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Search for α3β₂/₃γ2 subtype selective ligands that are stable on human liver microsomes.
Namjoshi OA, Wang ZJ, Rallapalli SK, Johnson EM Jr, Johnson YT, Ng H, Ramerstorfer J, Varagic Z, Sieghart W, Majumder S, Roth BL, Rowlett JK, Cook JM. Namjoshi OA, et al. Among authors: sieghart w. Bioorg Med Chem. 2013 Jan 1;21(1):93-101. doi: 10.1016/j.bmc.2012.10.057. Epub 2012 Nov 15. Bioorg Med Chem. 2013. PMID: 23218469 Free PMC article.
A study of the structure-activity relationship of GABA(A)-benzodiazepine receptor bivalent ligands by conformational analysis with low temperature NMR and X-ray analysis.
Han D, Holger Försterling F, Li X, Deschamps JR, Parrish D, Cao H, Rallapalli S, Clayton T, Teng Y, Majumder S, Sankar S, Roth BL, Sieghart W, Furtmuller R, Rowlett JK, Weed MR, Cook JM. Han D, et al. Among authors: sieghart w. Bioorg Med Chem. 2008 Oct 1;16(19):8853-62. doi: 10.1016/j.bmc.2008.08.072. Epub 2008 Sep 2. Bioorg Med Chem. 2008. PMID: 18790643 Free PMC article.
Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models.
Rivas FM, Stables JP, Murphree L, Edwankar RV, Edwankar CR, Huang S, Jain HD, Zhou H, Majumder S, Sankar S, Roth BL, Ramerstorfer J, Furtmüller R, Sieghart W, Cook JM. Rivas FM, et al. Among authors: sieghart w. J Med Chem. 2009 Apr 9;52(7):1795-8. doi: 10.1021/jm801652d. J Med Chem. 2009. PMID: 19275170 Free PMC article.
Anxiolytic-like effects of 8-acetylene imidazobenzodiazepines in a rhesus monkey conflict procedure.
Fischer BD, Licata SC, Edwankar RV, Wang ZJ, Huang S, He X, Yu J, Zhou H, Johnson EM Jr, Cook JM, Furtmüller R, Ramerstorfer J, Sieghart W, Roth BL, Majumder S, Rowlett JK. Fischer BD, et al. Among authors: sieghart w. Neuropharmacology. 2010 Dec;59(7-8):612-8. doi: 10.1016/j.neuropharm.2010.08.011. Epub 2010 Aug 18. Neuropharmacology. 2010. PMID: 20727364 Free PMC article.
Sh-I-048A, an in vitro non-selective super-agonist at the benzodiazepine site of GABAA receptors: the approximated activation of receptor subtypes may explain behavioral effects.
Obradović ALj, Joksimović S, Poe MM, Ramerstorfer J, Varagic Z, Namjoshi O, Batinić B, Radulović T, Marković B, Roth BL, Sieghart W, Cook JM, Savić MM. Obradović ALj, et al. Among authors: sieghart w. Brain Res. 2014 Mar 20;1554:36-48. doi: 10.1016/j.brainres.2014.01.036. Epub 2014 Jan 25. Brain Res. 2014. PMID: 24472579 Free PMC article.
Design and Synthesis of Novel Deuterated Ligands Functionally Selective for the γ-Aminobutyric Acid Type A Receptor (GABAAR) α6 Subtype with Improved Metabolic Stability and Enhanced Bioavailability.
Knutson DE, Kodali R, Divović B, Treven M, Stephen MR, Zahn NM, Dobričić V, Huber AT, Meirelles MA, Verma RS, Wimmer L, Witzigmann C, Arnold LA, Chiou LC, Ernst M, Mihovilovic MD, Savić MM, Sieghart W, Cook JM. Knutson DE, et al. Among authors: sieghart w. J Med Chem. 2018 Mar 22;61(6):2422-2446. doi: 10.1021/acs.jmedchem.7b01664. Epub 2018 Mar 6. J Med Chem. 2018. PMID: 29481759 Free PMC article.
Evidence That Sedative Effects of Benzodiazepines Involve Unexpected GABAA Receptor Subtypes: Quantitative Observation Studies in Rhesus Monkeys.
Duke AN, Meng Z, Platt DM, Atack JR, Dawson GR, Reynolds DS, Tiruveedhula VVNPB, Li G, Stephen MR, Sieghart W, Cook JM, Rowlett JK. Duke AN, et al. Among authors: sieghart w. J Pharmacol Exp Ther. 2018 Jul;366(1):145-157. doi: 10.1124/jpet.118.249250. Epub 2018 May 2. J Pharmacol Exp Ther. 2018. PMID: 29720564 Free PMC article.
An updated unified pharmacophore model of the benzodiazepine binding site on gamma-aminobutyric acid(a) receptors: correlation with comparative models.
Clayton T, Chen JL, Ernst M, Richter L, Cromer BA, Morton CJ, Ng H, Kaczorowski CC, Helmstetter FJ, Furtmüller R, Ecker G, Parker MW, Sieghart W, Cook JM. Clayton T, et al. Among authors: sieghart w. Curr Med Chem. 2007;14(26):2755-75. doi: 10.2174/092986707782360097. Curr Med Chem. 2007. PMID: 18045122 Review.
369 results