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Query: UNIPROT:P01350 (gastrin)
 9,683 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Gastric antisecretory effect of a new histamine H2-receptor antagonist, N"-cyano-N-methyl-N'-[2-T5-methyl-imidazol-4-yl)-methylthioethyl]guanidine (cimetidine), was studied in isolated bullfrog gastric mucosa and in anesthetized young chicken preparation with acute gastric fistulae. Cimetidine inhibited dose-dependently the secretory responses of frog gastric mucosa to histamine, and parallel shift of the concentration-response curve of histamine by cimetidine indicated the competitive character of the antagonism. However, cimetidine inhibited the stimulatory action of methacholine and gastrin as well as histamine on gastric secretion. Cimetidine pretreatment protected the histamine sensitivity of gastric mucosa from the irreversible blocking action of dibenamine. It was also found in the chicken preparation that cimetidine strongly depressed the maximal acid secretory response to histamine as well as to tetragastrin or methacholine. These results may afford the evidence indicating the specific action of cimetidine and the involvement of histamine-related mechanism in the action of the other two secretagogues.
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PMID:Inhibitory effect of cimetidine, an antagonist of histamine H2-receptor, on gastric acid secretion in isolated frog stomach and in anesthetized young chicken. 31 97

Sigma receptor involvement in the oxyntic mechanism of gastric parietal cells was investigated using isolated guinea pig parietal cells. Using the 14C-aminopyrine accumulation method, di(orthotolyl)guanidine (DTG), a sigma receptor agonist, demonstrated peak stimulation of acid production at a concentration of 5 x 10(-5) M. The DTG-induced stimulatory effect on 14C-aminopyrine accumulation in preparations enriched in parietal cells was inhibited by haloperidol, a DTG inhibitor, and omeprazole, a proton pump inhibitor, in a concentration-dependent manner. Assessment of the interaction between DTG and agonists for histamine, gastrin, and muscarine receptors demonstrated a potentiating interaction effect on acid production only when parietal cells were exposed to both DTG and histamine. A receptor-binding assay using 3H-DTG revealed two sigma receptor subtypes, sigma 1 and sigma 2, on the crude membranes of parietal cells. There was a direct relationship between DTG dose and intracellular Ca2+ concentration, but there was no change in intracellular cyclic adenosine 5'-monophosphate (cAMP) concentration when parietal cells were exposed to DTG. These results demonstrate that sigma receptors exist on guinea pig gastric parietal cells and suggest that they play a role in acid production via an increase in intracellular Ca2+ concentration.
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PMID:Roles of sigma receptors in isolated guinea pig parietal cells. 895 68

A novel series of potent and selective non-peptide neuropeptide Y (NPY) Y1 receptor antagonists, having benzazepine nuclei, have been designed, synthesized, and evaluated for activity. Chemical modification of the R(1) and R(3) substituents in structure 1 (Chart 1) yields several compounds that show high affinity for the Y1 receptor (K(i) values of less than 10 nM). SAR studies revealed that introduction of an isopropylurea group at R(1) and a 3-(benzo-condensed-urea) group, 3-(fluorophenylurea) group, or a 3-(N-(4-hydroxyphenyl)guanidine) group at R(3) in structure 1 afforded potent and subtype-selective NPY Y1 receptor antagonists. 3-(3-(Benzothiazol-6-yl)ureido)-1-N-(3-(N'-(3-isopropylureido++ +))benzyl )-2,3,4,5-tetrahydro-1H-1-benzazepin-2-one (21), which was one of the most potent derivatives, competitively inhibited specific [(125)I]peptide YY (PYY) binding to Y1 receptors in human neuroblastoma SK-N-MC cells (K(i) = 5.1 nM). 21 not only inhibited the Y1 receptor-mediated increase in cytosolic free Ca(2+) concentration in SK-N-MC cells but also antagonized the Y1 receptor-mediated inhibitory effect of peptide YY on gastrin-induced histamine release in rat enterochromaffin-like cells. 21 showed no significant affinity in 17 receptor binding assays including Y2, Y4, and Y5 receptors.
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PMID:1,3-Disubstituted benzazepines as novel, potent, selective neuropeptide Y Y1 receptor antagonists. 1041 82