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
Rapidly absorbed after parenteral administration.
ACTIVITY OF ORAL PENTAGASTRIN WAS DETERMINED BY ITS ACTION AS GASTRIC ACID STIMULANT IN 4 HEALTHY SUBJECTS, 2 PT WITH DUODENAL ULCERS, & 1 PT WITH ANNULAR PANCREAS IN ASSOC WITH DUODENAL ULCER.

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Metabolism / Metabolites
Primarily hepatic

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Biological Half-Life
10 minutes or less
HALF-LIFE OF PENTAGASTRIN IN CIRCULATION APPEARS TO BE ABOUT 10 MIN...

Interactions
RANITIDINE HYDROCHLORIDE INHIBITED PENTAGASTRIN STIMULATED GASTRIC SECRETION IN 15 PT WITH DUODENAL ULCERATION.

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Non-Human Toxicity Values
LD50 RATS INTRAVENOUS 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.
A synthetic pentapeptide that mimics the actions of endogenous gastrin when given parenterally. It works by stimulating the secretion of gastric acid, pepsin, and intrinsic factor. It has also been used as a diagnostic aid.
A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid.

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Drug Indication
Used as a diagnostic aid for evaluation of gastric acid secretory function

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Mechanism of Action
The exact mechanism by which pentagastrin stimulates gastric acid, pepsin, and intrinsic factor secretion is unknown; however, since pentagastrin is an analogue of natural gastrin, it is believed that it excites the oxyntic cells of the stomach to secrete to their maximum capacity. Pentagastrin stimulates pancreatic secretion, especially when administered in large intramuscular doses. Pentagastrin also increases gastrointestinal motility by a direct effect on the intestinal smooth muscle. However, it delays gastric emptying time probably by stimulation of terminal antral contractions, which enhance retropulsion.
MOST PROMINENT ACTION OF PENTAGASTRIN IS TO STIMULATE SECRETION OF GASTRIC ACID, PEPSIN, & INTRINSIC FACTOR OF CASTLE...STIMULATES PANCREATIC SECRETION, INHIBITS ABSORPTION OF WATER & ELECTROLYTES FROM ILEUM, CONTRACTS SMOOTH MUSCLE OF LOWER ESOPHAGEAL SPHINCTER & STOMACH (BUT DELAYS GASTRIC EMPTYING TIME)...
.../IT/ RELAXES SPHINCTER OF ODDI, INCR BLOOD FLOW IN GASTRIC MUCOSE, STIMULATES L-HISTIDINE DECARBOXYLASE ACTIVITY IN RAT GASTRIC MUCOSA, &, IN HIGH DOSES, STIMULATES VARIETY OF SMOOTH MUSCLES IN DIFFERENT SPECIES.
IT ALSO MIMICS OR BLOCKS EFFECTS OF POLYPEPTIDES PANCREOZYMIN-CHOLECYSTOKININ, SECRETIN, CAERULIN, NATURALLY OCCURRING DECAPEPTIDE THAT, ALONG WITH PANCREOZYMIN-CHOLECYSTOKININ, SHARES COMMON C-TERMINAL HEPTAPEPTIDE RESIDUE WITH GASTRIN.
PENTAGASTRIN ACTIVATES ADENYLATE CYCLASE IN GASTRIC MUCOSA...
PENTAGASTRIN INITIALLY PRODUCED MARKED ANTRAL ACTIVITY IN PHYSIOLOGICAL STRICTURE & SUBSEQUENT DELAY IN OVERALL RATE OF GASTRIC EMPTYING. FUNDAL MOTILITY WAS UNAFFECTED THOUGH REFLUX FROM ANTRUM OCCURRED.

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Therapeutic Uses
PENTAGASTRIN...USED WIDELY IN EUROPE SINCE 1966 TO MEASURE MAXIMAL ACID SECRETORY CAPACITY OF STOMACH. IT ELICITS REPRODUCIBLE SECRETORY RESPONSES COMPARABLE TO THOSE INDUCED BY HISTAMINE OR BETAZOLE...
.../IT/ OFFERS SEVERAL ADVANTAGES /TO HISTAMINE & BETAZOLE/. ...REQUIRES ONLY SINGLE SC OR IM INJECTION; IT IS RELATIVELY SHORT IN DURATION...
PENTAGASTRIN HAS DISTINCT EFFECT ON RATIOS OF NA+, K+, H+/AMINO ACID IN GASTRIC JUICE IN DIFFERENT STATES OF ACIDITY, VALUES OF ALL QUOTIENTS IN PT WITH HYPER, HYPO & ANACIDITY ARE SIGNIFICANTLY REDUCED.

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Pharmacodynamics
Pentagastrin is indicated as a diagnostic aid for evaluation of gastric acid secretory function. It is effective in testing for anacidity (achlorhydria) in patients with suspected pernicious anemia, atrophic gastritis, or gastric carcinoma. It is also effective in determining the reduction in acid output after operations for peptic ulcer, such as vagotomy or gastric resection.

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.)