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
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)
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.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1875 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11438309 |
8.6 null [pKi] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | RESOLOR Approved UseResolor is indicated for symptomatic treatment of chronic constipation in adults in whom laxatives fail to provide adequate relief Launch Date2008 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
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: |
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%) Other AEs:Headache (1%) Diarrhea (1%) Abdominal pain (1%) Headache (19%) Sources: 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%) |
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 Health Status: healthy Population Size: 60 Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical 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 | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0 |
no | |||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=189 Page: 189.0 |
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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=188 Page: 188.0 |
|||
yes [IC50 4 uM] | ||||
yes [IC50 69 uM] | ||||
yes [IC50 7.8 uM] | ||||
yes [IC50 9.4 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=187 Page: 188;189 |
yes [Km 116 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf#page=187 Page: 188;189 |
yes [Km 15 uM] | |||
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 |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
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
Sample Use Guides
Adults: 2 mg once daily with or without food, at any time of the day.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26427584
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
Edited
Fri Dec 15 16:38:52 GMT 2023
by
admin
on
Fri Dec 15 16:38:52 GMT 2023
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Record UNII |
0A09IUW5TP
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Record Status |
Validated (UNII)
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Record Version |
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-
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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
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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
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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
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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
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0A09IUW5TP
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admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
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7702
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admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
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2107310
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admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
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100000080862
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admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
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0A09IUW5TP
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admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
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SUB10155MIG
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admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
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C74386
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admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
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C406662
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admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
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3502
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admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
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DTXSID5057670
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admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
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Prucalopride
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admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
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CHEMBL117287
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admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
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243
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admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
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DB06480
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admin on Fri Dec 15 16:38:52 GMT 2023 , Edited by admin on Fri Dec 15 16:38:52 GMT 2023
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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
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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
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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
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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
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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
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Related Record | Type | Details | ||
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TRANSPORTER -> SUBSTRATE | |||
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EXCRETED UNCHANGED |
URINE
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TRANSPORTER -> SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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BINDER->LIGAND |
BINDING
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CUMULATIVE EXCRETION |
FECAL
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EXCRETED UNCHANGED |
URINE
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SALT/SOLVATE -> PARENT | |||
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TARGET -> AGONIST |
Interaction with the 5-HT4 receptor leads to the elevation of cyclic adenosine monophosphate (cAMP) levels in HEK293 cells
EC50
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CUMULATIVE EXCRETION |
URINE
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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
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SALT/SOLVATE -> PARENT |
Related Record | Type | Details | ||
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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
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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ROUTE OF ADMINISTRATION PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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DOSE PHARMACOKINETIC PHARMACOKINETIC |
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BREAST MILK/PLASMA RATIO | PHARMACOKINETIC |
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COMMENTS PHARMACOKINETIC |
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