For research use only. Not for therapeutic Use.
Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pKi =9.4) for human 5-HT4(c) receptors.
Felcisetrag produces an elevation of cAMP in HEK-293 cells expressing the h5-HT4(c) receptor (pEC50 = 9.3), and contracts the guinea pig colonic longitudinal muscle/myenteric plexus preparation (pEC50 = 8.6). Felcisetrag has moderate intrinsic activity in the vitro assays[1].
Felcisetrag (0.03~3 mg/kg; s.c.) increases the colonic transit of carmine red dye, reducing the time taken for its excretion[1].
Felcisetrag (0.03~10 mg/kg; intraduodenal administration) evokes a dose-dependent relaxation of the esophagus[1].
Felcisetrag (10 and 30 μg/kg; p.o) produces an increase in contractility of the antrum, duodenum, and jejunum[1].
| Catalog Number | I009728 |
| CAS Number | 916075-84-8 |
| Synonyms | methyl 4-[[4-[[(2-propan-2-yl-1H-benzimidazole-4-carbonyl)amino]methyl]piperidin-1-yl]methyl]piperidine-1-carboxylate |
| Molecular Formula | C25H37N5O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C25H37N5O3/c1-17(2)23-27-21-6-4-5-20(22(21)28-23)24(31)26-15-18-7-11-29(12-8-18)16-19-9-13-30(14-10-19)25(32)33-3/h4-6,17-19H,7-16H2,1-3H3,(H,26,31)(H,27,28) |
| InChIKey | MZOITCJKGUIQEI-UHFFFAOYSA-N |
| SMILES | CC(C)C1=NC2=C(C=CC=C2N1)C(=O)NCC3CCN(CC3)CC4CCN(CC4)C(=O)OC |
| Reference | [1]. Beattie DT, et al. The Pharmacology of TD-8954, a Potent and Selective 5-HT(4) Receptor Agonist with Gastrointestinal Prokinetic Properties. Front Pharmacol. 2011;2:25. |
