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Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of obesity.
Elliott RL, Cameron KO, Chin JE, Bartlett JA, Beretta EE, Chen Y, Jardine Pda S, Dubins JS, Gillaspy ML, Hargrove DM, Kalgutkar AS, LaFlamme JA, Lame ME, Martin KA, Maurer TS, Nardone NA, Oliver RM, Scott DO, Sun D, Swick AG, Trebino CE, Zhang Y. Elliott RL, et al. Among authors: dubins js. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6797-801. doi: 10.1016/j.bmcl.2010.08.115. Epub 2010 Sep 28. Bioorg Med Chem Lett. 2010. PMID: 20851601
Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor.
Kung DW, Coffey SB, Jones RM, Cabral S, Jiao W, Fichtner M, Carpino PA, Rose CR, Hank RF, Lopaze MG, Swartz R, Chen HT, Hendsch Z, Posner B, Wielis CF, Manning B, Dubins J, Stock IA, Varma S, Campbell M, DeBartola D, Kosa-Maines R, Steyn SJ, McClure KF. Kung DW, et al. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4281-7. doi: 10.1016/j.bmcl.2012.05.024. Epub 2012 May 17. Bioorg Med Chem Lett. 2012. PMID: 22677316
AdipoR1 and 2 are expressed on warm sensitive neurons of the hypothalamic preoptic area and contribute to central hyperthermic effects of adiponectin.
Klein I, Sanchez-Alavez M, Tabarean I, Schaefer J, Holmberg KH, Klaus J, Xia F, Marcondes MC, Dubins JS, Morrison B, Zhukov V, Sanchez-Gonzalez A, Mitsukawa K, Hadcock JR, Bartfai T, Conti B. Klein I, et al. Among authors: dubins js. Brain Res. 2011 Nov 14;1423:1-9. doi: 10.1016/j.brainres.2011.09.019. Epub 2011 Sep 17. Brain Res. 2011. PMID: 22000082 Free PMC article.
Insulin causes hyperthermia by direct inhibition of warm-sensitive neurons.
Sanchez-Alavez M, Tabarean IV, Osborn O, Mitsukawa K, Schaefer J, Dubins J, Holmberg KH, Klein I, Klaus J, Gomez LF, Kolb H, Secrest J, Jochems J, Myashiro K, Buckley P, Hadcock JR, Eberwine J, Conti B, Bartfai T. Sanchez-Alavez M, et al. Diabetes. 2010 Jan;59(1):43-50. doi: 10.2337/db09-1128. Epub 2009 Oct 21. Diabetes. 2010. PMID: 19846801 Free PMC article.
15 results