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Details

Stereochemistry ACHIRAL
Molecular Formula C18H26ClN3O3
Molecular Weight 367.87
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PRUCALOPRIDE

SMILES

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

InChI

InChIKey=ZPMNHBXQOOVQJL-UHFFFAOYSA-N
InChI=1S/C18H26ClN3O3/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/h11-12H,2-10,20H2,1H3,(H,21,23)

HIDE SMILES / InChI

Molecular Formula C18H26ClN3O3
Molecular Weight 367.87
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
8.6 null [pKi]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
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
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
7 ng/mL
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

AUC

ValueDoseCo-administeredAnalytePopulation
109 ng × h/mL
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
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
1 day
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
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
70%
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

Doses

DosePopulationAdverse 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:
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:
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:
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:
healthy
n = 60
AEs

AEs

AESignificanceDosePopulation
Abdominal pain 1%
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:
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:
Diarrhea 1%
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:
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:
Headache 1%
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:
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:
Abdominal pain 1%
Disc. AE
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:
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:
Diarrhea 1%
Disc. AE
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:
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:
Headache 1%
Disc. AE
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:
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:
Diarrhea 13%
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:
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:
Diarrhea 13%
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:
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:
Nausea 14%
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:
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:
Nausea 14%
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:
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:
Abdominal discomfort 16%
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:
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:
Abdominal discomfort 16%
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:
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:
Abdominal pain 16%
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:
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:
Abdominal pain 16%
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:
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:
Abdominal tenderness 16%
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:
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:
Abdominal tenderness 16%
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:
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:
Epigastric discomfort 16%
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:
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:
Epigastric discomfort 16%
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:
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:
Lower abdominal pain 16%
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:
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:
Lower abdominal pain 16%
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:
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:
Upper abdominal pain 16%
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:
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:
Upper abdominal pain 16%
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:
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:
Headache 19%
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:
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:
Headache 19%
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:
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:
Fatigue 2%
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:
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:
Fatigue 2%
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:
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:
Nausea 2%
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:
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:
Nausea 2%
Disc. AE
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:
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:
Flatulence 3%
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:
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:
Flatulence 3%
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:
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:
Vomiting 3%
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:
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:
Vomiting 3%
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:
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:
Dizziness 4%
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:
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:
Dizziness 4%
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:
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:
Abdominal distension 5%
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:
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:
Abdominal distension 5%
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:
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:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >=300 uM]
no [IC50 >=300 uM]
no
no
no
no
no
no
no
no
weak
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
Page: 188.0
yes [IC50 4 uM]
yes [IC50 69 uM]
yes [IC50 7.8 uM]
yes [IC50 9.4 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
yes [Km 116 uM]
yes [Km 15 uM]
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)
Page: 100;187
Tox targets

Tox targets

Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Pharmacological treatment of irritable bowel syndrome--from concept to sales.
2002
New and emerging treatments for irritable bowel syndrome and functional dyspepsia.
2002 May
The treatment of chronic constipation in elderly people: an update.
2004
Modulation of hippocampal excitability by 5-HT4 receptor agonists persists in a transgenic model of Alzheimer's disease.
2004
New and emerging treatment options for chronic constipation.
2004
Presynaptic modulation of cholinergic and non-cholinergic fast synaptic transmission in the myenteric plexus of guinea pig ileum.
2004 Jun
Management of faecal incontinence and constipation in adults with central neurological diseases.
2006 Apr 19
Porcine left atrial and sinoatrial 5-HT(4) receptor-induced responses: fading of the response and influence of development.
2006 Jan
Fading of 5-HT4 receptor-mediated inotropic responses to 5-hydroxytryptamine is caused by phosphodiesterase activity in porcine atrium.
2006 Jan
5HT4 agonists inhibit interferon-gamma-induced MHC class II and B7 costimulatory molecules expression on cultured astrocytes.
2006 Oct
5-HT4 receptor agonists enhance both cholinergic and nitrergic activities in human isolated colon circular muscle.
2006 Sep
5-HT4 receptor agonists increase sAPPalpha levels in the cortex and hippocampus of male C57BL/6j mice.
2007 Apr
Recent advances in understanding the role of serotonin in gastrointestinal motility in functional bowel disorders: alterations in 5-HT signalling and metabolism in human disease.
2007 Aug
The serotonin signaling system: from basic understanding to drug development for functional GI disorders.
2007 Jan
Little or no ability of obestatin to interact with ghrelin or modify motility in the rat gastrointestinal tract.
2007 Jan
Electrophysiological and arrhythmogenic effects of 5-hydroxytryptamine on human atrial cells are reduced in atrial fibrillation.
2007 Jan
The action of the novel gastrointestinal prokinetic prucalopride on the HERG K+ channel and the common T897 polymorph.
2007 Jan 12
5-HT4 receptor agonists: similar but not the same.
2008 Feb
Gastric and enteric involvement in progressive systemic sclerosis.
2008 Jan
Gateways to clinical trials. July-August 2008.
2008 Jul-Aug
Alternative splicing and exon duplication generates 10 unique porcine 5-HT 4 receptor splice variants including a functional homofusion variant.
2008 Jun 12
Prucalopride and donepezil act synergistically to reverse scopolamine-induced memory deficit in C57Bl/6j mice.
2008 Mar 5
Synergy between 5-HT4 receptor activation and acetylcholinesterase inhibition in human colon and rat forestomach.
2008 May
A placebo-controlled trial of prucalopride for severe chronic constipation.
2008 May 29
New treatments for irritable bowel syndrome in women.
2008 Nov
[Functional and motor gastrointestinal disorders].
2008 Oct
Gateways to clinical trials.
2008 Oct
Gateways to clinical trials.
2008 Sep
Management of constipation in the elderly: emerging therapeutic strategies.
2008 Sep 7
Gateways to clinical trials.
2009 Apr
Prucalopride: a new drug for the treatment of chronic constipation.
2009 Aug
Safety assessment of prucalopride in elderly patients with constipation: a double-blind, placebo-controlled study.
2009 Dec
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
Selective desensitization of the 5-HT4 receptor-mediated response in pig atrium but not in stomach.
2009 Jan
Motility: prucalopride for chronic constipation.
2009 Jun
Gateways to clinical trials.
2009 Mar
Prucalopride (Resolor) in the treatment of severe chronic constipation in patients dissatisfied with laxatives.
2009 Mar
The use of novel promotility and prosecretory agents for the treatment of chronic idiopathic constipation and irritable bowel syndrome with constipation.
2009 May
Investigations into the binding affinities of different human 5-HT4 receptor splice variants.
2010
Comments on tegaserod trial on irritable bowel syndrome.
2010 Apr
Update on the management of constipation in the elderly: new treatment options.
2010 Aug 9
Psychometric performance and clinical meaningfulness of the Patient Assessment of Constipation-Quality of Life questionnaire in prucalopride (RESOLOR) trials for chronic constipation.
2010 Feb
[New drugs for the treatment of constipation].
2010 Jul
New-generation 5-HT4 receptor agonists: potential for treatment of gastrointestinal motility disorders.
2010 Jun
Psychometric evaluation of a visual analog scale for the assessment of anxiety.
2010 Jun 8
Hyperfunction of muscarinic receptor maintains long-term memory in 5-HT4 receptor knock-out mice.
2010 Mar 4
Emerging pharmacologic therapies for irritable bowel syndrome.
2010 Oct
Efficacy and safety of prucalopride in patients with chronic noncancer pain suffering from opioid-induced constipation.
2010 Oct
Fixed combination of oxycodone with naloxone: a new way to prevent and treat opioid-induced constipation.
2010 Sep
A double-blind, placebo-controlled study of prucalopride in elderly patients with chronic constipation.
2010 Sep
Patents

