Felcisetrag

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.

Research Areas >> Others

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

huamn 5-HT4(c) Receptor:9.4 (pKi)

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]. Animal Model: Guinea pigs[1] Dosage: 0.03~3 mg/kg Administration: S.c. Result: Increased the colonic transit of carmine red dye, reducing the time taken for its excretion. Animal Model: Rats[1] Dosage: 0.03~10 mg/kg Administration: Intraduodenal administration Result: Evoked a dose-dependent relaxation of the esophagus. Animal Model: Dogs[1] Dosage: 10 and 30 μg/kg Administration: P.o Result: Produced an increase in contractility of the antrum, duodenum, and jejunum.

[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.