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Identification of a dual δ OR antagonist/μ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d).
Breslin HJ, Diamond CJ, Kavash RW, Cai C, Dyatkin AB, Miskowski TA, Zhang SP, Wade PR, Hornby PJ, He W. Breslin HJ, et al. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4869-72. doi: 10.1016/j.bmcl.2012.05.042. Epub 2012 May 24. Bioorg Med Chem Lett. 2012. PMID: 22695132
Synthesis and biological evaluation of benzocyclobutane-C-glycosides as potent and orally active SGLT1/SGLT2 dual inhibitors.
Kuo GH, Gaul MD, Liang Y, Xu JZ, Du F, Hornby P, Xu G, Qi J, Wallace N, Lee S, Grant E, Murray WV, Demarest K. Kuo GH, et al. Bioorg Med Chem Lett. 2018 Apr 15;28(7):1182-1187. doi: 10.1016/j.bmcl.2018.02.057. Epub 2018 Mar 1. Bioorg Med Chem Lett. 2018. PMID: 29523385
Identification of potent phenyl imidazoles as opioid receptor agonists.
Breslin HJ, Cai C, Miskowski TA, Coutinho SV, Zhang SP, Hornby P, He W. Breslin HJ, et al. Bioorg Med Chem Lett. 2006 May 1;16(9):2505-8. doi: 10.1016/j.bmcl.2006.01.082. Epub 2006 Feb 17. Bioorg Med Chem Lett. 2006. PMID: 16483774
Triazinediones as prokineticin 1 receptor antagonists. Part 1: SAR, synthesis and biological evaluation.
Ralbovsky JL, Lisko JG, Palmer JM, Mabus J, Chevalier KM, Schulz MJ, Dyatkin AB, Miskowski TA, Coats SJ, Hornby P, He W. Ralbovsky JL, et al. Bioorg Med Chem Lett. 2009 May 15;19(10):2661-3. doi: 10.1016/j.bmcl.2009.03.157. Epub 2009 Apr 5. Bioorg Med Chem Lett. 2009. PMID: 19375913
Modulation of gastrointestinal function by MuDelta, a mixed µ opioid receptor agonist/ µ opioid receptor antagonist.
Wade PR, Palmer JM, McKenney S, Kenigs V, Chevalier K, Moore BA, Mabus JR, Saunders PR, Wallace NH, Schneider CR, Kimball ES, Breslin HJ, He W, Hornby PJ. Wade PR, et al. Br J Pharmacol. 2012 Nov;167(5):1111-25. doi: 10.1111/j.1476-5381.2012.02068.x. Br J Pharmacol. 2012. PMID: 22671931 Free PMC article.
Acute colitis induction by oil of mustard results in later development of an IBS-like accelerated upper GI transit in mice.
Kimball ES, Palmer JM, D'Andrea MR, Hornby PJ, Wade PR. Kimball ES, et al. Am J Physiol Gastrointest Liver Physiol. 2005 Jun;288(6):G1266-73. doi: 10.1152/ajpgi.00444.2004. Epub 2005 Feb 3. Am J Physiol Gastrointest Liver Physiol. 2005. PMID: 15691868
Aza-bicyclic amino acid sulfonamides as alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists.
Dyatkin AB, Hoekstra WJ, Kinney WA, Kontoyianni M, Santulli RJ, Kimball ES, Fisher MC, Prouty SM, Abraham WM, de Garavilla L, Andrade-Gordon P, Hlasta DJ, He W, Hornby PJ, Damiano BP, Maryanoff BE. Dyatkin AB, et al. Bioorg Med Chem Lett. 2004 Feb 9;14(3):591-6. doi: 10.1016/j.bmcl.2003.11.063. Bioorg Med Chem Lett. 2004. PMID: 14741249
Aza-bicyclic amino acid carboxamides as alpha4beta1/alpha4beta7 integrin receptor antagonists.
Dyatkin AB, Gong Y, Miskowski TA, Kimball ES, Prouty SM, Fisher MC, Santulli RJ, Schneider CR, Wallace NH, Hornby PJ, Diamond C, Kinney WA, Maryanoff BE, Damiano BP, He W. Dyatkin AB, et al. Bioorg Med Chem. 2005 Dec 15;13(24):6693-702. doi: 10.1016/j.bmc.2005.07.022. Epub 2005 Aug 19. Bioorg Med Chem. 2005. PMID: 16112583
Small intestinal cannabinoid receptor changes following a single colonic insult with oil of mustard in mice.
Kimball ES, Wallace NH, Schneider CR, D'Andrea MR, Hornby PJ. Kimball ES, et al. Front Pharmacol. 2010 Nov 19;1:132. doi: 10.3389/fphar.2010.00132. eCollection 2010. Front Pharmacol. 2010. PMID: 21779244 Free PMC article.
Synthesis and biological evaluation of novel pyridazinone-based alpha4 integrin receptor antagonists.
Gong Y, Barbay JK, Dyatkin AB, Miskowski TA, Kimball ES, Prouty SM, Fisher MC, Santulli RJ, Schneider CR, Wallace NH, Ballentine SA, Hageman WE, Masucci JA, Maryanoff BE, Damiano BP, Andrade-Gordon P, Hlasta DJ, Hornby PJ, He W. Gong Y, et al. J Med Chem. 2006 Jun 1;49(11):3402-11. doi: 10.1021/jm060031q. J Med Chem. 2006. PMID: 16722660
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