Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C17H17N3O |
Molecular Weight | 279.3364 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C=C(C(=O)[C@@H]2CCC3=C(C2)N=CN3)C4=C1C=CC=C4
InChI
InChIKey=NTHPAPBPFQJABD-LLVKDONJSA-N
InChI=1S/C17H17N3O/c1-20-9-13(12-4-2-3-5-16(12)20)17(21)11-6-7-14-15(8-11)19-10-18-14/h2-5,9-11H,6-8H2,1H3,(H,18,19)/t11-/m1/s1
DescriptionSources: https://www.drugbank.ca/drugs/DB09290Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/21146988 | https://www.ncbi.nlm.nih.gov/pubmed/12195819 | https://www.ncbi.nlm.nih.gov/pubmed/25949526
Sources: https://www.drugbank.ca/drugs/DB09290
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/21146988 | https://www.ncbi.nlm.nih.gov/pubmed/12195819 | https://www.ncbi.nlm.nih.gov/pubmed/25949526
Ramosetron (INN) is a serotonin 5-HT3 receptor antagonist for the treatment of nausea, vomiting. And "diarrhea-predominant irritable bowel syndrome in males" (IBS-D). Ramosetron is licensed for use in India, Japan (Iribo) and selected Southeast Asian countries. In animal studies, ramosetron reduced defecation induced by corticotrophin-releasing hormone and had inhibitory effects on colonic nociception. In two randomized controlled studies including 957 patients with IBS-D, ramosetron increased monthly responder rates of patient-reported global assessment of IBS symptom relief compared with placebo. Ramosetron was also as effective as mebeverine in male patients with IBS-D. In a recent randomized controlled trial with 343 male patients with IBS-D, ramosetron has proved effective in improving stool consistency, relieving abdominal pain/discomfort, and improving health-related quality of life. Regarding safety, ramosetron is associated with a lower incidence of constipation compared with other 5-HT3 receptor antagonists and has not been associated with ischemic colitis.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1899 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21146988 |
0.06 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Iribo Approved UseUnknown |
|||
Primary | Iribo Approved UseUnknown |
|||
Primary | Iribo Approved UseUnknown |
Sample Use Guides
For treatment Nausea and vomiting associated with cancer chemotherapy in Adult: PO 100 mcg once daily. IV 300 mcg once daily. May administer an additional dose of 300 mcg if necessary. Max: 600 mcg/day.
For treatment Irritable bowel syndrome in men PO 5 mcg once daily, may adjust dose according to symptoms. Max: 10 mcg/day.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12195819
Mouse L cells and LV500 cells were washed three times with 1.0 mL of incubation buffer (composition (mm ): 141 NaCl, 4 KCl, 2.8 CaCl2, 1MgSO4, 10 d -glucose, 10 HEPES, pH 7.4).We used the same incubation buffer in the uptake study in all the cell lines. The uptake study was initiated by adding 250 L to multidishes of incubation buffer containing [14C]ramosetron (10 m ) or [3H]vinblastine (30 nm ) in the absence or presence of verapamil (10, 50 and 100 m ) or ciclosporin (20 m ). The cells were incubated at 37° C for a specified time. After incubation, the cells were washed three times with 1.0 mL of ice-cold incubation buffer to terminate the uptake. The cells were solubilized with 3 m NaOH and neutralized with 6 m HCl. [14C]ramosetron or [3H]vinblastine was measured by liquid scintillation counting after addition of scintillation fluid.
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
NCI_THESAURUS |
C267
Created by
admin on Fri Dec 15 16:27:14 GMT 2023 , Edited by admin on Fri Dec 15 16:27:14 GMT 2023
|
||
|
NCI_THESAURUS |
C94726
Created by
admin on Fri Dec 15 16:27:14 GMT 2023 , Edited by admin on Fri Dec 15 16:27:14 GMT 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
DB09290
Created by
admin on Fri Dec 15 16:27:14 GMT 2023 , Edited by admin on Fri Dec 15 16:27:14 GMT 2023
|
PRIMARY | |||
|
7161
Created by
admin on Fri Dec 15 16:27:14 GMT 2023 , Edited by admin on Fri Dec 15 16:27:14 GMT 2023
|
PRIMARY | |||
|
108000
Created by
admin on Fri Dec 15 16:27:14 GMT 2023 , Edited by admin on Fri Dec 15 16:27:14 GMT 2023
|
PRIMARY | |||
|
m9493
Created by
admin on Fri Dec 15 16:27:14 GMT 2023 , Edited by admin on Fri Dec 15 16:27:14 GMT 2023
|
PRIMARY | Merck Index | ||
|
SUB10254MIG
Created by
admin on Fri Dec 15 16:27:14 GMT 2023 , Edited by admin on Fri Dec 15 16:27:14 GMT 2023
|
PRIMARY | |||
|
C61921
Created by
admin on Fri Dec 15 16:27:14 GMT 2023 , Edited by admin on Fri Dec 15 16:27:14 GMT 2023
|
PRIMARY | |||
|
C071315
Created by
admin on Fri Dec 15 16:27:14 GMT 2023 , Edited by admin on Fri Dec 15 16:27:14 GMT 2023
|
PRIMARY | |||
|
132036-88-5
Created by
admin on Fri Dec 15 16:27:14 GMT 2023 , Edited by admin on Fri Dec 15 16:27:14 GMT 2023
|
PRIMARY | |||
|
RAMOSETRON
Created by
admin on Fri Dec 15 16:27:14 GMT 2023 , Edited by admin on Fri Dec 15 16:27:14 GMT 2023
|
PRIMARY | |||
|
DTXSID0043842
Created by
admin on Fri Dec 15 16:27:14 GMT 2023 , Edited by admin on Fri Dec 15 16:27:14 GMT 2023
|
PRIMARY | |||
|
7ZRO0SC54Y
Created by
admin on Fri Dec 15 16:27:14 GMT 2023 , Edited by admin on Fri Dec 15 16:27:14 GMT 2023
|
PRIMARY | |||
|
2357
Created by
admin on Fri Dec 15 16:27:14 GMT 2023 , Edited by admin on Fri Dec 15 16:27:14 GMT 2023
|
PRIMARY | |||
|
100000080335
Created by
admin on Fri Dec 15 16:27:14 GMT 2023 , Edited by admin on Fri Dec 15 16:27:14 GMT 2023
|
PRIMARY | |||
|
CHEMBL1643895
Created by
admin on Fri Dec 15 16:27:14 GMT 2023 , Edited by admin on Fri Dec 15 16:27:14 GMT 2023
|
PRIMARY |
ACTIVE MOIETY
SALT/SOLVATE (PARENT)