PRUCALOPRIDE SUCCINATE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C18H26ClN3O3.C4H6O4
Molecular Weight	485.958
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)CCC(O)=O.COCCCN1CCC(CC1)NC(=O)C2=C3OCCC3=C(N)C(Cl)=C2

InChI

InChIKey=QZRSNVSQLGRAID-UHFFFAOYSA-N

InChI=1S/C18H26ClN3O3.C4H6O4/c1-24-9-2-6-22-7-3-12(4-8-22)21-18(23)14-11-15(19)16(20)13-5-10-25-17(13)14;5-3(6)1-2-4(7)8/h11-12H,2-10,20H2,1H3,(H,21,23);1-2H2,(H,5,6)(H,7,8)

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11438309 | http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/001012/WC500053998.pdf | https://www.ncbi.nlm.nih.gov/pubmed/26628294

Prucalopride is a novel enterokinetic compound and is the first representative of the benzofuran class. Prucalopride is a potent, selective and specific serotonin 5-HT4 receptor (5-HT4-R) agonist. Prucalopride (Resolor®), a highly selective serotonin 5-HT4 receptor agonist, is indicated in the European Economic Area for the treatment of adults with chronic idiopathic constipation (CIC) in whom laxatives have failed to provide adequate relief.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Serotonin 4 (5-HT4) receptor 39 Target ID: CHEMBL1875 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11438309	Agonist 2678		8.6 null [pKi]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Constipation, chronic 3 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/001012/WC500053998.pdf	Primary		Approved 8429	RESOLOR Approved Use Resolor is indicated for symptomatic treatment of chronic constipation in adults in whom laxatives fail to provide adequate relief Launch Date 2008

C_max

Value	Dose	Co-administered	Analyte	Population
7 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf	2 mg 1 times / day steady-state, oral dose: 2 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		PRUCALOPRIDE plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
109 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf	2 mg 1 times / day steady-state, oral dose: 2 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		PRUCALOPRIDE plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
1 day DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf	2 mg 1 times / day steady-state, oral dose: 2 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		PRUCALOPRIDE plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
70% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf	2 mg 1 times / day steady-state, oral dose: 2 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		PRUCALOPRIDE plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
2 mg 1 times / day steady, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: steady Dose: 2 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf	unhealthy, 47 years (range: 17-95 years) n = 1251 Health Status: unhealthy Condition: chronic idiopathic constipation Age Group: 47 years (range: 17-95 years) Sex: M+F Population Size: 1251 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf	Disc. AE: Nausea, Headache... Other AEs: Headache, Abdominal pain... AEs leading to discontinuation/dose reduction: Nausea (2%) Headache (1%) Diarrhea (1%) Abdominal pain (1%) Other AEs: Headache (19%) Abdominal pain (16%) Upper abdominal pain (16%) Lower abdominal pain (16%) Abdominal tenderness (16%) Abdominal discomfort (16%) Epigastric discomfort (16%) Nausea (14%) Diarrhea (13%) Abdominal distension (5%) Dizziness (4%) Vomiting (3%) Flatulence (3%) Fatigue (2%) Nausea (2%) Headache (1%) Diarrhea (1%) Abdominal pain (1%) Headache (19%) Abdominal pain (16%) Upper abdominal pain (16%) Lower abdominal pain (16%) Abdominal tenderness (16%) Abdominal discomfort (16%) Epigastric discomfort (16%) Nausea (14%) Diarrhea (13%) Abdominal distension (5%) Dizziness (4%) Vomiting (3%) Flatulence (3%) Fatigue (2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
10 mg 1 times / day multiple, oral Highest studied dose Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf	healthy n = 60 Health Status: healthy Population Size: 60 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737 inhibitor 1587 inducer 781	substrate 1037 inhibitor 1767	substrate 1217 inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1524 CYP2A6 707 CYP2B6 810 CYP2C8 911 CYP2C19 1478 CYP2E1 882 OATP1B1 788 OATP1B3 706 OAT1 599 OAT3 642 BSEP 402 MRP2 383 OCT1 512 OCT2 647 MATE1 306 MATE2 263 P-gp 1461 BCRP 699	CYP1A1 349 CYP1A2 1054 CYP2A6 543 CYP2B6 664 CYP2C8 693 CYP2C19 991 CYP2E1 667 CYP3A5 395 P-gp 1537 BCRP 561 OATP1B1 406 OATP1B3 350 OAT1 326 OAT3 339 OCT1 327 OCT2 355 MATE1 135 MATE2 96 BSEP 52 MRP2 205	CYP1A2 701 CYP2B6 547

