Tegaserod (maleate)

Tegaserod (maleate) is a potent agonist of the serotonin 4 receptor (5-HT4, Ki = 3.9-31 nM). As 5-HT4 receptors are associated with cholinergic nerves lining the colon, tegaserod (maleate) stimulates colonic motility and transit in vivo, in both healthy and diseased gastrointestinal tracts. However, it lacks selectivity, since it also acts as an antagonist for the 5-HT2A, 5-HT2B, and 5-HT2C receptors (Ki = 32, 3.9, and 100 nM, respectively). It is a weak agonist of 5-HT3 (Ki = 10 µM).Formal Name: 2-[(5-methoxy-1H-indol-3-yl)methylene]-N-pentyl-hydrazinecarboximidamide, 2Z-butenedioate. CAS Number: 189188-57-6. Synonyms: SDZ-HTF 919, Zelnorm. Molecular Formula: C16H23N5O . C4H4O4. Formula Weight: 417.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.03 mg/ml, DMSO: 20 mg/ml. lambdamax: 279, 316 nm. SMILES: COC(C=C1)=CC2=C1NC=C2/C=N/NC(NCCCCC)=N.OC(/C=C\C(O)=O)=O. InChi Code: InChI=1S/C16H23N5O.C4H4O4/c1-3-4-5-8-18-16(17)21-20-11-12-10-19-15-7-6-13(22-2)9-14(12)15,5-3(6)1-2-4(7)8/h6-7,9-11,19H,3-5,8H2,1-2H3,(H3,17,18,21),1-2H,(H,5,6)(H,7,8)/b20-11+,2-1-. InChi Key: CPDDZSSEAVLMRY-FEQFWAPWSA-N.