Structure of Prucalopride
CAS No.: 179474-81-8
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Prucalopride is a high-affinity 5-HT4 receptor agonist。
Synonyms: R-93877
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CAS No. : | 179474-81-8 |
Formula : | C18H26ClN3O3 |
M.W : | 367.87 |
SMILES Code : | O=C(C1=C(OCC2)C2=C(N)C(Cl)=C1)NC3CCN(CCCOC)CC3 |
Synonyms : |
R-93877
|
MDL No. : | MFCD09837787 |
InChI Key : | ZPMNHBXQOOVQJL-UHFFFAOYSA-N |
Pubchem ID : | 3052762 |
GHS Pictogram: |
![]() ![]() ![]() |
Signal Word: | Danger |
Hazard Statements: | H302-H319-H372-H410 |
Precautionary Statements: | P501-P273-P260-P270-P264-P280-P391-P314-P337+P313-P305+P351+P338-P301+P312+P330 |
Class: | 9 |
UN#: | 3077 |
Packing Group: | Ⅲ |
In Vitro:
Concentration | Treated Time | Description | References |
M2-type bone marrow-derived macrophages | 20 ng/mL IL4 | 24 hours | To evaluate the effect of IL4 on BMDM polarization, results showed that IL4-treated BMDM expressed α7nAChR. | PMC6691854 |
CHO-K1 cells | 5 pM to 1 nM | 60 minutes | Evaluate the inhibitory effect of DLT on 5HT2AR | PMC5773938 |
Human colon circular muscle cells | 1 μM | Prucalopride usually increased the amplitude of cholinergically mediated contractions evoked by EFS, with smaller increases in the amplitude of the after-contractions. In the presence of L-NAME, the excitatory actions of prucalopride on cholinergic function were sometimes less clear. | PMC3838700 | |
Porcine right atrium | 0.1 nM to 10 μM | To investigate the chronotropic effects of 5-HT4 receptor agonists on porcine right atrium. Results showed that all agonists produced chronotropic effects when administered cumulatively, without fading. | PMC1615862 | |
Porcine left atrial pectinate muscles | 0.1 nM to 10 μM | 3 to 60 minutes | To investigate the inotropic and lusitropic effects of 5-HT4 receptor agonists on porcine left atrial pectinate muscles. Results showed that all agonists produced positive inotropic effects when administered noncumulatively, but only 5-HT produced positive inotropic effects when administered cumulatively. PDE inhibitor IBMX enhanced the inotropic effects of all agonists. | PMC1615862 |
In Vivo:
Administration | Dosage | Frequency | Description | References |
Mice | Postoperative ileus (POI) model | Oral gavage | 1 or 5 mg/kg | Single dose 1.5 hours before or 22.5 hours after surgery | To evaluate the effect of Prucalopride on postoperative ileus, results showed that preoperative administration reduced intestinal inflammation and improved intestinal transit, while postoperative administration was ineffective. | PMC6691854 |
Male C57BL/6j mice | Wild-type and APP/V717I transgenic mice | Subcutaneous injection | 5 or 10 mg/kg | Single injection, mice were killed 90 min after the injection | To investigate the effect of 5-HT4 receptor agonists on sAPPα levels. Results showed that prucalopride significantly increased sAPPα levels in the hippocampus and cortex, and this increase was inhibited by the 5-HT4 receptor antagonist GR125487. | PMC2013878 |
Male C57BL/6J mice | DSS-induced colitis model | Oral | 5 mg/kg | Once daily for 7 days | Restored small intestinal motility and attenuated colitis | PMC11127033 |
129S6/SvEv mice | Contextual fear conditioning model | Intraperitoneal injection | 3 or 10 mg/kg | Single injection, behavioral tests conducted one week later | Prucalopride at 3 mg/kg attenuated learned fear and decreased stress-induced depressive-like behavior. | PMC6969048 |
