Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P01350 (gastrin)
 9,683 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Eleven male and five female gastric ulcer outpatients as well as twenty eight male and seven female duodenal ulcer outpatients received Proglumide (1200 mg/day) or magnesiumtrisilicate (1320 mg/day) in a prospective double blind study. The sizes of the ulcers were assessed by endoscopy before and after 4 weeks therapy. A complete healing of gastric ulcers was observed in 75% (n = 8) of the patients receiving Proglumide and 25% (n = 8) of the antacid treated controls (p less than 0.05; x2 test). The healed area was significantly (p less than 0.05) larger in the Proglumide 91 mm2) than in the anticida group (23 mm2). In addition, the half time of the ulcer-healing was significantly (p less than 0.05) shorter in the Proglumide treated patients (18 days and 26 days respectively). There was no significant effect of the drug on the duodenal ulcers. The spontaneous healing rate was 61% in the antacid (n = 18) and 59% in the Proglumide treated (n = 17) patients. The drug does not effect the basal and pentagastrin stimulated gastric secretion nor the serum gastrin concentration. No side effects on blood pressure, blood cell count, transaminases or blood glucose concentrations could be observed.
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PMID:Efficient treatment of gastric ulcer with proglumide (Milid) in outpatients (double blind trial). 38 97

In a double-blind trial 16 persons with gastric ulcer and 35 with duodenal ulcer were treated as out-patients with 1200 mg proglumide daily or 1320 mg magnesium tricilicate daily (as an "active placebo") for four weeks. The ulcers were assessed by endoscopy before and after treatment. The gastric ulcers disappeared in 75% of patients receiving proglumide (six of eight subjects) but in only 25% of those on the placebo (two of eight). There was no significant effect of proglumide on duodenal ulcers (17 in the proglumide and 18 in the placebo groups). Proglumide failed to affect either basal or maximally stimulated acid secretion, nor was there any change in the serum gastrin level. There were no side effects during proglumide administration. This underlines its therapeutic value in the treatment of gastric ulcer, in comparison with cimetidine or carbenoxolone.
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PMID:[Effective out-patient treatment of gastric ulcer with proglumide: preliminary results (author's transl)]. 76 39

A brief review of the role of gastrin on gastric secretion and its influence in the genesis of peptic ulcer is made. A report is made of the pharmacological studies of Proglumida and its antigastrin action and the interest its association with Hioscin Butil-Bromuro may represent in the antiulcer therapy. A study is made of 26 patients submitted to a general treatment for peptic ulcer this drug together with a bland diet and psychotherapy. The results were: 19 (73%) cases cured; 6 (23%) cases improved; no results in 1 (4%) case. No secondary side effects appear and the symptomatic response appears 8 days after the treatment is initiated. The dosis used is of 2 tablets before the 3 main meals. Each tablet contains 250 mg of Proglumide and 10 mg of Hioscin Butil-Bromuro. It is considered useful in the antiulcer therapy to have available a drug which can control the physiological effects of gastrin and from this point of view its action is different from that of the antiacids and anticolinergics.
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PMID:[Antigastrin therapy in gastric ulcer]. 82 74

