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
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)
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 |
---|---|---|
Treatment of GI dysmotility in scleroderma with the new enterokinetic agent prucalopride. | 2002 Jan |
|
Presynaptic modulation of cholinergic neurotransmission in the human proximal stomach. | 2002 Jan |
|
Irritable bowel syndrome: an overview of diagnosis and pharmacologic treatment. | 2003 Jun |
|
Gateways to clinical trials. | 2003 May |
|
Gateways to clinical trials. | 2003 Oct |
|
Gastrointestinal motility disorders and gastrointestinal prokinetic therapy. | 2003 Sep |
|
Effect of enterokinetic prucalopride on intestinal motility in fast rats. | 2003 Sep |
|
New and emerging treatment options for chronic constipation. | 2004 |
|
Rationale for using serotonergic agents to treat irritable bowel syndrome. | 2005 Apr 1 |
|
Frontocortical 5-HT4 receptors exert positive feedback on serotonergic activity: viral transfections, subacute and chronic treatments with 5-HT4 agonists. | 2005 Apr 15 |
|
Management of faecal incontinence and constipation in adults with central neurological diseases. | 2006 Apr 19 |
|
Increased cholinergic contractions of jejunal smooth muscle caused by a high cholesterol diet are prevented by the 5-HT4 agonist--tegaserod. | 2006 Feb 23 |
|
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 |
|
Differential effects of 5-hydroxytryptamine4 receptor agonists at gastric versus cardiac receptors: an operational framework to explain and quantify organ-specific behavior. | 2006 Jun |
|
Investigation of serotonin receptors in the isolated penile bulb of rats. | 2006 Nov-Dec |
|
5-HT4 receptor agonists enhance both cholinergic and nitrergic activities in human isolated colon circular muscle. | 2006 Sep |
|
Gateways to clinical trials. July-August 2008. | 2008 Jul-Aug |
|
Prucalopride: the evidence for its use in the treatment of chronic constipation. | 2008 Jun |
|
Alternative splicing and exon duplication generates 10 unique porcine 5-HT 4 receptor splice variants including a functional homofusion variant. | 2008 Jun 12 |
|
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 |
|
Prucalopride. | 2009 |
|
Gateways to clinical trials. | 2009 Apr |
|
Prucalopride: a new drug for the treatment of chronic constipation. | 2009 Aug |
|
Gateways to clinical trials. | 2009 Dec |
|
Translating 5-HT receptor pharmacology. | 2009 Dec |
|
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 |
|
Effect of ICU interventions on gastrointestinal motility. | 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 |
|
Selective serotonin reuptake inhibitors potentiate the rapid antidepressant-like effects of serotonin4 receptor agonists in the rat. | 2010 Feb 16 |
|
[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).
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C47794
Created by
admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
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EMA ASSESSMENT REPORTS |
RESOLOR (AUTHORIZED: CONSTIPATION)
Created by
admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
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Code System | Code | Type | Description | ||
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YY-101
Created by
admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
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PRIMARY | |||
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DTXSID701027749
Created by
admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
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PRIMARY | |||
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4V2G75E1CK
Created by
admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
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9870009
Created by
admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
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SUB28850
Created by
admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
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2107309
Created by
admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
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C152112
Created by
admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
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179474-85-2
Created by
admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
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100000092989
Created by
admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
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CHEMBL117287
Created by
admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
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DBSALT002626
Created by
admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
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4V2G75E1CK
Created by
admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
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ACTIVE MOIETY
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