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no [IC50 >100 uM]
CYP2A6 739	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no [IC50 >100 uM]
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no [IC50 >100 uM]
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no [IC50 >100 uM]
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no [IC50 >100 uM]
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no [IC50 >100 uM]
CYP2E1 970	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no [IC50 >100 uM]
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no [IC50 >100 uM]
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no [IC50 >=300 uM]
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no [IC50 >=300 uM]
BSEP 403	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no
MRP2 475	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no
OAT1 603	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	no
CYP2B6 1001	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0	weak
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=188 Page: 188.0	yes [IC50 38 uM]	weak (co-administration study) Comment: administered with dextromethorphan; in vivo DDI potential via inhibition of CYP2D6 appears low at the proposed dose Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=188 Page: 188.0
MATE1 308	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=190 Page: 190.0	yes [IC50 4 uM]
MATE2 263	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=190 Page: 190.0	yes [IC50 69 uM]
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=190 Page: 190.0	yes [IC50 7.8 uM]
OCT1 543	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=190 Page: 190.0	yes [IC50 9.4 uM]

Drug as victim

Target	Modality	Activity	Clinical evidence
BSEP 52	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=188 Page: 188.0	no
CYP1A1 349	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=187 Page: 187.0	no
CYP1A2 1054	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=187 Page: 187.0	no
CYP2A6 543	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=187 Page: 187.0	no
CYP2B6 664	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=187 Page: 187.0	no
CYP2C19 991	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=187 Page: 187.0	no
CYP2C8 693	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=187 Page: 187.0	no
CYP2C9 1037	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=187 Page: 187.0	no
CYP2D6 1217	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=187 Page: 187.0	no
CYP2E1 667	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=187 Page: 187.0	no
CYP3A5 395	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=187 Page: 187.0	no
MATE1 135	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=188 Page: 188.0	no
MATE2 96	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=188 Page: 188.0	no
MRP2 205	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=188 Page: 188.0	no
OAT1 326	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=188 Page: 188.0	no
OAT3 339	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=188 Page: 188.0	no
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=188 Page: 188.0	no
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=188 Page: 188.0	no
OCT1 327	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=188 Page: 188.0	no
OCT2 355	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=188 Page: 188.0	no
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=187 Page: 188;189	yes [Km 116 uM]
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=187 Page: 188;189	yes [Km 15 uM]
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=100 Page: 100;187	yes	weak (co-administration study) Comment: co-administration of ketoconazole increased the Cmax and AUCtau of prucalopride at steady state by 38% and 37%, respectively; Administration of erythromycin, probenecid, cimetidine, and paroxetine did not have a significant effect on the PK of prucalopride (<10% change in Cmax and AUC) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=100 Page: 100;187

