Velusetrag

Velusetrag is an agonist of the serotonin (5-HT) receptor subtype 5-HT4. It increases cAMP accumulation in HEK293 cells expressing human 5-HT4(c), 5-HT4(d), and 5-HT4(g) receptors (EC50s = 5.01, 2.51, and 6.31 nM, respectively). Velusetrag is greater than 500-fold selective for the 5-HT4 receptor over ten other 5-HT receptors and greater than 25-fold selective over eighteen other non-5-HT biogenic amine receptors at 10 µM. It induces contractions in guinea pig colonic longitudinal muscle-myenteric plexus (LM-MP) preparations (EC50 = 12.59 nM) and relaxation in carbachol-precontracted rat esophagus preparations (EC50 = 12.59 nM). Velusetrag reduces fecal transit time in guinea pigs and increases contractility of the antrum, duodenum, and jejunum in dogs.. SMILES: [H][C@@]12CC[C@@](C[C@H](C1)NC(C3=CC4=CC=CC=C4N(C(C)C)C3=O)=O)(N2C[C@H](CN(S(=O)(C)=O)C)O)[H]. InChi Code: InChI=1S/C25H36N4O5S/c1-16(2)29-23-8-6-5-7-17(23)11-22(25(29)32)24(31)26-18-12-19-9-10-20(13-18)28(19)15-21(30)14-27(3)35(4,33)34/h5-8,11,16,18-21,30H,9-10,12-15H2,1-4H3,(H,26,31)/t18-,19+,20-,21-/m0/s1. InChi Key: HXLOHDZQBKCUCR-WOZUAGRISA-N