Intracellular Ca2+ is increased by pengastrin (ICI-50123) (0.1-100 μM; GH3 cells) in a dose-dependent manner, up to a maximal rise of 2.77-fold [1]. GH3 cells bind to pengastrin (ICI-50123) in a dose-dependent manner (0.1–100 μM) [1].

Pengastrin (ICI-50123) (80 µg/kg/h; intravenous injection; male Sprague-Dawley rats) protects the gastrointestinal mucosa of rats against injury by acidified aspirin [2].

Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (approximately 200 grams) [2]
Doses: 80 µg/kg/h
Route of Administration: intravenous (iv) (iv)injection
Experimental Results: Protect the gastric mucosa of rats from acidified aspirin damage. Causes a hyperemic response to luminal acid challenge, increases mucus gel thickness, and increases pHi during acid challenge.

Absorption, Distribution and Excretion
Rapid absorption after parenteral administration. The activity of orally administered Pentagastrin was determined by its role as a gastric acid stimulant in 4 healthy subjects, 2 patients with duodenal ulcers, and 1 patient with annular pancreas and duodenal ulcers. Metabolism/Metabolites Primarily metabolized in the liver. Biological Half-Life 10 minutes or less. The half-life of circulating Pentagastrin appears to be approximately 10 minutes…

Interactions
Ranitidine hydrochloride inhibited Pentagastrin-stimulated gastric secretion in 15 patients with duodenal ulcers. Non-human Toxicity The intravenous LD50 in rats was 160-170 mg/kg.

[1]. Characterisation of CCKB receptors on GH3 pituitary cells: receptor activation is linked to Ca2+ mobilisation. Eur J Pharmacol. 1994 Apr 15;267(2):215-23.

[2]. Pentagastrin gastroprotection against acid is related to H2 receptor activation but not acid secretion. Gut. 1998 Sep;43(3):334-41.

Pentagastrin is an organic molecular entity. It is a synthetic pentapeptide that, when administered parenterally, mimics the effects of endogenous gastrin. Its mechanism of action is through stimulation of the secretion of gastric acid, pepsin, and intrinsic factor. It is also used as an adjunct diagnostic tool. It is a synthetic pentapeptide that, when administered parenterally, has a gastrin-like effect. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor and is used as an adjunct diagnostic tool. Drug Indications Used for adjunct diagnostic assessment of gastric acid secretion function. Mechanism of Action The exact mechanism by which Pentagastrin stimulates the secretion of gastric acid, pepsin, and intrinsic factor is not fully understood; however, because Pentagastrin is an analog of natural gastrin, it is believed to stimulate gastric fundic gland cells to secrete to their maximum capacity. Pentagastrin can stimulate pancreatic secretion, especially with high-dose intramuscular injection. Pentagastrin can also enhance gastrointestinal motility by acting directly on intestinal smooth muscle. However, it may enhance counter-pumping force by delaying gastric emptying time through stimulating terminal antral contraction. The most significant effects of Pentagastrin are stimulating the secretion of gastric acid, pepsin, and intrinsic factor…stimulating pancreatic secretion, inhibiting ileal absorption of water and electrolytes, contracting the lower esophageal sphincter and gastric smooth muscle (but delaying gastric emptying time)… It relaxes the sphincter of Oddi, increases gastric mucosal blood flow, stimulates the activity of L-histidine decarboxylase in the rat gastric mucosa, and at high doses, stimulates various smooth muscles in different species. It can also mimic or block the effects of peptides such as cholecystokinin, secretin, secretin, and the naturally occurring decapeptide, which, like cholecystokinin, shares a common C-terminal heptapeptide residue with gastrin. Pentagastrin activates adenylate cyclase in the gastric mucosa… Pentagastrin initially produces significant antral activity in physiological stenosis, subsequently delaying the overall rate of gastric emptying. Despite antral reflux, fundic motility remains unaffected.

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Therapeutic Uses
Pentagastrin…has been widely used in Europe since 1966 to measure the maximum acid secretion capacity of the stomach. It elicits a reproducible secretory response, comparable to that induced by histamine or betazol…
…Compared to histamine and betazol, it has several advantages…requiring only a single subcutaneous or intramuscular injection; its duration of action is relatively short…
Pentagastrin significantly affects the ratios of sodium, potassium, and hydrogen ions to amino acids in gastric juice under different acidity conditions; these ratios are significantly reduced in patients with hyperacidity, hypoacidity, and anacidity.

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Pharmacodynamics
Pentagastrin is suitable for the auxiliary diagnosis of assessing gastric acid secretion function. It is effective in detecting anacidity (low gastric acid) in patients suspected of having pernicious anemia, atrophic gastritis, or gastric cancer. It is also effective in determining the reduction in gastric acid secretion after peptic ulcer surgery (such as vagotomy or gastrectomy).

C37H49N7O9S

767.891460000001

767.331

5534-95-2

Pentagastrin meglumine;57448-84-7

9853654

White to off-white solid powder

1.3±0.1 g/cm3

1196.6±65.0 °C at 760 mmHg

229-230° (dec)

677.5±34.3 °C

0.0±0.3 mmHg at 25°C

1.604

3.03

8

10

22

54

1310

4

O=C(N[C@@H](CCSC)C(N[C@@H](CC(O)=O)C(N[C@H](C(N)=O)CC1=CC=CC=C1)=O)=O)[C@@H](NC(CCNC(OC(C)(C)C)=O)=O)CC2=CNC3=C2C=CC=C3

NEYNJQRKHLUJRU-DZUOILHNSA-N

InChI=1S/C37H49N7O9S/c1-37(2,3)53-36(52)39-16-14-30(45)41-28(19-23-21-40-25-13-9-8-12-24(23)25)34(50)42-26(15-17-54-4)33(49)44-29(20-31(46)47)35(51)43-27(32(38)48)18-22-10-6-5-7-11-22/h5-13,21,26-29,40H,14-20H2,1-4H3,(H2,38,48)(H,39,52)(H,41,45)(H,42,50)(H,43,51)(H,44,49)(H,46,47)/t26-,27-,28-,29-/m0/s1

(3S)-4-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-2-[[(2S)-3-(1H-indol-3-yl)-2-[3-[(2-methylpropan-2-yl)oxycarbonylamino]propanoylamino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-oxobutanoic acid

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ≥ 34 mg/mL (~44.28 mM)
H2O : < 0.1 mg/mL

Solubility in Formulation 1: ≥ 2.08 mg/mL (2.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.08 mg/mL (2.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)