Synonyms
Peptavlon; Pentagastrina; Pentagastrine; Gastrodiagnost; ICI-50123; Pentagastrinum; Petogasrin
Molecular Formula
C37H49N7O9S
Smiles
CC(C)(C)OC(=O)NCCC(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC3=CC=CC=C3)C(=O)N
Melting Point
229-230°C (dec.)
Boiling Point
1196.6±65.0°C at 760 mmHg (Predicted)
Relative Density
1.303±0.06 (Predicted)
General Description
Pentagastrin is a synthetic pentapeptide analogue of the hormone gastrin, consisting of the C-terminal tetrapeptide of gastrin with a protected N-terminal. Its sequence is N-[(benzyloxy)carbonyl]-β-alanyl-L-tryptophyl-L-methionyl-L-aspartyl-L-phenylalanine amide. Pentagastrin is a white to off-white powder, soluble in water. It is a potent stimulator of gastric acid secretion.
Mechanism of Action
Pentagastrin binds to the cholecystokinin-2 (CCK-2) receptor on the parietal cells of the stomach, stimulating the release of gastric acid through a series of intracellular signaling pathways. This leads to a dose-dependent increase in acid secretion. The drug also increases the secretion of pepsin and intrinsic factor.
Application
Pentagastrin is used as a diagnostic agent for the assessment of gastric acid secretion (gastric acid stimulation test) and for the evaluation of the function of the parietal cells. It is also used for the diagnosis of Zollinger-Ellison syndrome and for the testing of the responsiveness of the stomach to gastrin. The drug is effective in stimulating maximal acid output.
In HT‑29 colon cancer cells, pentagastrin (a gastrin analog) stimulated proliferation and inhibited apoptosis via the CCK‑B receptor, activating the Ras‑Raf‑MEK1/2‑ERK1/2 pathway and increasing ERK1/2 and K‑ras phosphorylation. Proglumide (a CCK‑B antagonist) blocked these effects. The study confirms that gastrin promotes growth through this signaling cascade, providing a mechanistic basis for targeting the pathway in colorectal carcinoma.
Fig. 1 Analysis of apoptosis by flow cytometry. (Mao JD, et al., 2014)
References
- Mao JD, et al. Role of ERK-MAPK signaling pathway in pentagastrin-regulated growth of large intestinal carcinoma. World J Gastroenterol. 2014;20(35):12542-12550.
Does Pentagastrin require strict cold chain storage as a synthetic peptide?
Yes, it must be stored at 2-8°C. As a pentapeptide, it is thermally labile and susceptible to deamidation and aggregation at room temperature.
Is Pentagastrin sensitive to light during handling and storage?
Yes, it is photosensitive. Store in light-resistant containers and handle under subdued light to prevent photodegradation of the tryptophan residue.
What is the stability of Pentagastrin after reconstitution for diagnostic use?
Reconstituted solutions are stable for up to 24 hours under refrigeration.
How is the purity of Pentagastrin confirmed given its peptide nature?
We use reverse-phase HPLC for chemical purity, SEC-HPLC for aggregates, and mass spectrometry for identity confirmation on each batch.