Cholecystokinin type B receptor antagonist PD-136,450 is a partial secretory agonist in the stomach and a full agonist in the pancreas of the rat. Gastrin (cholecystokinin type B (CCK-B)) receptor antagonists may help to elucidate the physiological role of gastrin, have therapeutic potential as acid antisecretory drugs, and may be of use as adjuvant therapy for gastrin sensitive tumours. The agonist effect of PD-136,450 is mediated via interaction with the gastrin (CCK-B) receptor in the stomach and the CCK-A receptor in the pancreas. References: Chandranath SI, Bastaki SM, D'Souza A, Adem A, Singh J. Attenuation of stress-induced gastric lesions by lansoprazole, PD-136450 and ranitidine in rats. Mol Cell Biochem. 2011 Mar;349(1-2):205-12. doi: 10.1007/s11010-010-0675-3. Epub 2010 Nov 30. PubMed PMID: 21116686. 2: Chandranath SI, Bastaki SM, Singh J. A comparative study on the activity of lansoprazole, omeprazole and PD-136450 on acidified ethanol- and indomethacin-induced gastric lesions in the rat. Clin Exp Pharmacol Physiol. 2002 Mar;29(3):173-80. PubMed PMID: 11906479. 3: Koop I, Eissele R, Richter S, Patberg H, Meyer F, Mossner J, Arnold R, Koop H. A new CCK-B/gastrin receptor antagonist acts as an agonist on the rat pancreas. Int J Pancreatol. 1994 Jun;15(3):215-22. PubMed PMID: 7523549. 4: Eissele R, Koop H, Bothe-Sandfort E, Arnold R. Effect of gastrin receptor antagonists on gastric acid secretion and gastrin and somatostatin release in the rat stomach. Digestion. 1992;53(3-4):179-88. PubMed PMID: 1363320. 5: Eissele R, Patberg H, Koop H, Krack W, Lorenz W, McKnight AT, Arnold R. Effect of gastrin receptor blockade on endocrine cells in rats during achlorhydria. Gastroenterology. 1992 Nov;103(5):1596-601. PubMed PMID: 1426880. 6: Hayward NJ, Harding M, Lloyd SA, McKnight AT, Hughes J, Woodruff GN. The effect of CCKB/gastrin antagonists on stimulated gastric acid secretion in the anaesthetized rat. Br J Pharmacol. 1991 Dec;104(4):973-7. PubMed PMID: 1687371; PubMed Central PMCID: PMC1908834. 7: Ding XQ, Chen D, Hakanson R. Cholecystokinin-B receptor ligands of the dipeptoid series act as agonists on rat stomach histidine decarboxylase. Gastroenterology. 1995 Oct;109(4):1181-7. PubMed PMID: 7557084. 8: Blevins GT Jr, van de Westerlo EM, Yule DI, Williams JA. Characterization of cholecystokininA receptor agonist activity by a family of cholecystokininB receptor antagonists. J Pharmacol Exp Ther. 1994 Jun;269(3):911-6. PubMed PMID: 7516969. 9: Bastaki SM, Hasan MY, Chandranath SI, Schmassmann A, Garner A. PD-136,450: a CCK2 (gastrin) receptor antagonist with antisecretory, anxiolytic and antiulcer activity. Mol Cell Biochem. 2003 Oct;252(1-2):83-90. PubMed PMID: 14577579. 10: Beinborn M, Chen C, DeMeo L, McBride EW, Kopin AS. Small synthetic ligands of the cholecystokinin-B/gastrin receptor can mimic the function of endogenous peptide hormones. Yale J Biol Med. 1998 May-Aug;71(3-4):337-46. PubMed PMID: 10461364; PubMed Central PMCID: PMC2578980. 1 Hughes J, Dockray GJ, Hill D, Garcia L, Pritchard MC, Forster E, Toescu E, Woodruff G, Horwell DC. Characterization of novel peptoid agonists for the CCK-A receptor. Regul Pept. 1996 Aug 27;65(1):15-21. PubMed PMID: 8876031. 12: Simon B, Eissele R, Czornik M, Swarovsky B, Arnold R. Effect of gastrin receptor blockade on gastrin and histidine decarboxylase gene expression in rats during achlorhydria. Scand J Gastroenterol. 1995 Jun;30(6):503-10. PubMed PMID: 7569754. 13: Schmassmann A, Garner A, Flogerzi B, Hasan MY, Sanner M, Varga L, Halter F. Cholecystokinin type B receptor antagonist PD-136,450 is a partial secretory agonist in the stomach and a full agonist in the pancreas of the rat. Gut. 1994 Feb;35(2):270-4. PubMed PMID: 8307482; PubMed Central PMCID: PMC1374507. 14: Lindstrom E, Bjorkqvist M, Hakanson R. Pharmacological analysis of CCK2 receptor antagonists using isolated rat stomach ECL cells. Br J Pharmacol. 1999 May;127(2):530-6. PubMed PMID: 10385255; PubMed Central PMCID: PMC1566020.

纯度：≥98%

CAS：139067-52-0