Regulation by vasoactive intestinal peptide of cyclic amp accumulation in gastric epithelial glands

Dupont, Christophe; Gespach, Christian; Chenut, Bernard; Rosselin, G

doi:10.1016/0014-5793(80)80486-8

Cited by 42 publications

(7 citation statements)

References 11 publications

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“…As shown in Fig. 2, the HZ receptor antagonist In contrast, famotidine has no action on other effectors of the adenylate cyclase system in human fundic membranes, including forskolin and membrane receptors sensitive to isoproterenol &-type adrenergic receptor), PGEz and vasoactive intestinal peptide VIP [8,25,27,36,371.…”

Section: Receptor Specijicity Of Famotidine Antagonismmentioning

confidence: 96%

Pharmacological control of the human gastric histamine H2 receptor by famotidine: comparison with H₁, H₂ and H₃ receptor agonists and antagonists

Gespach

Fagot

Emami

1989

Eur J Clin Investigation

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Histamine 0.1 microM-0.1 mM increased adenylate cyclase activity five- to ten-fold in human fundic membranes, with a potency Ka = 3 microM. The histamine dose-response curve was mimicked by the H3 receptor agonist (R) alpha-MeHA, but at 100 times lower potency, Ka = 0.3 mM. Histamine-induced adenylate cyclase activation was abolished by H2, H1 and H3 receptor antagonists, according to the following order of potency IC50: famotidine (0.3 microM) greater than triprolidine (0.1 mM) thioperamide (2 mM), respectively. Famotidine has no action on membrane components activating the adenylate cyclase system, including the Gs subunit of the enzyme stimulated by forskolin and cell surface receptors sensitive to isoproterenol (beta 2-type), PGE2 and VIP. The Schild plot was linear for famotidine (P less than 0.01) with a regression coefficient r = 0.678. The slope of the regression line was 0.64 and differs from unity. Accordingly, famotidine showed a slow onset of inhibition and dissociation from the H2 receptor in human cancerous HGT-1 cells. The results demonstrate that famotidine is a potent and selective H2 receptor antagonist with uncompetitive actions in human gastric mucosa. Consequently, famotidine might be a suitable drug with long-lasting actions in the treatment of Zollinger-Ellison syndrome. The results also confirm and extend the previous observations that (R) alpha-MeHA and thioperamide are two selective ligands at histamine H3 receptor sites. In the human gastric mucosa, these drugs are respectively 330 and 6700 times less potent than histamine and famotidine on the adenylate cyclase system. The possible involvement of histamine H3 receptors in the regulation of gastric secretion is proposed.

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Section: Receptor Specijicity Of Famotidine Antagonismmentioning

confidence: 96%

Pharmacological control of the human gastric histamine H2 receptor by famotidine: comparison with H₁, H₂ and H₃ receptor agonists and antagonists

Gespach

Fagot

Emami

1989

Eur J Clin Investigation

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“…42 both species the studies, carried out on homogenates of mucosal samples, concluded to the presence of a gastric beta adrenergic receptor [4,6,71. The present study was designed to take advantage of a preparation of pure human fundic and antral epithelial glands, (1) to characterize the pharmacological properties of the beta adrenoreceptor, (2) to compare the effect of catecholamines to that of the other substances controlling cyclic AMP production in human gastric epithelial cells, i.e. VIP and histamine, (3) to test the effect of somatostatin, a well known inhibitor of gastric acid secretion, on the beta adrenergic cyclic AMP regulating system.…”

Section: Introductionmentioning

confidence: 99%

Beta‐adrenergic regulation of cyclic adenosine 3‘,5’ monophosphate accumulation in human gastric epithelial glands. Inhibitory effect of somatostatin

Boige

Dupont

Chenut

et al. 1984

Eur J Clin Investigation

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The action of catecholamines and somatostatin on cyclic adenosine 3',5' monophosphate (cyclic AMP) formation in human isolated gastric glands is reported. We show that: (1) there is a beta 2 receptor-mediated stimulation of cyclic AMP production in fundus. Catecholamines act with the order of potencies isoproterenol (ED50 = 50 nmol 1(-1) greater than epinephrine (ED50 = 0.1 mumol 1(-1] greater than norepinephrine (ED50 = 5 mumol 1(-1]. Their action is completely reversed by propranolol at doses 10(3) times lower than practolol, while unaffected by phentolamine; (2) isoproterenol and Vasoactive Intestinal Peptide (VIP) have additive effects on cyclic AMP in fundic glands whereas no additivity is observed between histamine and isoproterenol; this, together with the absence of catecholamine effect in antral glands, suggests that the beta 2 receptor is located on parietal cells; (3) somatostatin (1 mumol 1(-1] non-competitively inhibits the stimulation by catecholamines but does not affect VIP and histamine stimulations. These results suggest a physiological stimulatory effect of catecholamines on gastric acid secretion in man, through a beta 2 receptor coupled to the cyclic AMP system, regulated by somatostatin.