The rat pancreatic cell line, AR42J possessed high-affinity gastrin and somatostatin receptors and its growth was stimulated by physiological gastrin-17 concentrations between 5 x 10(-11) mol/l and 10(-9) mol/l as measured by [75Se]selenomethionine uptake. The somatostatin analogue, octreotide (2 x 10(-7) to 2 x 10(-11) mol/l), reduced this stimulated growth. Gastrin-stimulated AR42J growth was also inhibited by proglumide (3 x 10(-4) mol/l) and lorglumide (3 x 10(-5) mol/l) at maximal G17 concentrations of 5 x 10(-11) and 10(-10) mol/l, respectively, and the analogues competed with [125I] gastrin-17 (5 x 10(-10) mol/l) for binding to gastrin receptors on AR42J (50% inhibitory concentrations, less than or equal to 10(-3) mol/l and 4 x 10(-6) mol/l, respectively. Octreotide reduced the basal growth of the human gastric cell line, MKN45G, (which is associated with intracellular gastrin immunoreactivity) in serum-free medium to 73% of control at a concentration of 2 x 10(-8) mol/l, which was reversed by gastrin-17 (10(-10) mol/l). Lorglumide (3 x 10(-5) mol/l) also reduced the basal growth to 30% of control, which was reversed to 78% by 10(-5) mol/l gastrin. Proglumide had no effect on the basal growth of MKN45G.
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PMID:Inhibition of gastrin-stimulated growth of gastrointestinal tumour cells by octreotide and the gastrin/cholecystokinin receptor antagonists, proglumide and lorglumide. 135 50

In the present study we have investigated the effects of proglumide (PRO) and somatostatin analog (SMS 201-995) on the mitotic activity of colonic mucosa in rats under basal conditions and after omeprazole (OM). The stathmokinetic method was used. Proglumide and OM were administered for 5 days, twice daily, SMS 201-995 on the 5th day of the experiment only, also twice daily. It was found that: 1) OM enhanced the proliferation of colonic mucosa, as well as increased serum gastrin, when compared to controls, 2) OM and PRO, when applied jointly, decreased the mitotic activity of the colonic epithelium, 3) PRO alone increased the colonic cell proliferation.
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PMID:Effect of omeprazole-induced hypergastrinaemia on the proliferation of colonic mucosal epithelial cells in the rat. 186 13

The effects of gastrin (G-17), proglumide (a gastrin receptor antagonist), and enprostil (a synthetic analog of prostaglandin E2) used alone or in association were studied in colonic cancer Prob and Regb cell growth. The Prob (progressive in BD IX rats) and Regb (regressive) cell lines were cloned from a single chemically-induced rat colonic cancer. After a serum-free period corresponding to one doubling cell time, cells were incubated with 100 to 1,200 pM G-17, 40 or 80 mM proglumide, and 2.5 to 5 micrograms/ml enprostil for 8 h. Cell growth was measured 48 h later by colorimetric MTT assay. Two and four hundred pM G-17 gave a growth stimulation of 17.4 percent and 31 percent for Prob cells respectively or 35.5 percent and 49 percent for Regb cells. Growth stimulation was found to be statistically different (P less than 0.01) for Prob and Regb cells. Proglumide partially inhibited this growth stimulation whereas enprostil inhibited in totally. These results suggest that growth of some colonic cancer cell lines may be G-17 dependent. However the intensity of cell-growth stimulation depends on the level of cell malignancy or differentiation in a single tumor.
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PMID:[Effect of gastrin and enprostil, a PGE2 analog, on colonic cancerous cell growth]. 191 30

Gastrin is trophic for rodent gut mucosa. Proglumide, a competitive inhibitor of gastrin, can exert an antitrophic effect and can block pentagastrin-stimulated DNA synthesis. We have examined the influence of the circadian system on pentagastrin-stimulated DNA synthesis in the murine stomach (glandular and nonglandular stomach) and colon. We studied 224 male CD2F1 mice divided into four groups. Group A was ad lib fed (controls). Groups B, C, and D received 6-9 intraperitoneal injections of either NaCl, pentagastrin or pentagastrin + proglumide, at 8-h intervals prior to sacrifice. Mice from each group (A-D) were killed (by cervical dislocation) at 3-h intervals for 24 h. Incorporation of tritiated thymidine (DNA synthesis) was measured, and significant (p less than 0.001) circadian rhythms were found, which were not eliminated after treatment with either pentagastrin or pentagastrin + proglumide. DNA synthesis in the glandular stomach increased significantly after treatment with pentagastrin , but only during the span of time when DNA synthesis was increasing also in control mice; it had no effect at other times. Proglumide blocked the effect of pentagastrin only during the time of increasing DNA synthesis; it had no effect at other times. The identical regimen given at different times in the circadian cycle yielded significantly different results. In the intact animal, studies on the effects of various stimulators or inhibitors of DNA synthesis should be time-qualified.
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PMID:Pentagastrin-stimulated DNA synthesis in mouse gut is influenced by the circadian system. 192 22

