|Alias||Gastridine, Milid, Nulsa; 4-benzamido-5-(dipropylamino)-5-oxopentanoic acid; Binoside; Xylamide; Dl-proglumide|
|Appearance||White crystal powder|
Proglumide is a white crystalline powder; odorless and slightly bitter. Soluble in ethanol or chloroform, very slightly soluble in water; dissolved in sodium hydroxide test solution, Are an antacid and a peptic ulcer drug, has been evaluated in the treatment of peptic ulcer disease, postoperative pain, Huntington's chorea, schizophrenia, gastric carcinoma, and colorectal carcinoma.
Proglumide has a protective effect on the gastric mucosa and promotes ulcer healing. Applicable to gastric and duodenal ulcer, gastritis, stress ulcer, etc., the effective rate of 81-96%, the application of this product does not occur gastric acid rebound, and the recurrence rate is low.
Using glutamic acid as a starting material, reacting with benzoyl chloride to obtain N-benzoylglutamic acid, Then, acetic anhydride is reacted to obtain N-benzoylglutamic acid anhydride, and then aminated with dipropylamine to obtain proglumide. The total yield is 26-30% based on glutamic acid.
Proglumide has anti-gastrin action, has a better effect on controlling gastric acid and inhibiting pepsin secretion; and has a protective effect on gastric mucosa and promotes healing. It can be used for the treatment of gastric ulcer and duodenal ulcer, gastritis, etc. It has a good effect on the improvement of clinical symptoms of peptic ulcer and the healing of the ulcer.
It acts as a cholecystokinin antagonist, which blocks both the CCK A and CCK B subtypes. It was used mainly in the treatment of stomach ulcers, although it has now been largely replaced by newer drugs for this application.
Proglumide has also been shown to act as a δ-opioid agonist, which may contribute to its analgesic effects.
An interesting side effect of proglumide is that it enhances the analgesia produced by opioid drugs, and can prevent or even reverse the development of tolerance to opioid drugs. This can make it a useful adjuvant treatment to use alongside opioid drugs in the treatment of chronic pain conditions such as cancer, where opioid analgesics may be required for long periods and development of tolerance reduces clinical efficacy of these drugs.
Proglumide also works as a placebo effect amplifier for pain conditions. When injected visibly to a subject, its analgesic effect is bigger than a similarly administered placebo. When injected secretly, it does not have any effect, whereas standard pain drugs have an effect, even if they are administered without the subject's awareness.
The supposed mechanism is an enhancement of the neural pathways of expectation as a result of dopamine and endogenous opioids being suddenly released throughout numerous structures of the brain and spinal cord.
The ventral tegmental area is the structure believed to mediate proglumides analgesic and euphoric effects, however dozens of areas with a wide range of physical and psychological functions are implicated in the mediation of the placebo effect (this accounts for proglumides ability to produce physically measurable effects on vital signs such as heart rate, blood pressure, respiration rate, and tidal volume which can not be accounted for by its clinically insignificant δ-opioid affinity.
- Pharmaceuticals Proglumide
- Dietary Supplement, such as capsules or tablets.
Proglumide is a drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers.
Proglumide is a racemate composed of equal amounts of (R)- and (S)-proglumide. A non-selective CCK antagonist that was used primarily for the treatment of stomach ulcers, but has been replaced by newer drugs. It has a role as a drug metabolite, a xenobiotic metabolite, a cholinergic antagonist, an anti-ulcer drug, a cholecystokinin antagonist, a gastrointestinal drug, a delta-opioid receptor agonist and an opioid analgesic. It contains a (R)-proglumide and a (S)-proglumide.
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