Kimia Biosciences Limited

Prucalopride Succinate

General Information:

PrucaloprideSuccinate is indicated for the treatment of chronic idiopathic constipation (CIC) in adults.CIC is one of the most common chronic functional gastrointestinal disorders worldwide. Prucalopride is a dihydro benzofuran carboxamide derivative from the benzofurane family that selectively stimulates 5-HT4 receptors and thus, it presents enterokinetic properties.2 The high selectivity of prucalopride allowed further development as it prevented the cardiac adverse reactions observed due to non-target effects of precedent therapies. Prucalopride has been associated with a minimal rate of transient serum enzyme elevations during therapy and has not been implicated in cases of clinically apparent liver injury with jaundice.

CAS No.

179474-85-2

Therapeutic Category:

Prokinetic Agent.

IUPAC Name:

4-Amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-7-benzofurancarboxamide

Molecular Formula:

C18H26CIN3O3

Molecular Weight:

C18H26CIN3O3

Molecular Structure:

Prucalopride succinate

Mechanism of Action

Prucalopride acts as a selective stimulator of the 5-HT4 receptors while having no interaction with the hERG channel or 5-HT1 receptors which reduces significantly the cardiovascular risk found in other similar drugs.5-HT4 receptors can be found throughout the gastrointestinal tract primarily in smooth muscle cells, enterochromaffin cells, and myenteric plexus. Its activation produces the release of acetylcholine which is the major excitatory neurotransmitter in the GI tract. Hence, prucalopride stimulates motility by interacting specifically with 5-HT4 receptors in the GI tract which causes a release of acetylcholine and further contraction of the muscle layer of the colon and relaxation of the circular muscle layer leading to the propulsion of luminal content.