Preferred Label : Dolcanatide;
NCIt synonyms : D-Leucine, D-asparaginyl-L-alpha-aspartyl-L-alpha-glutamyl-L-cysteinyl-L-alpha-glutamyl-L-leucyl-L-cysteinyl-L-valyl-L-asparaginyl-L-valyl-L-alanyl-L-cysteinyl-L-threonylglycyl-L-cysteinyl-,
Cyclic (4- 12),(7- 15)-bis(disulfide);
NCIt definition : An orally administered analog of the human endogenous natriuretic hormone uroguanylin
and guanylate cyclase C (GC-C) agonist, with potential laxative, anti-nociceptive
and anti-inflammatory activities. Upon administration, dolcanatide, by mimicking uroguanylin,
binds to and activates GC-C locally on endothelial cells in the gastrointestinal (GI)
tract, without entering the systemic circulation. Activation of GC-C results in an
increase in cyclic guanosine monophosphate (cGMP). Increased concentrations of cGMP
lead to the activation of the anion channel cystic fibrosis transmembrane conductance
regulator (CFTR). CFTR activation increases the secretion of negatively charged ions,
particularly chloride and bicarbonate, into the GI tract lumen, which further drives
sodium ions and then water into the lumen. This leads to increased fluid secretion
in the GI tract, accelerated transit and changes in stool consistency. In addition,
ion channel modulation may decrease muscle contractions and the activity of pain-sensing
nerves, thereby decreasing intestinal pain. Also, GC-C may inhibit the secretion of
pro-inflammatory cytokines, which may ameliorate GI inflammation. Uroguanylin, a naturally
occurring human GI peptide, is a ligand for GC-C and plays a key role in anti-inflammatory
processes in the GI tract.;
UNII : WU977T914K;
CAS number : 1092457-65-2;
Molecule name : SP-333; SP 333;
NCI Metathesaurus CUI : CL554973;
Origin ID : C153478;
UMLS CUI : C4519311;
Automatic exact mappings (from CISMeF team)
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