Patents

Sample Use Guides

Adults: 2 mg once daily with or without food, at any time of the day.
Route of Administration: Oral
Cell shortening and real-time Ca(2+) measurements were processed on field-stimulated intact cardiomyocytes with the selective 5-HT4R agonist, prucalopride (1 uM).
Substance Class Chemical
Created
by admin
on Fri Dec 15 16:38:52 GMT 2023
Edited
by admin
on Fri Dec 15 16:38:52 GMT 2023
Record UNII
0A09IUW5TP
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PRUCALOPRIDE
EMA EPAR   INN   MART.   MI   USAN   WHO-DD  
INN   USAN  
Official Name English
R-093877
Code English
PRUCALOPRIDE [EMA EPAR]
Common Name English
PRUCALOPRIDE [MI]
Common Name English
R093877
Common Name English
PRUCALOPRIDE [USAN]
Common Name English
4-Amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidyl]-7-benzofurancarboxamide
Systematic Name English
Prucalopride [WHO-DD]
Common Name English
PRUCALOPRIDE [MART.]
Common Name English
prucalopride [INN]
Common Name English
Classification Tree Code System Code
WHO-ATC A03AE04
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
NCI_THESAURUS C47794
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
WHO-ATC A06AX05
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
WHO-VATC QA06AX05
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
Code System Code Type Description
FDA UNII
0A09IUW5TP
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
INN
7702
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
RXCUI
2107310
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
SMS_ID
100000080862
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
DAILYMED
0A09IUW5TP
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
EVMPD
SUB10155MIG
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
NCI_THESAURUS
C74386
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
MESH
C406662
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
DRUG CENTRAL
3502
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
EPA CompTox
DTXSID5057670
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
LACTMED
Prucalopride
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
ChEMBL
CHEMBL117287
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
IUPHAR
243
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
DRUG BANK
DB06480
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
WIKIPEDIA
PRUCALOPRIDE
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
USAN
YY-100
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
MERCK INDEX
m9285
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY Merck Index
CAS
179474-81-8
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
PUBCHEM
3052762
Created by admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
PRIMARY
Related Record Type Details
TRANSPORTER -> SUBSTRATE
EXCRETED UNCHANGED
URINE
TRANSPORTER -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
BINDER->LIGAND
BINDING
CUMULATIVE EXCRETION
FECAL
EXCRETED UNCHANGED
URINE
SALT/SOLVATE -> PARENT
TARGET -> AGONIST
Interaction with the 5-HT4 receptor leads to the elevation of cyclic adenosine monophosphate (cAMP) levels in HEK293 cells
EC50
CUMULATIVE EXCRETION
URINE
BINDER->LIGAND
In human plasma, the binding of R093877 increased at higher pH values. In the pH-range 7.1 to 7.7, the percentage bound increased from 23.3% to 35.5%
BINDING
SALT/SOLVATE -> PARENT
Related Record Type Details
METABOLITE -> PARENT
Seven metabolites were recovered in urine and feces, with the most abundant metabolite R107504 (O-desmethyl prucalopride acid) accounting for 3.2% and 3.1% of the dose in urine and feces, respectively.
FECAL; URINE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC ROUTE OF ADMINISTRATION
PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC DOSE
PHARMACOKINETIC
ROUTE OF ADMINISTRATION
PHARMACOKINETIC
BREAST MILK/PLASMA RATIO PHARMACOKINETIC COMMENTS
PHARMACOKINETIC