| Bioactivity | 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. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | 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]. Animal Model: | ||||||||||||
| Name | Felcisetrag | ||||||||||||
| CAS | 916075-84-8 | ||||||||||||
| Formula | C25H37N5O3 | ||||||||||||
| Molar Mass | 455.59 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |
Felcisetrag
CAS: 916075-84-8 F: C25H37N5O3 W: 455.59
Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic
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