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- W2003998900 abstract "Gastrin-recognizing CCK2 receptors are expressed in parietal cells and in so-called ECL cells in the acid-producing part of the stomach. ECL cells are endocrine/paracrine cells that produce and store histamine and chromogranin A (CGA)-derived peptides, such as pancreastatin. The ECL cells are the principal cellular transducer of the gastrin-acid signal. Activation of the CCK2 receptor results in mobilization of histamine (and pancreastatin) from the ECL cells with consequent activation of the parietal cell histamine H2 receptor. Thus, release of ECL-cell histamine is a key event in the process of gastrin-stimulated acid secretion. The oxyntic mucosal histidine decarboxylase (HDC) activity and the serum pancreastatin concentration are useful markers for the activity of the gastrin-ECL cell axis. Powerful and selective CCK2 receptor antagonits have been developed from a series of benzodiazepine compounds. These agents are useful tools to study how gastrin controls the ECL cells. Conversely, the close control of ECL cells by gastrin makes the gastrin-ECL cell axis well suited for evaluating the antagonistic potential of CCK2 receptor antagonists with the ECL-cell HDC activity as a notably sensitive and reliable parameter. The CCK2 receptor antagonists YF476, YM022, RP73870, JB93182 and AG041R were found to cause prompt inhibition of ECL-cell histamine and pancreastatin secretion and synthesis. The circulating pancreastatin concentration is raised, was lowered when the action of gastrin on the ECL cells was blocked by the CCK2 receptor antagonists. These effects were associated with inhition of gastrin-stimulated acid secretion. In addition, sustained receptor blockade was manifested in permanently decreased oxyntic mucosal HDC activity, histamine concentration and HDC mRNA and CGA mRNA concentrations. CCK2 receptor blockade also induced hypergastrinemia, which probably reflects the impaired gastric acid secretion (no acid feedback inhibition of gastrin release). Upon withdrawal of the CCK2 receptor antagonists, their effects on the ECL cells were readily reversible. In conclusion, gastrin mobilizes histamine from the ECL cells, thereby provoking the parietal cells to secrete acid. While CCK2 receptor blockade prevents gastrin from evoking acid secretion, it is without effect on basal and vagally stimulated acid secretion. We conclude that specific and potent CCK2 receptor antagonists represent powerful tools to explore the functional significance of the ECL cells." @default.
- W2003998900 created "2016-06-24" @default.
- W2003998900 creator A5012601095 @default.
- W2003998900 creator A5018953314 @default.
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- W2003998900 date "1999-03-01" @default.
- W2003998900 modified "2023-10-17" @default.
- W2003998900 title "CCK2 receptor antagonists: pharmacological tools to study the gastrin–ECL cell-parietal cell axis" @default.
- W2003998900 cites W126815498 @default.
- W2003998900 cites W1562288220 @default.
- W2003998900 cites W1587968290 @default.
- W2003998900 cites W1594704683 @default.
- W2003998900 cites W1849557368 @default.
- W2003998900 cites W1954221632 @default.
- W2003998900 cites W1958401509 @default.
- W2003998900 cites W1962139363 @default.
- W2003998900 cites W1965260950 @default.
- W2003998900 cites W1967079036 @default.
- W2003998900 cites W1967273790 @default.
- W2003998900 cites W1975216061 @default.
- W2003998900 cites W1975689335 @default.
- W2003998900 cites W1979100850 @default.
- W2003998900 cites W1982249220 @default.
- W2003998900 cites W1982319667 @default.
- W2003998900 cites W1983493986 @default.
- W2003998900 cites W1984550271 @default.
- W2003998900 cites W1984552889 @default.
- W2003998900 cites W1985363141 @default.
- W2003998900 cites W1986832734 @default.
- W2003998900 cites W1988646125 @default.
- W2003998900 cites W1991517152 @default.
- W2003998900 cites W1992087641 @default.
- W2003998900 cites W1995388074 @default.
- W2003998900 cites W1995959790 @default.
- W2003998900 cites W1996402824 @default.
- W2003998900 cites W1996627742 @default.
- W2003998900 cites W1996960148 @default.
- W2003998900 cites W2000604473 @default.
- W2003998900 cites W2002658312 @default.
- W2003998900 cites W2004295964 @default.
- W2003998900 cites W2008961630 @default.
- W2003998900 cites W2009289013 @default.
- W2003998900 cites W2012071259 @default.
- W2003998900 cites W2013501509 @default.
- W2003998900 cites W2013538870 @default.
- W2003998900 cites W2020946796 @default.
- W2003998900 cites W2021857921 @default.
- W2003998900 cites W2024476894 @default.
- W2003998900 cites W2024691708 @default.
- W2003998900 cites W2026480824 @default.
- W2003998900 cites W2027055988 @default.
- W2003998900 cites W2027119507 @default.
- W2003998900 cites W2029944031 @default.
- W2003998900 cites W2029959432 @default.
- W2003998900 cites W203119193 @default.
- W2003998900 cites W2032042210 @default.
- W2003998900 cites W2036414165 @default.
- W2003998900 cites W2036661477 @default.
- W2003998900 cites W2038279061 @default.
- W2003998900 cites W2038402088 @default.
- W2003998900 cites W2044589560 @default.
- W2003998900 cites W2053192907 @default.
- W2003998900 cites W2054009022 @default.
- W2003998900 cites W2056340255 @default.
- W2003998900 cites W2056764782 @default.
- W2003998900 cites W2056862273 @default.
- W2003998900 cites W2062769140 @default.
- W2003998900 cites W2066806375 @default.
- W2003998900 cites W2066944012 @default.
- W2003998900 cites W2068270752 @default.
- W2003998900 cites W2068591738 @default.
- W2003998900 cites W2068752736 @default.
- W2003998900 cites W2068917080 @default.
- W2003998900 cites W2071881271 @default.
- W2003998900 cites W2082476467 @default.
- W2003998900 cites W2089227275 @default.
- W2003998900 cites W2091211165 @default.
- W2003998900 cites W2091825425 @default.
- W2003998900 cites W2093800476 @default.
- W2003998900 cites W2094020906 @default.
- W2003998900 cites W2095297219 @default.
- W2003998900 cites W2099611610 @default.
- W2003998900 cites W2128883674 @default.
- W2003998900 cites W2130241523 @default.
- W2003998900 cites W2143390390 @default.
- W2003998900 cites W2159870483 @default.
- W2003998900 cites W2160896806 @default.
- W2003998900 cites W2163549442 @default.
- W2003998900 cites W2396947151 @default.
- W2003998900 cites W2463898543 @default.
- W2003998900 cites W2886800621 @default.
- W2003998900 cites W327545536 @default.
- W2003998900 cites W4205738382 @default.
- W2003998900 cites W4233414125 @default.
- W2003998900 cites W4236372037 @default.
- W2003998900 cites W4296759708 @default.
- W2003998900 cites W4322701877 @default.