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CAS No. 179474-85-2
Prucalopride is a selective, high affinity 5-HT4 receptor agonist. The Ki values of prucalopride for human 5-HT(4a) and 5-HT(4b) receptor are 2.5 nM and 8 nM, respectively.
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Prucalopride in the presence of IBMX on the S2/S1 ratio of electrically induced total tritium outflow. Tissues were stimulated twice (S1 and S2; 1 millisecond, 15 V, 4 Hz, 2 minutes); IBMX was added 36 minutes and prucalopride 15 minutes before S2. Mean S2/S1±SEM; one‐way ANOVA followed by Bonferroni corrected t test with ns not significant, *P<.05 and ***P<.001.
Neurogastroenterol Motil, 2018, 30(2). Prucalopride Succinate purchased from Selleck.
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|Description||Prucalopride is a selective, high affinity 5-HT4 receptor agonist. The Ki values of prucalopride for human 5-HT(4a) and 5-HT(4b) receptor are 2.5 nM and 8 nM, respectively.|
Prucalopride induces contractions in a concentration-dependent manner with pEC50 of 7.5. Prucalopride (1 mM) significantly amplifies the rebound contraction of the guinea-pig proximal colon after electrical field stimulation. Prucalopride induces relaxation of the rat oesophagus preparation of rat oesophagus tunica muscularis mucosae with pEC50 of 7.8, yielding a monophasic concentration–response curve.  Prucalopride (0.1 μM) concentration-dependently increases the amplitude of submaximal cholinergic contractions and of acetylcholine release induced by electrical field stimulation in pig gastric circular muscle, and the effect is induced and enhanced IBMX (10 μM).  Prucalopride (1 μM) significantly enhances the electrically induced cholinergic contractions in pig descending colon, and the facilitating effect is significantly enhanced by Rolipram. 
|In vivo||Prucalopride alters colonic contractile motility patterns in a dose-dependent fashion by stimulating high-amplitude clustered contractions in the proximal colon and by inhibiting contractile activity in the distal colon of fasted dogs. Prucalopride also causes a dose-dependent decrease in the time to the first giant migrating contraction (GMC); at higher doses of prucalopride, the first GMC generally occurres within the first half-hour after treatment. |
|In vitro||DMSO||97 mg/mL (199.6 mM)|
|Water||97 mg/mL (199.6 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04429802||Completed||Drug: Prucalopride||Gastrointestinal Motility Disorder|Dyspepsia||Universitaire Ziekenhuizen Leuven||September 26 2013||Not Applicable|
|NCT01807000||Completed||Drug: Radiolabeled Prucalopride Succinate||Healthy||Shire||March 2013||Phase 1|
|NCT01692132||Withdrawn||Drug: Prucalopride||Chronic Constipation||Janssen Pharmaceutica||February 2013||--|
|NCT03279341||Completed||Drug: polyethylene glycol|Drug: Bisacodyl|Drug: Prucalopride||Chronic Constipation||University Hospital Gasthuisberg||December 3 2012||Phase 4|
|NCT01117051||Terminated||Drug: placebo|Drug: prucalopride||Non-cancer Pain|Opioid Induced Constipation||Shire||May 2010||Phase 3|
|NCT00903747||Completed||Drug: prucalopride|Drug: moxifloxacin|Drug: placebo||Constipation||Movetis||January 2009||Phase 1|
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