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Elimination of a cholecystokinin receptor agonist 'trigger' in an effort to develop positive allosteric modulators without intrinsic agonist activity.
Desai AJ, Henke BR, Miller LJ. Desai AJ, et al. Bioorg Med Chem Lett. 2015 May 1;25(9):1849-55. doi: 10.1016/j.bmcl.2015.03.051. Epub 2015 Mar 24. Bioorg Med Chem Lett. 2015. PMID: 25862198 Free PMC article.
We have studied analogues of the 1,5-benzodiazepine agonist, GI181771X, in which the N1-isopropyl agonist 'trigger' was modified. ...
We have studied analogues of the 1,5-benzodiazepine agonist, GI181771X, in which the N1-isopropyl agonist 'trigger' was modified. ...
Species- and dose-specific pancreatic responses and progression in single- and repeat-dose studies with GI181771X: a novel cholecystokinin 1 receptor agonist in mice, rats, and monkeys.
Myer JR, Romach EH, Elangbam CS. Myer JR, et al. Toxicol Pathol. 2014 Jan;42(1):260-74. doi: 10.1177/0192623313506792. Epub 2013 Oct 31. Toxicol Pathol. 2014. PMID: 24178573
To highlight such variations, we evaluated the species- and dose-specific pancreatic responses and progression caused by GI181771X, a novel cholecystokinin 1 receptor agonist investigated by GlaxoSmithKline for the treatment of obesity. ...In contrast to rodents, pancreati …
To highlight such variations, we evaluated the species- and dose-specific pancreatic responses and progression caused by GI181771X, a …
Molecular basis for benzodiazepine agonist action at the type 1 cholecystokinin receptor.
Harikumar KG, Cawston EE, Lam PCH, Patil A, Orry A, Henke BR, Abagyan R, Christopoulos A, Sexton PM, Miller LJ. Harikumar KG, et al. J Biol Chem. 2013 Jul 19;288(29):21082-21095. doi: 10.1074/jbc.M113.480715. Epub 2013 Jun 10. J Biol Chem. 2013. PMID: 23754289 Free PMC article.
Here, we explore the molecular basis for action of a unique small molecule ligand that is a type 1 cholecystokinin (CCK) receptor agonist and type 2 CCK receptor antagonist, GI181771X. We characterize its binding utilizing structurally related radioiodinated ligands select …
Here, we explore the molecular basis for action of a unique small molecule ligand that is a type 1 cholecystokinin (CCK) receptor agonist an …
Stimulation of cholecystokinin-A receptors with GI181771X does not cause weight loss in overweight or obese patients.
Jordan J, Greenway FL, Leiter LA, Li Z, Jacobson P, Murphy K, Hill J, Kler L, Aftring RP. Jordan J, et al. Clin Pharmacol Ther. 2008 Feb;83(2):281-7. doi: 10.1038/sj.clpt.6100272. Epub 2007 Jun 27. Clin Pharmacol Ther. 2008. PMID: 17597711 Clinical Trial.
Cholecystokinin (CCK) decreases meal size through activation of CCK-A receptors on vagal afferents. We tested the hypothesis that the selective CCK-A agonist GI181771X induces weight loss in obese patients. Patients with body mass index > or = 30 or > or = 27 kg/m2 w …
Cholecystokinin (CCK) decreases meal size through activation of CCK-A receptors on vagal afferents. We tested the hypothesis that the select …
Effect of oral CCK-1 agonist GI181771X on fasting and postprandial gastric functions in healthy volunteers.
Castillo EJ, Delgado-Aros S, Camilleri M, Burton D, Stephens D, O'Connor-Semmes R, Walker A, Shachoy-Clark A, Zinsmeister AR. Castillo EJ, et al. Am J Physiol Gastrointest Liver Physiol. 2004 Aug;287(2):G363-9. doi: 10.1152/ajpgi.00074.2004. Am J Physiol Gastrointest Liver Physiol. 2004. PMID: 15246968 Free article. Clinical Trial.
CCK influences satiation and gastric and gallbladder emptying. GI181771X is a novel oral CCK-1 agonist; its effects on gastric emptying of solids, accommodation, and postprandial symptoms are unclear. ...Adverse effects and safety were monitored. There were overall group e …
CCK influences satiation and gastric and gallbladder emptying. GI181771X is a novel oral CCK-1 agonist; its effects on gastric emptyi …