39133-31-8 Trimebutine AKSci H947
 
 
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  H947    
Trimebutine
, 98%
 
3,4,5-Trimethoxybenzoic acid 2-(dimethylamino)-2-phenylbutyl ester




IDENTITY
CAS Number:39133-31-8
MDL Number:MFCD00133873
MF:C22H29NO5
MW:387.47
EINECS:254-309-2
SPECIFICATIONS & PROPERTIES
Purity:98%
Physical Form:White powder
Melting Point:78-83°C
Long-Term Storage:Store long-term at 2-8°C
UN #:Not hazmat

BIOLOGICAL INFO
Application(s):Agonist of peripheral mu, kappa and delta opiate receptors

REVIEW

 Trimebutine is a spasmolytic with possible local anesthetic action used in gastrointestinal disorders. The compound is a antimuscarinic drug, with weak mu opioid agonist effects. The maleic acid salt of trimebutine is marketed under the trademark of Debridat, Recutin, Polybutin,] or Modulon for treatment of irritable bowel syndrome and other gastrointestinal disorders.. Trimebutine exerts its effects in part due to causing a premature activation of phase III of the migrating motor complex in the digestive tract. The actions of trimebutine] on the gastrointestinal tract are mediated via (i) an agonist effect on peripheral mu, kappa and delta opiate receptors and (ii) release of gastrointestinal peptides such as motilin and modulation of the release of other peptides, including vasoactive intestinal peptide, gastrin and glucagon. Trimebutine accelerates gastric emptying, induces premature phase III of the migrating motor complex in the intestine and modulates the contractile activity of the colon. Recently, trimebutine has also been shown to decrease reflexes induced by distension of the gut lumen in animals and it may therefore modulate visceral sensitivity. Clinically, trimebutine has proved to be effective in the treatment of both acute and chronic abdominal pain in patients with functional bowel disorders, especially irritable bowel syndrome, at doses ranging from 300 to 600 mg/day. It is also effective in children presenting with abdominal pain.

REFERENCES
[1]Kaneto H, Takahashi M, Watanabe J. The opioid receptor selectivity for trimebutine in isolated tissues experiments and receptor binding studies. Journal of Pharmacobiodynamics. 1990 Jul;13(7):448-53.
[2] Fraitag B, Hostein J, Pascaud X, Junien JL.Trimebutine. Pharmacology, recent concepts about its mechanism of action, therapeutic results. Gastroenterol Clin Biol. 1992;16(5):413-20.
[3] Delvaux M, Wingate D. Trimebutine: mechanism of action, effects on gastrointestinal function and clinical results. J Int Med Res. 1997 Sep-Oct;25(5):225-46.
[4] Tanaka M. Gastric ulcer, motility, and trimebutine. J Gastroenterol. 1998 Dec;33(6):916-7.

GHS

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319; H335

Precautionary Statements
P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501


RELATED PRODUCTS
H947Trimebutine
H948Trimebutine maleate

Current as of January 18, 2019


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CATEGORIES

 APIs and Bioactives > AChR Antagonists


PubChem
  @PubMed