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Drug
Enzyme
Compound
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Target Concepts:
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Query: UNIPROT:P01350 (
gastrin
)
9,683
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
The functional role of the cholinergic nervous system in regulating
gastrin
release was investigated using enriched canine antral G cells.
Gastrin
content was 30.1 +/- 2.9 pmol per well and basal
gastrin
release was 900 +/- 27 fmol per well (n = 45). Carbachol (10(-8) to 10(-5) M) dose-dependently stimulated
gastrin
release with a maximal stimulatory response achieved at a concentration of 10(-5) M (330% over basal). To characterize the muscarinic receptor which mediates
gastrin
release from antral G cells, we examined the effect of three muscarinic receptor antagonists on carbachol-stimulated
gastrin
release; atropine (nonselective muscarinic receptor antagonist), pirenzepine (M1 muscarinic receptor antagonist) and 4-DAMP (
M3 muscarinic receptor
antagonist). Atropine (10(-9) to 10(-6) M), pirenzepine (10(-8) to 10(-5) M) and 4-DAMP (10(-9) to 10(-6) M) had no effect on the basal
gastrin
release. However, carbachol (10(-5) M)-stimulated
gastrin
release was effectively inhibited by atropine and 4-DAMP with Ki values of 0.48 and 0.66 nM, respectively. Pirenzepine at a high concentration (10(-5) M) also inhibited carbachol-stimulated
gastrin
release with a Ki value of 46.3 nM. These results suggest that the cholinergic nervous system directly stimulates
gastrin
release via M3 muscarinic receptors located on antral G cells.
...
PMID:Muscarinic M3 receptor-mediated release of gastrin from canine antral G cells in primary culture. 789 29