Preferred Label : Trimebutine 3-Thiocarbamoylbenzenesulfonate;
NCIt synonyms : Benzoic Acid, 3,4,5-Trimethoxy-, 2-(Dimethylamino)-2-phenylbutyl Ester, 3-(Aminothioxomethyl)benzenesulfonate
(1:1);
NCIt 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.;
UNII : 5O1CF9IS48;
InChIKey : ACKBGPXURGPUEW-UHFFFAOYSA-N;
CAS number : 1456509-46-8;
Molecule name : TB-905-02; GIC-1001;
Origin ID : C111045;
UMLS CUI : C4049135;
Automatic exact mappings (from CISMeF team)
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
