YM022 is a very potent, selective antagonist of the gastrin/cholecystokinin (CCK)-B receptor.
YM022 is a very potent, selective antagonist of the gastrin/cholecystokinin (CCK)-B receptor. The Ki value for CCKB is 68 pM vs 63 nM for CCKA. In rats, YM022 inhibits pentagastrin-induced gastric emptying with an ED50 or 7.8 nM/kg.
The Journal of biological chemistry, 280(39), 33368-33373 (2005-08-05)
The third intracellular loop domain of G protein-coupled receptors regulates their desensitization, internalization, and resensitization. Colorectal and pancreatic cancers, but not the nonmalignant tissue, express a splice variant of the cholecystokinin 2 receptor (CCK2R) called CCK(2i4sv)R that, because of intron
Gastrin acts via cholecystokinin-B/gastrin receptors to control histamine- and chromogranin A-producing ECL cells, which constitute the quantitatively predominant endocrine cell population in the acid-producing part of the rat stomach. Cholecystokinin-B receptor blockade is known to suppress the activity of ECL
Mechanisms by which premalignant Barrett's metaplasia (BM) progresses to esophageal adenocarcinoma are currently being sought. This study investigated the role played by the polypeptide hormone gastrin, specifically its antiapoptotic effects through activation of protein kinase B/Akt (PKB/Akt). In esophageal cell
Rat stomach ECL cells are rich in histamine and chromogranin A-derived peptides, such as pancreastatin. Gastrin causes the parietal cells to secrete acid by flooding them with histamine from the ECL cells. In the past, gastric histamine release has been
Gastrin has a growth-promoting effect on the oxyntic mucosa of the stomach but has been claimed also to affect other parts of the gastrointestinal tract and pancreas. This report describes the effects of the cholecystokinin, (CCK2) receptor antagonists YM022 and
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