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“…The cell yield obtained by our method was 2-fold higher than that of Ruoff et al [6], who first described the correlation between cell number and biopsy weight. Cy clic AMP levels were very similar to those in human gastric glands obtained from sections of subtotal gastrectomy [10], Half-maximal cyclic AMP production was found at 35 ± 25 pmol/1 histamine in the absence and presence of IBMX, indicating that phosphodiesterase inhibition does not alter the potency of hista mine. The H2 receptor antagonists used in this study inhibited stimulated cyclic AMP production in the same range as it had been described in previous studies with gastric mucosa from guinea pig or human resections [15,16]: the order of potency was famotidine > ranitidine > cimetidine.…”

Section: Discussionmentioning

confidence: 52%

“…(3) Only a 2-fold stimulation of adenylate cyclase activity could be obtained by 100 pmol/l histamine [5,9]. On the other hand, measurements of cyclic AMP production in human gastric mucosal cells have been per formed in gastric glands obtained from sec tions of subtotal gastrectomy [ 10], The aim of the present study was to develop a simple method for studies on cyclic AMP-mediated regulatory processes such as gastric secretion by measuring the production of intracellular cyclic AMP in isolated gastric mucosal cells. In order to set up a more physiological in vitro test system, gastric mucosal cells were isolated from human biopsy samples, which are better available than material from re sected stomachs.…”

Section: Introductionmentioning

confidence: 99%

A Method to Assess Histamine-Induced Cyclic AMP Production in Isolated Gastric Mucosal Cells from Human Biopsies

Sarem-Aslani¹,

Ratge²,

Bigge³

et al. 1991

Pharmacology

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Human gastric mucosal cells were isolated by digestion of fundic biopsies with pronase and collagenase. The mean value of gastric cells per milligram biopsy specimen ± SEM was 59,000 ± 4,300 (n = 31) with a viability of 90 ± 5 %. With the cell yield of 1 patient a series of approximately 70 – 80 cyclic AMP measurements was possible. Histamine stimulated intracellular cyclic AMP production with an EC50 value of 35 ± 25 μmol/l (SEM; n = 4). In the presence of 100 μmol/l histamine the Ki values (μmol/l) for the histamine H2 receptor antagonists averaged 1.45 (cimetidine), 0.10 (ranitidine), and 0.02 (famotidine). No significant inhibition of histamine-induced cyclic AMP production was obtained with the histamine H₁ receptor antagonist triprolidine. With the new method histamine-induced cyclic AMP production can be measured in intact human gastric mucosal cells from fundic biopsy samples.

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Regulation by vasoactive intestinal peptide of cyclic amp accumulation in gastric epithelial glands

Cited by 42 publications

References 11 publications

Pharmacological control of the human gastric histamine H2 receptor by famotidine: comparison with H₁, H₂ and H₃ receptor agonists and antagonists

Pharmacological control of the human gastric histamine H2 receptor by famotidine: comparison with H₁, H₂ and H₃ receptor agonists and antagonists

Beta‐adrenergic regulation of cyclic adenosine 3‘,5’ monophosphate accumulation in human gastric epithelial glands. Inhibitory effect of somatostatin

A Method to Assess Histamine-Induced Cyclic AMP Production in Isolated Gastric Mucosal Cells from Human Biopsies

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Regulation by vasoactive intestinal peptide of cyclic amp accumulation in gastric epithelial glands

Cited by 42 publications

References 11 publications

Pharmacological control of the human gastric histamine H2 receptor by famotidine: comparison with H1, H2 and H3 receptor agonists and antagonists

Pharmacological control of the human gastric histamine H2 receptor by famotidine: comparison with H1, H2 and H3 receptor agonists and antagonists

Beta‐adrenergic regulation of cyclic adenosine 3‘,5’ monophosphate accumulation in human gastric epithelial glands. Inhibitory effect of somatostatin

A Method to Assess Histamine-Induced Cyclic AMP Production in Isolated Gastric Mucosal Cells from Human Biopsies

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Pharmacological control of the human gastric histamine H2 receptor by famotidine: comparison with H₁, H₂ and H₃ receptor agonists and antagonists

Pharmacological control of the human gastric histamine H2 receptor by famotidine: comparison with H₁, H₂ and H₃ receptor agonists and antagonists