C57BL/6 mice | MPTP-induced Parkinson’s disease model mice | Intraperitoneal injection | 1.5 or 3 mg/kg | Administered 2 h before each training session, twice in total | Prucalopride prevented the facilitation of contextual fear extinction in PD mice at days 2 and 3 in a dose-dependent manner, but did not have any significant effect on contextual fear extinction in control mice. | PMC6862438 |
Rats | Postoperative ileus model | Intravenous injection | 1 mg/kg and 5 mg/kg | Single dose one minute before the operation | To evaluate the effect of prucalopride on postoperative ileus. Results showed that prucalopride at 1 mg/kg significantly increased intestinal transit after laparotomy, but the effect was not significant at 5 mg/kg. | PMC1727718 |
Guinea pigs | Guinea pig isolated distal colon longitudinal muscle myenteric plexus (LMMP) | Oral | 0.1 to 10 mg/kg | Single dose, observed for 6 hours | Evaluate the effect of Prucalopride on faecal pellet output in guinea pigs. Results showed Prucalopride was most effective at 3 mg/kg. | PMC5773938 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT03610217 | Scleroderma, Systemic ... More >> Sclerosis, Systemic Less << | Not Applicable | Not yet recruiting | October 2021 | Canada, Ontario ... More >> Saint Joseph's Health Care London Not yet recruiting London, Ontario, Canada, n6a 4v2 Contact: Janet E Pope, MD, MPH, FRCPSC 15196466332 Janet.Pope@sjhc.london.on.ca Contact: Andreu Fernandez-Codina 151964661023 doccodina@gmail.com Less << |
NCT02538367 | Functional Constipation | Phase 1 Phase 2 | Completed | - | Korea, Republic of ... More >> Seoul National University Hospital Seoul, Korea, Republic of Less << |
NCT01902537 | - | Completed | - | Korea, Republic of ... More >> Seoul, Korea, Republic of Less << | |
NCT02425774 | Postoperative Ileus | Phase 4 | Recruiting | December 2017 | Belgium ... More >> University hospitals Leuven Recruiting Leuven, Vlaams-Brabant, Belgium, 3000 Contact: Nathalie Stakenborg, MSc +32 16 342883 nathalie.stakenborg@med.kuleuven.be Contact: Kim Van Beek, MSc +32 16 341326 kim.vanbeek@med.kuleuven.be Principal Investigator: Guy Boeckxstaens, M.D. Less << |
NCT01655095 | Quality of Bowel Preparation f... More >>or the Colon Capsule Colon Capsule Completion Rates Colon Capsule Polyp Detection Less << | Phase 3 | Completed | - | Canada, Ontario ... More >> Hotel Dieu Hospital Kingston, Ontario, Canada Less << |
NCT00793429 | Healthy | Phase 1 | Completed | - | - |
NCT01870674 | Healthy | Phase 1 | Completed | - | Korea, Republic of ... More >> Inje Busan Paik hospital Busan, Korea, Republic of, 614-735 Less << |
NCT00485940 | Constipation | Phase 3 | Completed | - | - |
NCT00627692 | Constipation | Phase 2 | Completed | - | - |
NCT00577018 | Constipation | Phase 3 | Completed | - | - |
NCT01070615 | Chronic Constipation | PHASE3 | COMPLETED | - | University Hospital Antwerp, E... More >>degem, 2650, Belgium Less << |
NCT01330381 | Functional Constipation | Phase 3 | Completed | - | Netherlands ... More >> Academisch Medisch Centrum Amsterdam, Netherlands, 1105 AZ Less << |
NCT01869751 | Constipation | WITHDRAWN | 2025-12-18 | University Hospitals Leuven, L... More >>euven, Vlaams-Brabant, 3000, Belgium Less << | |
NCT01330381 | - | Completed | - | - | |
