Velusetrag (TD-5108) is a potent, selective and oral 5-HT4 receptor agonist with pKi of 7.7, shows >500-fold selectivity over other 5-HT receptors.
Velusetrag (TD-5108) displays >25-fold selectivity over other biogenic amine receptors, and no effect on hERG channels.
Velusetrag (TD-5108) increases the contractility of the canine antrum, duodenum and jejunum with higher potency than tegaserod, demonstrates robust in vivo activity in the guinea pig, rat and dog gastrointestinal tracts.
