Felcisetrag (TAK-954, TD-8954) is a highly selective and potent 5-HT4 receptor agonist with pKi of 9.4 (human 5-HT4).
Felcisetrag (TAK-954, TD-8954) displays high selectivity (>2,000-fold) over all other 5-HT receptors and non-5-HT receptors, ion channels, enzymes and transporters.
Felcisetrag (TAK-954, TD-8954) produced an elevation of cAMP in HEK-293 cells expressing the h5-HT(4(c)) receptor (pEC=9.3), and contracted the guinea pig colonic longitudinal muscle/myenteric plexus preparation (pEC50=8.6).
Felcisetrag (TAK-954, TD-8954) (0.03-3 mg/kg) increased the colonic transit of carmine red dye, reducing the time taken for its excretion.
Felcisetrag (TAK-954, TD-8954) demonstrated robust in vivo stimulatory activity in the gastrointestinal (GI) tract of guinea pigs, rats, dogs, and humans.
