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Research Article

Mitigation of opioid off-target effects and identification of structural drivers of opioid receptor engagement for BACE-1 small molecule inhibitors

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Pages 478-486 | Received 20 May 2015, Accepted 23 Jun 2015, Published online: 14 Aug 2015

References

  • CDER, U.S. Department of Health and Human Services Food and Drug Administration Center for Drug Evaluation and Research (CDER). Assessment of abuse potential of drugs. Draft guidance; 2010
  • Granier S, Manglik A, Kruse AC, et al. (2012). Structure of the delta-opioid receptor bound to naltrindole. Nature 485:400–4
  • Grider JR, Makhlouf GM. (1987). Role of opioid neurons in the regulation of intestinal peristalsis. Am J Physiol 253:G226–31
  • Halgren TA. (1996). Merck molecular force field. I. Basis, form, scope, parameterization, and performance of MMFF 94. J Comput Chem 17:490–519
  • Hanwell MD, Curtis DE, Lonie DC, et al. (2012). Avogadro: an advanced semantic chemical editor, visualization, and analysis platform. J Cheminf 4:17
  • Hayashida M, Fukunaga A, Hanaoka K. (2003). Detection of acute tolerance to the analgesic and nonanalgesic effects of remifentanil infusion in a rabbit model. Anesth Analg 97:1347–52
  • Hunt KW, Cook AW, Watts RJ, et al. (2013). Spirocyclic beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloid beta in a higher species. J Med Chem 56:3379–403
  • Konturek SJ. (1980). Opiates and the gastrointestinal tract. Am J Gastroenterol 74:285–91
  • Leander JD. (1984). Effects of full and partial kappa agonists and mu agonists on urine output of normally hydrated rats. Neuropeptides 5:283–6
  • Manara L, Bianchetti A. (1985). The central and peripheral influences of opioids on gastrointestinal propulsion. Annu Rev Pharmacol Toxicol 25:249–73
  • Manglik A, Kruse AC, Kobilka TS, et al. (2012). Crystal structure of the micro-opioid receptor bound to a morphinan antagonist. Nature 485:321–6
  • Nimmo WS, Heading RC, Wilson J, et al. (1975). Inhibition of gastric emptying and drug absorption by narcotic analgesics. Br J Clin Pharmacol 2:509–13
  • Pogozheva ID, Lomize AL, Mosberg HI. (1998). Opioid receptor three-dimensional structures from distance geometry calculations with hydrogen bonding constraints. Biophys J 75:612–34
  • Tan-No K, Niijima F, Nakagawasai O, et al. (2003). Development of tolerance to the inhibitory effect of loperamide on gastrointestinal transit in mice. Eur J Pharm Sci: Off J Eur Fed Pharmaceut Sci 20:357–63
  • Thomas AA, Hunt KW, Volgraf M, et al. (2014). Discovery of 7-tetrahydropyran-2-yl chromans: beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid beta-protein (Abeta) in the central nervous system. J Med Chem 57:878–902
  • Trott O, Olson AJ. (2010). AutoDock Vina: improving the speed and accuracy of docking with a new scoring function, efficient optimization, and multithreading. J Comput Chem 31:455–61
  • Wu H, Wacker D, Mileni M, et al. (2012). Structure of the human kappa-opioid receptor in complex with JDTic. Nature 485:327–32

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