A potent and selective 5-HT4 agonist (Ki = 2.5 and 8 nM for 5-HT4A and 5-HT4B, respectively); greater than 250-fold selective for 5-HT4 over a panel of 53 overexpressed receptors, including 5-HT subtypes, but does bind to human D4 and σ1 receptors and mouse 5-HT3 receptors (Kis = 2.3, 3.7, and 3.8 μM respectively); induces 5-HT4-dependent contractions in guinea pig colon (EC50 = 33 nM) and facilitates non-cholinergic contractions induced by electrical stimulation; increases colonic motility by inhibiting distal colon contractions in dogs (ED50 = 0.04 mg/kg, p.o.); increases acetylcholine and histamine levels in the rat prefrontal cortex and the power of hippocampal theta oscillations (5-10 mg/kg, s.c.)