Page last updated: 2024-12-08
pumosetrag
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
Pumosetrag: a 5-HT3 receptor agonist MKC-733 on upper gastrointestinal motility in human [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 154104 |
| CHEMBL ID | 1643880 |
| SCHEMBL ID | 390615 |
| MeSH ID | M0510702 |
Synonyms (18)
| Synonym |
|---|
| bdbm50334438 |
| (r)-7-oxo-n-(quinuclidin-3-yl)-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamide |
| pumosetrag |
| ddp733 |
| CHEMBL1643880 , |
| thieno(3,2-b)pyridine-6-carboxamide, n-1-azabicyclo(2.2.2)oct-3-yl-4,7-dihydro-7-oxo-, (r)- |
| unii-1g26b32139 |
| 153062-94-3 |
| n-((3r)-1-azabicyclo(2.2.2)oct-3-yl)-7-oxo-4,7-dihydrothieno(3,2-b)pyridine-6-carboxamide |
| 1g26b32139 , |
| pumosetrag [inn] |
| ddp 733 |
| 1055328-70-5 |
| thieno(3,2-b)pyridine-6-carboxamide, n-(3r)-1-azabicyclo(2.2.2)oct-3-yl-4,7-dihydro-7-oxo- |
| SCHEMBL390615 |
| DTXSID70165211 |
| DB12402 |
| Q27252379 |
Research Excerpts
Pharmacokinetics
| Excerpt | Reference | Relevance |
|---|---|---|
| "A randomized, double-blind, placebo-controlled cross-over study evaluated the pharmacodynamic effects of DDP733 (0." | ( A novel partial 5HT3 agonist DDP733 after a standard refluxogenic meal reduces reflux events: a randomized, double-blind, placebo-controlled pharmacodynamic study. Choung, RS; Dierkhising, RA; Ferguson, DD; Kammer, PP; Landau, SB; Murray, JA; Nurbhai, S; Talley, NJ; Zinsmeister, AR, 2008) | 0.35 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (7)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0001 | 1.7740 | 10.0000 | AID552300 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 9.3000 | 0.0001 | 1.7536 | 10.0000 | AID552299 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 2.0151 | 10.0000 | AID552304 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 2.8005 | 10.0000 | AID552302 |
| Cytochrome P450 2B6 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0011 | 3.4186 | 10.0000 | AID552301 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 2.3983 | 10.0000 | AID552303 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 3A | Homo sapiens (human) | EC50 (µMol) | 0.0073 | 0.0010 | 0.6550 | 3.8000 | AID552107; AID552111 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (50)
Molecular Functions (42)
Ceullar Components (12)
Bioassays (12)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID552107 | Partial agonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as effect on serotonin-induced response | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome. |
| AID552302 | Inhibition of human CYP2C9 | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome. |
| AID552297 | Partial agonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as decrease in 100 uM 5-chloroindole-induced increase in intracellular calcium release at 3 uM relative to 5-HT | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome. |
| AID552110 | Partial agonist activity at human 5HT3A receptor expressed in HEK293 cells at 3 uM relative to 5HT | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome. |
| AID552304 | Inhibition of human CYP2D6 | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome. |
| AID552303 | Inhibition of human CYP2C19 | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome. |
| AID552301 | Inhibition of human CYP2B6 | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome. |
| AID552300 | Inhibition of human CYP1A2 | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome. |
| AID552309 | Partial agonist activity at 5HT3 receptor in po dosed mouse assessed inhibition of serotonin-induced bradycardia administered 1 hr before serotonin challenge by von Bezold-Jarisch reflex test | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome. |
| AID552299 | Inhibition of human CYP3A4 | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome. |
| AID552305 | Intrinsic clearance in human liver microsomes assessed per mg of protein | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome. |
| AID552111 | Partial agonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as decrease in 10 uM 5-chloroindole-induced increase in intracellular calcium release | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (8)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 5 (62.50) | 29.6817 |
| 2010's | 3 (37.50) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 11.84
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (11.84) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 4 (50.00%) | 5.53% |
| Reviews | 1 (12.50%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 3 (37.50%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||