. (1R,2R)-Ifenprodil ((1R,2R)-1c) showed the highest affinity toward GluN2B-NMDA receptors (K(i) = 5.8 nM) and high inhibition of ion flux in two-electrode voltage clamp experiments (IC(50) = 223 nM). Whereas the configuration did not influence considerably the GluN2B-NMDA receptor binding, (1R)-configuration is crucial for elevated inhibitory activity. (1R,2R)-Configured ifenprodil (1R,2R)-1c exhibited high selectivity for GluN2B-NMDA receptors over adrenergic, serotonergic, and sigma(1) receptors. Twit Text FOAVip Ifenprodil Stereoisomers: Synthesis, Absolute Configuration, and Correlation with Biological Activity ????J Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=33426889 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=33426889 #FOAvip English Wikipedia <ref>{{Cite pmid|33426889}}</ref> Ifenprodil Stereoisomers: Synthesis, Absolute Configuration, and Correlation with Biological Activity #MMPMID33426889 Bechthold E; Schreiber JA; Lehmkuhl K; Frehland B; Schepmann D; Bernal FA; Daniliuc C; Alvarez I; Garcia CV; Schmidt TJ; Seebohm G; Wunsch B J Med Chem 2021[Jan]; 64 (2): 1170-1179 PMID33426889show ga Ifenprodil (1) is a potent GluN2B-selective N-methyl-d-aspartate (NMDA) receptor antagonist that is used as a cerebral vasodilator and has been examined in clinical trials for the treatment of drug addiction, idiopathic pulmonary fibrosis, and COVID-19. To correlate biological data with configuration, all four ifenprodil stereoisomers were prepared by diastereoselective reduction and subsequent separation of enantiomers by chiral HPLC. The absolute configuration of ifenprodil stereoisomers was determined by X-ray crystal structure analysis of (1R,2S)-1a and (1S,2S)-1d. GluN2B affinity, ion channel inhibitory activity, and selectivity over alpha, sigma, and 5-HT receptors were evaluated. (1R,2R)-Ifenprodil ((1R,2R)-1c) showed the highest affinity toward GluN2B-NMDA receptors (K(i) = 5.8 nM) and high inhibition of ion flux in two-electrode voltage clamp experiments (IC(50) = 223 nM). Whereas the configuration did not influence considerably the GluN2B-NMDA receptor binding, (1R)-configuration is crucial for elevated inhibitory activity. (1R,2R)-Configured ifenprodil (1R,2R)-1c exhibited high selectivity for GluN2B-NMDA receptors over adrenergic, serotonergic, and sigma(1) receptors. |Antifibrinolytic Agents/chemical synthesis/*chemistry/*pharmacology[MESH] |Antiviral Agents/chemical synthesis/*chemistry/*pharmacology[MESH] |COVID-19 Drug Treatment[MESH] |COVID-19/metabolism[MESH] |Crystallography, X-Ray[MESH] |Dose-Response Relationship, Drug[MESH] |Humans[MESH] |Idiopathic Pulmonary Fibrosis/drug therapy/metabolism[MESH] |Models, Molecular[MESH] |Molecular Structure[MESH] |Piperidines/*chemical synthesis/chemistry/*pharmacology[MESH] |Receptors, N-Methyl-D-Aspartate/*antagonists & inhibitors/metabolism[MESH] |Stereoisomerism[MESH]Ifenprodil Stereoisomers: Synthesis, Absolute Configuration, and Corre(epmc).pdf DeepDyve Pubget Overpricing