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=40 Page: 40.0

Sourcing

Vendor/Aggregator	ID	URL
AA Blocks	AA0026Y3	http://www.aablocks.com/goods/Goods/detail?id=AA0026Y3
AK Scientific, Inc. (AKSCI)	Y0251	http://www.aksci.com/item_detail.php?cat=Y0251
Aaron Chemicals	AR0027PV	http://www.aaronchem.com/179474-81-8
AbMole Bioscience	M2146	http://www.abmole.com/products/prucalopride.html
Achemtek	0104-024538	http://www.achemtek.com/179474-81-8
Adooq BioScience	A11771	https://www.adooq.com/prucalopride.html
Alfa Chemistry	AP179474818	https://reagents.alfa-chemistry.com/product/prucalopride-cas-179474-81-8-6688.html
Alsachim	2960	http://www.alsachim.com/product-C4032-glo.bal-view.html
Ambinter	Amb20241338	http://www.ambinter.com/reference/20241338
Angel Pharmatech	AG151228	http://www.angelpharmatech.com/179474-81-8.html
ApexBio Technology	B2253	http://www.apexbt.com/prucalopride.html
Ark Pharm	AK170477	http://www.arkpharminc.com/products/179474-81-8.html
Aurora Fine Chemicals LLC	A24.082.365	http://online.aurorafinechemicals.com/info?ID=A24.082.365
Aurora Fine Chemicals LLC	K16.609.755	http://online.aurorafinechemicals.com/info?ID=K16.609.755
Aurum Pharmatech LLC	Q-3828	http://www.Aurumpharmatech.com/Product/ProductDetails/Q_3828
Axon MedChem	1479	https://www.axonmedchem.com/product/1479
BLD Pharm	BD149417	http://www.bldpharm.com/products/179474-81-8.html
BioChemPartner	BCP02177	http://www.biochempartner.com/179474-81-8-BCP02177
BioCrick	BCC5055	http://www.biocrick.com/Prucalopride-BCC5055.html
CSNpharm	CSN11795	https://www.csnpharm.com/products/prucalopride.html
Capot Chemical	22481	http://www.capotchem.com/en/22481.htm
Capot Chemical	PubChem22481	http://www.capotchem.com/en/22481.htm
Chem Scene	CS-2574	http://www.chemscene.com/179474-81-8.html
ChemMol	49400298	http://www.chemmol.com/chemmol/49400298.html
ChemMol	97900178	http://www.chemmol.com/chemmol/97900178.html
Chemenu	CM107382	http://www.chemenu.com/products/CM107382
Chemspace	CSSB00016993940	https://chem-space.com/CSSB00016993940
Clearsynth	CS-O-30738	https://www.clearsynth.com/en/CSO30738.html
DC Chemicals	DC4147	http://www.dcchemicals.com/product_show-Prucalopride.html
Excenen	EX-A1333	http://www.excenen.com/searchresultlist.php?id=179474-81-8
Finetech	FT-0674128	http://www.finetechnology-ind.com/prod/detail/pub/179474-81-8.html
Glentham Life Sciences	GP6979	http://www.glentham.com/products/product/GP6979/
Hairui	HR103880	http://www.hairuichem.com/en/product/179474-81-8.html
Lab Network	LN01343283	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01343283
MedChem Express	HY-14151	https://www.medchemexpress.com/Prucalopride.html
MuseChem	A000859	https://www.musechem.com/product/A000859.html
OChem	25269	http://www.ocheminc.com/index.php?act=psearch&pid=474P818
Renno Tech	RL02293	http://www.rennotech.com/product_show.asp?id=2542
Smolecule	S540468	http://www.smolecule.com/products/s540468
Synblock Inc	PB31402	http://www.synblock.com/product/179474-81-8.html
THE BioTek	bt-280940	https://www.thebiotek.com/product/inhibitors/bt-280940
THE BioTek	bt-331990	https://www.thebiotek.com/product/others/bt-331990
VladaChem	VL261712-1G	https://www.vladachem.com/product.php?products=179474-81-8
abcr GmbH	AB454709	http://www.abcr.com/shop/en/AB454709
eNovation Chemicals	D381138	http://www.enovationchem.com/productDetails.asp?productID=D381138
eNovation Chemicals	Y1012706	https://www.enovationchem.com/ProductDetails.asp?ProductID=Y1012706
iChemical	EBD25754	http://www.ichemical.com/chemicals/cas-179474-81-8

