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Pharmaceutical intermediates Proglumide raw Materials powder
Product Overview:
Proglumine is the earliest gastrin antagonist discovered, and it and benzotript are derivatives of glutaramicacid. proglumide, also a racemic compound, is called (±) -5-dipropyl amino-4-benzoylamino-5-oxo-valeric acid, English name Proglumide, included in the Chinese Pharmacopoeia 2000, Part II, page 96, as a gastrin receptor antagonist. The chemical structure is similar to the terminal chemical structure of gastrin (G-17) and cholecystokinin (CCK). Its functional group amido specifically competes with gastrin for gastrin receptors on parietal cells, so it can significantly inhibit the secretion of gastric acid and pepsin induced by gastrin, but has no obvious effect on the secretion of gastric acid induced by histamine and vagus nerve stimulation.
Pharmaceutical intermediates Proglumide raw Materials powder Attributes
CAS:6620-60-6
MF:C18H26N2O4
MW:334.41
EINECS:229-567-4
Specification: 99% min Proglumide powder
Sample:Proglumide powder
Packaging:1kg/bag, 25kg/drum
Brand:Henrikang
Appearance:white
Storage: Cool Dry Place
Shelf Life: 2 Years
Test Method: HPLC
Pharmaceutical intermediates Proglumide raw Materials powder Details
Proglumide powder Usage and Synthesis.
Dipropanglutamide is used for gastric and duodenal ulcers, gastritis (e.g. chronic superficial gastritis), and duodenoculitis.
1. Combined with other anti-ulcer drugs (such as H2 receptor antagonists), it can enhance the effect of inhibiting gastric acid secretion and accelerate ulcer healing.
2. When used in combination with morphine, it can enhance the analgesic effect of morphine and prolong the duration of its effect.
3. This product can antagonize the effect of haloperidol to aggravate movement disorders, so the two can not be used in the treatment of Huntington's disease.
Uses of Proglumide.
Dipropanglutamide is a gastrin receptor antagonist, which can protect gastric mucosa and promote ulcer healing. Suitable for gastric and duodenal ulcer, gastritis, stress ulcer, the effective rate of 81-96%, the application of this product does not occur the increase of gastric acid rebound, and the recurrence rate is low. It is a gastrin receptor antagonist for gastric and duodenal ulcer disease.
Pharmacological action of Proglumide.
This product is an antagonist of cholecystokinin receptor and gastrin receptor, and its molecular structure is similar to the terminal molecular structure of gastrin (G-17) and cholecystokinin (CCK), so the functional group amyl group can specifically compete with G-17 on the G-17 receptor in parietal cells, and significantly inhibit the secretion of gastric acid and pepsin caused by G-17. Increase the content of hexosamine in gastric mucosa, promote glycoprotein synthesis, protect gastric mucosa, thus improve the symptoms of peptic ulcer and promote ulcer healing. The inhibitory effect of this product on gastric acid secretion caused by histamine and vagus nerve stimulation is not obvious, and the rebound phenomenon of gastric acid secretion does not occur in the treatment of peptic ulcer and gastritis, and the gastric acid secretion can still be at the normal level for half a year after the termination of treatment. Because of its weaker inhibition of gastric acid secretion than H2 receptor antagonists, it is no longer used in the treatment of ulcer disease alone in clinic, but its gallbladder effect has been paid more attention recently.
Product Methods of Proglumide.
Glutamic acid is used as the starting material to obtain N-benzoyl glutamic acid by reacting with benzoyl chloride, and then reacting with acetic anhydride to obtain N-benzoyl glutamic anhydride, and then aminating with dipropylamine to obtain proglumine. The total yield was 26-30% as measured by glutamic acid.