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10.1021/acschemneuro.5b00137 http://scihub22266oqcxt.onion/10.1021/acschemneuro.5b00137 C4641535!4641535!26148793     free     free     free Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       ACS+Chem+Neurosci 2015 ; 6 (9): 1570-7 Nephropedia Template TP {{tp|p=26148793|t=2015. Synthesis of Carfentanil Amide Opioids Using the Ugi Multicomponent Reaction |pdf=|usr=}}{{26148793}} gab.com Text Synthesis of Carfentanil Amide Opioids Using the Ugi Multicomponent Reaction JO: ACS Chem Neurosci http://www.kidney.de/pget.php?&tw=1&pmid=26148793 #FOAvip We report a novel approach to synthesize carfentanil amide analogues utilizing the isocyanide-based four-component Ugi multicomponent reaction. A small library of bis-amide analogues of carfentanil was created using N-alkylpiperidones, aniline, propionic acid, and various aliphatic isocyanides. Our lead compound showed high affinity for mu (MOR) and delta opioid receptors (DOR) with no appreciable affinity for kappa (KOR) receptors in radioligand binding assays. The compound was found to be a mixed MOR agonist/partial DOR agonist in [35S]GTP?S functional assays, and it showed moderate analgesic potency in vivo. The compound showed no visible signs of physical dependence or constipation in mice. In addition, it produced less respiratory depression than morphine. Most mixed MOR/DOR opioids reported in the literature are peptides and thereby systemically inactive. Our approach utilizing a multicomponent reaction has the promise to deliver potent and efficacious small-molecule analgesics with potential clinical utility. Twit Text FOAVip Synthesis of Carfentanil Amide Opioids Using the Ugi Multicomponent Reaction ????ACS Chem Neurosci http://www.kidney.de/pget.php?&tw=1&pmid=26148793 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=26148793 #FOAvip English Wikipedia <ref>{{Cite pmid|26148793}}</ref> Synthesis of Carfentanil Amide Opioids Using the Ugi Multicomponent Reaction #MMPMID26148793 Váradi A; Palmer TC; Haselton N; Afonin D; Subrath JJ; Le Rouzic V; Hunkele A; Pasternak GW; Marrone GF; Borics A; Majumdar S ACS Chem Neurosci 2015[Sep]; 6 (9): 1570-7 PMID26148793show ga We report a novel approach to synthesize carfentanil amide analogues utilizing the isocyanide-based four-component Ugi multicomponent reaction. A small library of bis-amide analogues of carfentanil was created using N-alkylpiperidones, aniline, propionic acid, and various aliphatic isocyanides. Our lead compound showed high affinity for mu (MOR) and delta opioid receptors (DOR) with no appreciable affinity for kappa (KOR) receptors in radioligand binding assays. The compound was found to be a mixed MOR agonist/partial DOR agonist in [35S]GTP?S functional assays, and it showed moderate analgesic potency in vivo. The compound showed no visible signs of physical dependence or constipation in mice. In addition, it produced less respiratory depression than morphine. Most mixed MOR/DOR opioids reported in the literature are peptides and thereby systemically inactive. Our approach utilizing a multicomponent reaction has the promise to deliver potent and efficacious small-molecule analgesics with potential clinical utility. äSynthesis of Carfentanil Amide Opioids Using the Ugi Multicomponent Re(epmc).pdf DeepDyve Pubget Overpricing