tcsc2574 Prucalopride

Prucalopride (R093877) is a drug acting as a selective, high affinity 5-HT4 receptor agonist(pKi=8.6/8.1 for 5-HT4a/4b); >150-fold higher affinity for 5-HT4 receptors than for other receptors.

IC50 value: 8.6/8.1 for 5-HT4a/4b(pKi)

Target: 5-HT4 receptor

Prucalopride is a novel enterokinetic compound and is the first representative of the benzofuran class. Receptor binding data have demonstrated prucalopride's high affinity to both investigated 5-HT(4) receptor isoforms, with mean pK(i) estimates of 8.60 and 8.10 for the human 5-HT(4a) and 5-HT(4b) receptor, respectively. From the 50 other binding assays investigated in this study only the human D(4) receptor (pK(i) 5.63), the mouse 5-HT(3) receptor (pK(i) 5.41) and the human sigma(1) (pK(i) 5.43) have shown measurable affinity, resulting in at least 290-fold selectivity for the 5-HT(4) receptor [1].