Table 1.
Receptor binding profile of 5-HT4 agonists for GI disorders, at therapeutic concentrations
Receptor binding profile at therapeutic concentrations | ||||||
---|---|---|---|---|---|---|
Drug | 5-HT4 | 5-HT3 | 5-HT2 | 5-HT1 | D2 | hERG |
Cisapride | + | + | + | + | ||
Tegaserod | + | + | + | + | ||
Renzapride | + | + | ||||
Clebopride | + | + | + | |||
Mosapride | + | + | ||||
Prucalopride | + | |||||
Velusetrag | + | |||||
Naronapride | + |
GI, gastrointestinal.
+ indicates affinity for this receptor (as either agonist or antagonist) that is likely to be clinically relevant at concentrations necessary for 5-HT4 agonism (i.e. for therapeutic action). Information from De Maeyer et al.2008