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Trimebutine 3-Thiocarbamoylbenzenesulfonate (Code C111045)

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Terms & Properties

Preferred Name: Trimebutine 3-Thiocarbamoylbenzenesulfonate

Definition: A sulfonate-based salt form of a trimebutine derivative, an orally available, peripherally-acting opioid agonist and muscarinic antagonist, with potential visceral analgesic activity. Upon oral administration of GIC-1001, this agent may exert its therapeutic effects through the potential mechanisms of action for the trimebutine and sulfonate moieties: The trimebutine moiety can act as a motility enhancer in the gastrointestinal (GI) tract, as an antispasmodic agent to reduce colonic spasms, as an agonist of colonic mu and kappa opioid receptors, which could provide an analgesic effect, and blocks sodium channels and the release of a variety of GI peptides, which modulates the activity of visceral afferents. The sulfonate moiety releases hydrogen sulfide (H2S), which is involved, through an as of yet not fully elucidated mechanism of action, in the modulation of visceral perception and pain, possibly through the activation of ATP-sensitive potassium (KATP) ion channels and mu opioid receptors. Altogether, administration of this agent may both facilitate the insertion of the colonoscope during a colonoscopy and reduce colonic spasms and pain.

Label: Trimebutine 3-Thiocarbamoylbenzenesulfonate

NCI Thesaurus Code: C111045 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C4049135  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
Benzoic Acid, 3,4,5-Trimethoxy-, 2-(Dimethylamino)-2-phenylbutyl Ester, 3-(Aminothioxomethyl)benzenesulfonate (1:1)
GIC-1001
TB-905-02
TRIMEBUTINE 3-THIOCARBAMOYLBENZENESULFONATE
Trimebutine 3-Thiocarbamoylbenzenesulfonate

External Source Codes: 
CAS Registry Number 1456509-46-8 (see NLM ChemIDplus info)
FDA UNII Code 5O1CF9IS48
PDQ Closed Trial Search ID 751908
PDQ Open Trial Search ID 751908 (check for NCI PDQ open clinical trial info)
UMLS CUI C4049135

Other Properties:
     Name Value (qualifiers indented underneath)
code C111045
Contributing_Source FDA
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  

URL: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&ns=ncit&code=C111045

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