prucalopride-hcl-r-108512-r-93877

Description: Prucalopride (also known as R-93877; trade name: Motegrity), a novel enterokinetic compound and is the first representative of the benzofuran class, is a novel selective, high affinity 5-HT (serotonin) receptor agonist for 5-HT4A and 5-HT4B receptor with Ki of 2.5 nM and 8 nM, respectively, it exhibits > 290-fold selectivity against other 5-HT receptor subtypes. Prucalopride induces contractions in a concentration-dependent manner with pEC50 of 7.5. Prucalopride significantly amplifies the rebound contraction of the guinea-pig proximal colon after electrical field stimulation. Prucalopride was approved by FDA in December 2018 to treat chronic idiopathic constipation.

References: Eur J Pharmacol. 2001 Jun 29; 423(1):71-83; N Engl J Med. 2008 May 29; 358(22):2344-54.

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