Prucalopride is an orally-available, dibenzofuran-based, enterokinetic agonist of the human serotonin 5-HT4a and 5-HT4b receptor isoforms with Ki estimates of 3 nM and 8 nM, respectively. It has modest selectivity over the human D4 receptor (2.3 uM), mouse 5-HT3 receptor (3.7 uM) and human s1 receptor (3.7 uM). (1, 2)
Initial tolerability studies show that prucalopride does not encounter cardiotoxicity issues to the extent seen in other drugs of this class. [3]
Technical information:
Chemical Formula: | C18H26ClN3O3 | |
CAS #: | 179474-81-8 | |
Molecular Weight: | 367.87 | |
Purity: > 98% | ||
Appearance: | White | |
Chemical Name: | 7-Benzofurancarboxamide, 4-amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl] | |
Solubility: | Up to 100 mM in DMSO | |
Synonyms: | 0 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
1. | Briejer et al., The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound, Eur. J. Pharmcol. 2001, 423, 71-83. Pubmed ID: 11438309 |
2. | Frampton et al., Prucalopride: ADIS Drug Profile. Drugs, 2009, 69(17), 2453-2476. Pubmed ID: 19911858 |
3. | Quigley et al., Prucalopride: safety, efficacy and potential applications. Ther. Adv. Gastroenterol. 2012, 5(1), 23-30. |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.