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10.1021/acs.jmedchem.0c01964 http://scihub22266oqcxt.onion/10.1021/acs.jmedchem.0c01964 33372782!ä!33372782 Deprecated: Implicit conversion from float 209.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 209.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 209.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 209.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Warning: imagejpeg(C:\Inetpub\vhosts\kidney.de\httpdocs\phplern\33372782.jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117       J+Med+Chem 2021 ; 64 (1): 890-904 Nephropedia Template TP {{tp|p=33372782|t=2021. Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management |pdf=|usr=}}{{33372782}} gab.com Text Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management JO: J Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=33372782 #FOAvip The sigma 1 receptor (S1R) is a molecular chaperone protein located in the endoplasmic reticulum and plasma membranes and has been shown to play important roles in various pathological disorders including pain and, as recently discovered, COVID-19. Employing structure- and QSAR-based drug design strategies, we rationally designed, synthesized, and biologically evaluated a series of novel triazole-based S1R antagonists. Compound 10 exhibited potent binding affinity for S1R, high selectivity over S2R and 87 other human targets, acceptable in vitro metabolic stability, slow clearance in liver microsomes, and excellent blood-brain barrier permeability in rats. Further in vivo studies in rats showed that 10 exhibited negligible acute toxicity in the rotarod test and statistically significant analgesic effects in the formalin test for acute inflammatory pain and paclitaxel-induced neuropathic pain models during cancer chemotherapy. These encouraging results promote further development of our triazole-based S1R antagonists as novel treatments for pain of different etiologies. Twit Text FOAVip Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management ????J Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=33372782 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=33372782 #FOAvip English Wikipedia <ref>{{Cite pmid|33372782}}</ref> Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management #MMPMID33372782 Peng Y; Zhang Q; Welsh WJ J Med Chem 2021[Jan]; 64 (1): 890-904 PMID33372782show ga The sigma 1 receptor (S1R) is a molecular chaperone protein located in the endoplasmic reticulum and plasma membranes and has been shown to play important roles in various pathological disorders including pain and, as recently discovered, COVID-19. Employing structure- and QSAR-based drug design strategies, we rationally designed, synthesized, and biologically evaluated a series of novel triazole-based S1R antagonists. Compound 10 exhibited potent binding affinity for S1R, high selectivity over S2R and 87 other human targets, acceptable in vitro metabolic stability, slow clearance in liver microsomes, and excellent blood-brain barrier permeability in rats. Further in vivo studies in rats showed that 10 exhibited negligible acute toxicity in the rotarod test and statistically significant analgesic effects in the formalin test for acute inflammatory pain and paclitaxel-induced neuropathic pain models during cancer chemotherapy. These encouraging results promote further development of our triazole-based S1R antagonists as novel treatments for pain of different etiologies. |Animals[MESH] |Binding Sites[MESH] |Blood-Brain Barrier/metabolism[MESH] |Drug Design[MESH] |Guinea Pigs[MESH] |Half-Life[MESH] |Humans[MESH] |Microsomes, Liver/metabolism[MESH] |Molecular Dynamics Simulation[MESH] |Neuralgia/chemically induced/drug therapy[MESH] |Pain Management/*methods[MESH] |Protein Structure, Tertiary[MESH] |Quantitative Structure-Activity Relationship[MESH] |Rats[MESH] |Receptors, sigma/*antagonists & inhibitors/metabolism[MESH] |Sigma-1 Receptor[MESH]Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain (epmc).pdf DeepDyve Pubget Overpricing