Gastric cancer remains a disease with a very poor prognosis, and there is no safe and effective form of therapy for advanced disease. Evidence is now abundant to show that gastrin stimulates the growth of both gastric and colorectal cancer cells in vitro and in vivo, and that blockade of gastrin receptors can prolong survival in xenografted nude mice. We have thus performed a randomized, controlled study of the gastrin/cholecystokinin receptor antagonist proglumide as therapy in 110 patients with gastric carcinoma. Proglumide had no overall effect on survival (Mantel-Cox statistic = 0.5, P = 0.48). The 95% confidence interval for the proglumide treated group was 260 to 474 days compared to 230 to 372 days for the control group. No significant difference was seen with proglumide, which has a relatively low affinity with the gastrin receptor and also has partial agonist activity. Drugs that are far more specific and potent gastrin receptor antagonists are becoming available, which may have a greater effect on survival, and further clinical trials of such compounds are clearly indicated to determine the efficacy of hormonal control of gastrointestinal malignancy.
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PMID:The effect of the gastrin receptor antagonist proglumide on survival in gastric carcinoma. 220 95

This study was done to compare the effects of two cholecystokinin antagonists, proglumide and CR-1409, on cholecystokinin-induced changes in intrabiliary pressure in vivo. We have substantially modified the constant infusion biliary manometry model, successfully used in large animals, to measure contractility of the gallbladder in guinea pigs. A silicone catheter for manometry was placed in the fundus of the gallbladder of an anesthetized guinea pig, and the biliary tree was constantly infused at 0.1 milliliter per minute with normal saline solution. The intraluminal pressure of the system was continuously recorded. The model was used to demonstrate a dose-response curve to bolus administration of exogenous cholecystokinin (0.01 to 1.0 nanomole per kilogram) and also to study the actions of proglumide, an antagonist to gastrin and cholecystokinin, and CR-1409, a newer, specific cholecystokinin antagonist, on cholecystokinin-induced contraction of the gallbladder of the guinea pig in vivo. Proglumide, at a dose of 5 millimoles per kilogram, completely abolished increases in intrabiliary pressure caused by cholecystokinin (0.5 nanomole per kilogram), whereas this effect was achieved by only 5 micromoles per kilogram of CR-1409. In both, there was full recovery from cholecystokinin antagonism within one hour. CR-1409 is one thousand times more potent than proglumide against cholecystokinin-induced changes in intrabiliary pressure in vivo and appears to be a useful pharmacologic reagent to study cholecystokinin-mediated components of physiologic contraction of the gallbladder.
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PMID:In vivo comparison of inhibition with proglumide and CR-1409 of cholecystokinin-induced pressure in the biliary tract of the guinea pig. 230 48

Proglumide, a glutaramic acid derivative, is a specific competitive inhibitor of gastrin and cholecystokinin (CCK) receptors. As such, it blocks gastrin-stimulated acid secretion, the trophic effect of gastrin, and CCK-stimulated smooth muscle contraction and acinar cell secretion. In the current study we have demonstrated that proglumide (100 mg/kg three times per day) blocks the trophic effect of a low dose of CCK octapeptide (300 ng/kg) given three times a day for 2 days. The same dose of proglumide when given alone for 6 days, however, resulted in a significant stimulation of pancreatic growth. Proglumide had no effect on the trophic response to a high dose of CCK-OP (5 micrograms/kg) administered for either 2 or 6 days. These results indicate that given over a period of several days proglumide behaves like a partial agonist of pancreatic growth.
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PMID:Effect of proglumide on rat pancreatic growth. 241 Nov 50


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