scholarly journals Macrocyclic chelator-coupled gastrin-based radiopharmaceuticals for targeting of gastrin receptor-expressing tumours

2008 ◽  
Vol 35 (10) ◽  
pp. 1868-1877 ◽  
Author(s):  
Stephan Good ◽  
Martin A. Walter ◽  
Beatrice Waser ◽  
Xuejuan Wang ◽  
Jan Müller-Brand ◽  
...  
Keyword(s):  
Gastrin Receptor ◽  
Macrocyclic Chelator

Attenuation of gastrininduced gastric acid secretion by antisense oligonucleotide to the CCKB/ gastrin receptor

Neuroreport ◽  
1995 ◽  
Vol 6 (17) ◽  
pp. 2373-2377 ◽  
Author(s):  
R. K. Rao ◽  
Y. Lopez ◽  
J. Lai ◽  
P. J. M. Riviere ◽  
J. L. Junien ◽  
...  
Keyword(s):  
Acid Secretion ◽  
Gastric Acid Secretion ◽  
Gastric Acid ◽  
Antisense Oligonucleotide ◽  
Gastrin Receptor

Abstract 341: Synergistic Effects of Renal Dopamine and Gastrin Receptors in Hypertension

Hypertension ◽  
2012 ◽  
Vol 60 (suppl_1) ◽  
Author(s):  
Yue Chen ◽  
Shuo Zhen ◽  
Laureano Asico ◽  
Pedro Jose ◽  
Chunyu Zeng
Keyword(s):  
Atpase Activity ◽  
Sodium Excretion ◽  
Synergistic Effects ◽  
Inhibitory Effect ◽  
Receptor Interaction ◽  
Gastrin Receptor ◽  
Wky Rats ◽  
Link Type ◽  
Renal Dopamine ◽  
Stimulation Of

Oral NaCl produces stronger natriuresis and diuresis as compared with venous infusion of same amount of NaCl, indicating the existence of renal-gastric axis. Although numerous hormones are secreted in gastrointestinal tract, gastrin is evident one due to its natriuretic effects and taken-up by the renal proximal tubule (RPT) cells. We hypothesize that there is an interaction between gastrin and dopamine receptor in kidney, which synergistically increases sodium excretion, the impaired interaction would be involved in the pathogenesis of hypertension. In WKY rats, infusion of gastrin, via renal artery, induced natriuresis and diuresis, which was blocked in the presence of CI988, a gastrin receptor blocker. Similarly, the natriuretic and diuretic effect of fenoldopam, a D1-like receptor agonist, was blocked by the D1-like receptor antagonist, SCH23390 , indicating that gastrin and fenoldopam, via individual receptor, play natriuretic and diuretic effects. Our further study found that lower dosages of gastrin or fenoldopam could not induce natriuresis and diuresis alone, while putting together induced natriuretic and diuretic effects. The above-mentioned effects were lost in SHRs. We also found, in the presence of SCH23390 , gastrin-mediated natriuresis and diuresis was partially blocked. Similarly, in the presence of CI988, the natriuretic and diuretic effects of fenoldopam were partially blocked, indicating the interaction between gastrin and D1-like receptor. The gastrin/D1-like receptor interaction was also confirmed in the RPT cells. Stimulation of one receptor increased the expression of the other. Stimulation of either D1-like receptor or gastrin receptor inhibited the Na + -K + -ATPase activity in RPT cells, while in the presence of SCH23390 , the inhibitory effect of gastrin on Na + -K + -ATPase activity was partially blocked. In the presence of CI988, D1-like receptor-mediated inhibitory effect of Na + -K + -ATPase activity in RPT cells was partially inhibited. It indicated the synergistic effect between gastrin and D1-like receptor would increase the sodium excretion in WKY rats; the impaired interaction might be involved in the pathogenesis of hypertension.

Mucosal gastrin receptor. III. Regulation by gastrin

1980 ◽  
Vol 238 (2) ◽  
pp. G135-G140 ◽  
Author(s):  
K. Takeuchi ◽  
G. R. Speir ◽  
L. R. Johnson
Keyword(s):  
Serum Gastrin ◽  
Binding Capacity ◽  
Specific Binding ◽  
Equilibrium Constants ◽  
Biological Response ◽  
Liquid Diet ◽  
Regulatory Process ◽  
Membrane Preparation ◽  
Gastrin Receptor ◽  
Dissociation Equilibrium

Specific binding of 125I-labeled gastrin to rat gastric mucosal membranes was found to vary with serum gastrin levels. The dissociation equilibrium constants were not significantly different between receptor preparations. However, the binding capacities of the membrane preparations were directly correlated with serum gastrin levels. Fasting, feeding a liquid diet, and antrectomy significantly decreased serum gastrin and the concentrations of the gastrin receptor. Treatment of fasted and liquid-fed animals with pentagastrin prevented the decrease in receptors. Vagotomy increased both binding capacity and serum gastrin levels. These data indicate that gastrin stimulates the production of its own receptor. The upregulation of the gastrin receptor was evident if the binding capacity was expressed per milligram of protein, per microgram of DNA, or per amount of 125I-labeled choleragen bound to the same membrane preparation. This indicates that the biological response to gastrin is controlled in part by the regulation of the number of gastrin receptors present and that gastrin plays a role in this regulatory process.

Identification of a CCK-B/GASTRIN receptor amino acid determinant of inverse agonist activity

2000 ◽  
Vol 118 (4) ◽  
pp. A308
Author(s):  
John S. Pratt ◽  
Mathieu Goumain ◽  
Kirsten Schaffer ◽  
Ci Chen ◽  
Martin Beinborn ◽  
...  
Keyword(s):  
Amino Acid ◽  
Inverse Agonist ◽  
Agonist Activity ◽  
Gastrin Receptor

Effect of Aging on Gastrin Receptor Gene Expression in Rat Stomach

Peptides ◽  
1998 ◽  
Vol 19 (2) ◽  
pp. 225-229 ◽  
Author(s):  
Shinya Waki ◽  
Yoshikazu Kinoshita ◽  
He-yao Wang ◽  
Masakyo Asahara ◽  
Yumi Matsushima ◽  
...  
Keyword(s):  
Gene Expression ◽  
Receptor Gene ◽  
Rat Stomach ◽  
Gastrin Receptor ◽  
Receptor Gene Expression
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