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Chemical Structure| 179474-81-8 Chemical Structure| 179474-81-8
Chemical Structure| 179474-81-8

Prucalopride

CAS No.: 179474-81-8

Prucalopride is a high-affinity 5-HT4 receptor agonist。

Synonyms: R-93877

4.5 *For Research Use Only !

Cat. No.: A126651 Purity: 98%

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Product Details of Prucalopride

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

Safety of Prucalopride

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:

Related Pathways of Prucalopride

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description Reference
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:

Species
Animal Model
Administration Dosage Frequency Description Reference
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 <<

Protocol

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

References

 

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