PubMed

Title	Date	PubMed
New and emerging treatments for irritable bowel syndrome and functional dyspepsia.	2002 May	15989538
Gateways to clinical trials.	2002 Oct	12500432
5-HT4 receptors exert a frequency-related facilitatory control on dorsal raphé nucleus 5-HT neuronal activity.	2002 Sep	12372017
Prucalopride is effective in patients with severe chronic constipation in whom laxatives fail to provide adequate relief. Results of a double-blind, placebo-controlled clinical trial.	2003	12743445
Irritable bowel syndrome: an overview of diagnosis and pharmacologic treatment.	2003 Jun	12825862
Gateways to clinical trials.	2003 May	12808477
Gastrointestinal motility disorders and gastrointestinal prokinetic therapy.	2003 Sep	14552159
Effect of enterokinetic prucalopride on intestinal motility in fast rats.	2003 Sep	12970907
The treatment of chronic constipation in elderly people: an update.	2004	15554750
Modulation of hippocampal excitability by 5-HT4 receptor agonists persists in a transgenic model of Alzheimer's disease.	2004	15489027
New and emerging treatment options for chronic constipation.	2004	15184816
Presynaptic modulation of cholinergic and non-cholinergic fast synaptic transmission in the myenteric plexus of guinea pig ileum.	2004 Jun	15198658
Electrophysiological effects of prucalopride, a novel enterokinetic agent, on isolated atrial myocytes from patients treated with beta-adrenoceptor antagonists.	2005 Apr	15644433
Rationale for using serotonergic agents to treat irritable bowel syndrome.	2005 Apr 1	15790796
Frontocortical 5-HT4 receptors exert positive feedback on serotonergic activity: viral transfections, subacute and chronic treatments with 5-HT4 agonists.	2005 Apr 15	15820713
Prucalopride is a partial agonist through human and porcine atrial 5-HT4 receptors: comparison with recombinant human 5-HT4 splice variants.	2005 Jun	16012870
Fading of 5-HT4 receptor-mediated inotropic responses to 5-hydroxytryptamine is caused by phosphodiesterase activity in porcine atrium.	2006 Jan	16331292
Investigation of serotonin receptors in the isolated penile bulb of rats.	2006 Nov-Dec	16528294
5HT4 agonists inhibit interferon-gamma-induced MHC class II and B7 costimulatory molecules expression on cultured astrocytes.	2006 Oct	16839612
5-HT4 receptor agonists enhance both cholinergic and nitrergic activities in human isolated colon circular muscle.	2006 Sep	16918765
5-HT4 receptor agonists increase sAPPalpha levels in the cortex and hippocampus of male C57BL/6j mice.	2007 Apr	17325649
The serotonin signaling system: from basic understanding to drug development for functional GI disorders.	2007 Jan	17241888
Gastric and enteric involvement in progressive systemic sclerosis.	2008 Jan	18097282
Prucalopride: the evidence for its use in the treatment of chronic constipation.	2008 Jun	20694083
Alternative splicing and exon duplication generates 10 unique porcine 5-HT 4 receptor splice variants including a functional homofusion variant.	2008 Jun 12	18430808
Prucalopride and donepezil act synergistically to reverse scopolamine-induced memory deficit in C57Bl/6j mice.	2008 Mar 5	18061284
Synergy between 5-HT4 receptor activation and acetylcholinesterase inhibition in human colon and rat forestomach.	2008 May	18194150
New treatments for irritable bowel syndrome in women.	2008 Nov	19072463
[Functional and motor gastrointestinal disorders].	2008 Oct	19434861
Gateways to clinical trials.	2008 Sep	18985183
Prucalopride.	2009	19911858
Gateways to clinical trials.	2009 Apr	19536362
Prucalopride: a new drug for the treatment of chronic constipation.	2009 Aug	19673621
Clinical trial: the efficacy, impact on quality of life, and safety and tolerability of prucalopride in severe chronic constipation--a 12-week, randomized, double-blind, placebo-controlled study.	2009 Feb 1	19035970
Selective desensitization of the 5-HT4 receptor-mediated response in pig atrium but not in stomach.	2009 Jan	19154432
Gateways to clinical trials.	2009 Mar	19455266
Prucalopride (Resolor) in the treatment of severe chronic constipation in patients dissatisfied with laxatives.	2009 Mar	18987031
The use of novel promotility and prosecretory agents for the treatment of chronic idiopathic constipation and irritable bowel syndrome with constipation.	2009 May	19444393
Comments on tegaserod trial on irritable bowel syndrome.	2010 Apr	20535361
Update on the management of constipation in the elderly: new treatment options.	2010 Aug 9	20711435
Psychometric performance and clinical meaningfulness of the Patient Assessment of Constipation-Quality of Life questionnaire in prucalopride (RESOLOR) trials for chronic constipation.	2010 Feb	19761492
Selective serotonin reuptake inhibitors potentiate the rapid antidepressant-like effects of serotonin4 receptor agonists in the rat.	2010 Feb 16	20169084
[New drugs for the treatment of constipation].	2010 Jul	20676949
New-generation 5-HT4 receptor agonists: potential for treatment of gastrointestinal motility disorders.	2010 Jun	20408739
Psychometric evaluation of a visual analog scale for the assessment of anxiety.	2010 Jun 8	20529361
Influence of 5-HT4 receptor activation on acetylcholine release in human large intestine with endometriosis.	2010 May	20025676
Emerging pharmacologic therapies for irritable bowel syndrome.	2010 Oct	20694841
Efficacy and safety of prucalopride in patients with chronic noncancer pain suffering from opioid-induced constipation.	2010 Oct	20428949
Fixed combination of oxycodone with naloxone: a new way to prevent and treat opioid-induced constipation.	2010 Sep	20714946
A double-blind, placebo-controlled study of prucalopride in elderly patients with chronic constipation.	2010 Sep	20529205

Patents

Sample Use Guides

In Vivo Use Guide

Adults: 2 mg once daily with or without food, at any time of the day.

Route of Administration: Oral

In Vitro Use Guide

Cell shortening and real-time Ca(2+) measurements were processed on field-stimulated intact cardiomyocytes with the selective 5-HT4R agonist, prucalopride (1 uM).

Name

Type

Language

PRUCALOPRIDE SUCCINATE

Official Name

English

PRUCALOPRIDE SUCCINATE [USAN]

Common Name

English

PRUCALOPRIDE SUCCINATE [MART.]

Common Name

English

MOTEGRITY

Brand Name

English

Prucalopride succinate [WHO-DD]

Common Name

English

PRUCALOPRIDE (AS SUCCINATE)

Common Name

English

BUTANEDIOIC ACID, COMPD. WITH 4-AMINO-5-CHLORO-2,3-DIHYDRO-N-(1-(3-METHOXYPROPYL)-4-PIPERIDINYL)-7-BENZOFURANCARBOXAMIDE (1:1)

Common Name

English

RESOLOR

Brand Name

English

PRUCALOPRIDE SUCCINATE [ORANGE BOOK]

Common Name

English

R-108512

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C47794