NCT00987844 | Chronic Constipation | PHASE3 | COMPLETED | - | Mayo Clinic, Rochester, Minnes... More >>ota, 55905, United States Less << |
NCT01036893 | Healthy Volunteers | Phase 1 | Completed | - | Germany ... More >> FOCUS GmbH Neuss, Germany, D-41460 Less << |
NCT00575614 | Constipation | Phase 2 | Completed | - | - |
NCT01134185 | Hepatic Impairment | Phase 1 | Completed | - | Russian Federation ... More >> Moscow, Russian Federation Less << |
NCT00483886 | Constipation | Phase 3 | Completed | - | - |
NCT00617513 | Constipation | Phase 2 | Completed | - | - |
NCT01147926 | Male Subjects With Chronic Con... More >>stipation Less << | Phase 3 | Completed | - | - |
NCT00598338 | Constipation | Phase 3 | Completed | - | - |
NCT02228616 | Constipation | Phase 4 | Completed | - | China ... More >> Beijing, China Bin Zhou, China Chongqing, China Hangzhou, China Nanjing, China Shanghai, China Tianjin, China Wuhan, China Zhengzhou, China Less << |
NCT01251822 | Constipation | Phase 3 | Completed | - | Romania ... More >> Pierrel Research Timisoara, Romania, RO-300244 Less << |
NCT01147926 | - | Completed | - | - | |
NCT00631813 | Constipation | Phase 2 | Completed | - | - |
NCT00596596 | Constipation | Phase 2 | Completed | - | - |
NCT01707667 | Chronic Constipation | Phase 4 | Completed | - | United States, Oklahoma ... More >> Oklahoma Foundation for Digestive Research Oklahoma City, Oklahoma, United States Belgium UNIVERSITY OF LEUVEN, UNVERSITY HOSPITAL, Gasthuisberg Leuven, Belgium, 3000 United Kingdom Barts Health NHS Trust Whitechapel, London, United Kingdom Less << |
NCT01424228 | Constipation | Phase 4 | Completed | - | - |
NCT01707667 | - | Completed | - | - | |
NCT00488137 | Constipation | Phase 3 | Completed | - | - |
NCT00576511 | Chronic Constipation | Phase 2 | Completed | - | - |
NCT01424228 | - | Completed | - | - | |
NCT00793247 | Chronic Intestinal Pseudo-Obst... More >>ruction Less << | Phase 2 | Completed | - | United Kingdom ... More >> Northwick Park Hospital London, United Kingdom Less << |
NCT02031081 | Gastroparesis ... More >> Diabetes Mellitus Less << | Phase 2 Phase 3 | Completed | - | Canada, Alberta ... More >> University of Calgary Calgary, Alberta, Canada, T2N 4Z6 Less << |
NCT03244553 | Ineffective Esophageal Motilit... More >>y|Dysphagia Less << | PHASE2 | COMPLETED | 2019-12-02 | University of Calgary, Calgary... More >>, Alberta, T2N 1N4, Canada Less << |
NCT01807000 | Healthy | Phase 1 | Completed | - | United States, Wisconsin ... More >> Covance Global Clinical Research Unit Inc. Madison, Wisconsin, United States, 53704 Less << |
NCT01864915 | Bowel Cleansing ... More >> Colon Capsule Completion Times Less << | Phase 3 | Completed | - | Canada, Ontario ... More >> Hotel Dieu Hospital Kingston, Ontario, Canada, K7L 5V7 Less << |
NCT02047045 | Constipation | Not Applicable | Completed | - | - |
NCT00488215 | Constipation | Phase 1 | Completed | - | - |
NCT01807000 | - | Completed | - | - | |
NCT03279341 | Chronic Constipation | Phase 4 | Completed | - | Belgium ... More >> TARGID Leuven, Belgium, 3000 Less << |
NCT02781493 | Prucalopride Plus Polyethylene... More >> Glycol in Bowel Preparation for Colonoscopyp Less << | Phase 4 | Unknown | March 2017 | China, Shandong ... More >> Department of Gastroenterology, Qilu Hospital, Shandong University Not yet recruiting Jinan, Shandong, China, 250012 Contact: Yanqing Li, MD, PhD 86-0531-82169236 liyanqing@sdu.edu.cn Less << |
NCT01117051 | Non-cancer Pain ... More >> Opioid Induced Constipation Less << | Phase 3 | Terminated(The study was stopp... More >>ed by the sponsor based on a non-safety related business priority decision) Less << | - | Belgium ... More >> Leuven, Belgium Less << |
NCT00903747 | Constipation | Phase 1 | Completed | - | - |
NCT01117051 | - | Terminated(The study was stopp... More >>ed by the sponsor based on a non-safety related business priority decision) Less << | - | - | |
NCT03676374 | GERD | Phase 4 | Recruiting | April 2021 | Belgium ... More >> UZ Leuven Recruiting Leuven, Belgium, 3000 Contact: Hannelore Geysen +32 (0)16 324921 hannelore.geysen@kuleuven.be Less << |
NCT01674166 | Constipation | Phase 1 | Completed | - | - |
NCT02947269 | Postoperative Ileus ... More >> Colorectal Surgery Postoperative Complications Less << | Phase 3 | Recruiting | February 2019 | New Zealand ... More >> University of Auckland Recruiting Auckland, New Zealand, 1023 Contact: Ian Bissett, MD, FRACS +649 3737599 ext 89821 i.bissett@auckland.ac.nz Less << |
NCT01692132 | Chronic Constipation | WITHDRAWN | 2025-12-14 | Makati City, Philippines|Manil... More >>a, Philippines|Marikina City, Philippines|Muntinlupa, Philippines|Quezon City, Philippines|San Juan, Philippines|Taguig, Philippines Less << | |
NCT02510976 | Gastroparesis | Phase 4 | Unknown | - | Belgium ... More >> University Hospitals Recruiting Leuven, Vlaanderen, Belgium, 3000 Contact: Jan Tack, M.D., Ph.D. +3216344225 jan.tack@med.kuleuven.be Principal Investigator: Jan Tack, M.D., Ph.D. Less << |
NCT02004652 | Postoperative Ileus | Phase 2 | Completed | - | China, Jiangsu ... More >> Department of Generay Surgery, Jinling hosptal, Medical School of Nanjing University Nanjing, Jiangsu, China, 210002 Less << |
NCT03572790 | Molecular Mechanisms of Pharma... More >>cological Action Depression Depressive Disorder Mood Disorders Mental Disorders Antidepressive Agents Cognition Less << | Not Applicable | Not yet recruiting | March 2020 | United Kingdom ... More >> University of Oxford Not yet recruiting Oxford, United Kingdom, OX3 7JX Less << |
NCT01116206 | Constipation | Phase 3 | Completed | - | Australia ... More >> Adelaide, Australia Box Hill, Australia Kingswood, Australia Kogarah, Australia Newcastle, Australia Parkville, Australia Prahran, Australia Sydney, Australia China Beijing, China Chongqing, China Guangzhou, China Hangzhou, China Hefei, China Jinan, China Nanjing, China Shanghai, China Wuhan, China Xian, China Korea, Republic of Busan, Korea, Republic of Dae-Gu, Korea, Republic of Deajun, Korea, Republic of Gwangju-Si, Korea, Republic of Iksan, Korea, Republic of Seoul, Korea, Republic of Taiwan Taipei, Taiwan Thailand Bamgkok, Thailand Bangkok, Thailand Less << |
NCT01674192 | Constipation | Phase 1 | Completed | - | - |
NCT01670669 | Constipation | Phase 1 | Completed | - | - |
NCT00487422 | Constipation | Phase 3 | Completed | - | - |
NCT02806206 | Gastrointestinal Hemorrhage ... More >> Crohn Disease Celiac Disease Intestinal Diseases Inflammatory Bowel Diseases Less << | Phase 4 | Unknown | May 2017 | Canada, British Columbia ... More >> Vancouver General Hospital Vancouver, British Columbia, Canada, V5Z 1M9 Less << |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.72mL 0.54mL 0.27mL |
13.59mL 2.72mL 1.36mL |
27.18mL 5.44mL 2.72mL |