ersentilide: has class II & III activities; RN given refers to (+-)-isomer; structure given in first source; CK-4000 (S- isomer); CK-4001 (R- isomer) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 130400 |
| CHEMBL ID | 99585 |
| SCHEMBL ID | 8781117 |
| MeSH ID | M0175345 |
| Synonym |
|---|
| 125228-82-2 |
| 4-hippm |
| CHEMBL99585 , |
| ersentilide |
| n-[4-(2-hydroxy-3-{2-[4-(3h-imidazol-1-yl)-phenoxy]-ethylamino}-propoxy)-phenyl]-methanesulfonamide |
| bdbm50010833 |
| n-(4-{2-hydroxy-3-[2-(4-imidazol-1-yl-phenoxy)-ethylamino]-propoxy}-phenyl)-methanesulfonamide; hydrochloride |
| n-[4-[2-hydroxy-3-[2-(4-imidazol-1-ylphenoxy)ethylamino]propoxy]phenyl]methanesulfonamide |
| ck 4000 |
| he 93 |
| (+-)-n-(4-(2-hydroxy-3-((2-(4-(1h-imidazol-1-yl)phenoxy)ethyl)amino)propoxy)phenyl)methanesulfonamide |
| ck 3579 |
| 128264-20-0 |
| SCHEMBL8781117 |
| Q15634016 |
| DTXSID30869708 |
| n-{4-[2-hydroxy-3-({2-[4-(1h-imidazol-1-yl)phenoxy]ethyl}amino)propoxy]phenyl}methanesulfonamide |
| methanesulfonamide, n-[4-[2-hydroxy-3-[[2-[4-(1h-imidazol-1-yl)phenoxy]ethyl]amino]propoxy]phenyl]- |
Ersentilide is a benzamide derivative that has been found effective in several intact animal models of arrhythmia.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Ersentilide is a benzamide derivative that has been found effective in several intact animal models of arrhythmia. " | ( The electrophysiologic effects of ersentilide on canine hearts. Beloshapko, G; Lee, JH; Rosen, MR; Rosenshtraukh, L, 1995) | 2.01 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Beta-1 adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 2.4000 | 0.0002 | 1.4681 | 9.0000 | AID42031 |
| Beta-2 adrenergic receptor | