Molecular Formula | C18H26ClN3O3.C4H6O4 |
Molar Mass | 485.95838 |
Melting Point | >196°C (dec.) |
Solubility | DMSO (Slightly), Methanol (Slightly) |
Appearance | Solid |
Color | White to Pale Brown |
Storage Condition | Sealed in dry,Room Temperature |
Use | This product is for scientific research only and shall not be used for other purposes. |
In vitro study | Prucalopride induced contraction in a concentration-dependent manner with a pEC50 of 7.5. Prucalopride (1 mM) significantly amplifies rebound contractions after electrical stimulation of the proximal colon in guinea pigs. Prucalopride induced relaxation of the mucosal basal layer of the prepared rat esophagus with a pEC50 of 7.8, resulting in a monophasic concentration-response curve. Prucalopride (0.1 μm) concentration-dependently increases the amplitude of non-maximal cholinergic contractions and acetylcholine release elicited by electric field stimulation in pig gastric ring muscle, an effect that can be expressed by IBMX (10 μm) induced and reinforced. Prucalopride (1 μm) can significantly enhance the cholinoid contraction induced by porcine descending colon electricity, and the promotion can be significantly enhanced by Rolipram. |
In vivo study | Prucalopride dose-dependently alters the pattern of colonic contractile motility by stimulating contractions of the proximal colonic high-amplitude tuft and by inhibiting the terminal colonic contractile activity in fasted dogs. Prucalopride also caused a dose-dependent decrease in the time to the first macromigratory contraction (GMC); With higher doses of prucalopride, the first GMC usually occurred within the first half hour after treatment. |
Introduction | prucalopride succinate, chemical name 4-amino-5-chloro-2, 3-dihydro-n-[1-(3-methoxypropyl)-4-piperidinyl]-7-benzofuran formamide, it is a selective 5-hydroxytryptamine receptor agonist developed by Belgium MovetisNV company. In October 2009, the European Medical Administration approved its monosuccinate for marketing, which is clinically used for the treatment of constipation in women who cannot be relieved by laxative. |
biological activity | Prucalopride is a selective, high-affinity 5-HT4 receptor agonist, acts on impaired gastrointestinal movements associated with chronic constipation, thereby normalizing bowel movements. Prucalopride is a selective, high-affinity 5-HT4 receptor agonist that acts on impaired gastrointestinal motility associated with chronic constipation, thereby normalizing bowel movements. |
contraindication | 1. Allergic to the active ingredient of this product or any auxiliary material. 2, renal dysfunction in patients requiring dialysis. 3. Patients with intestinal perforation or obstruction due to structural or functional abnormalities of the intestinal wall, obstructive ileus, severe intestinal inflammatory diseases such as Crohn's disease, ulcerative colitis, and toxic megacolon/giant rectum. 4. Recent bowel surgery. |
Target | Value |
5-HT4A | 2.5 nM(Ki) |
5-HT4B | 8 nM(Ki) |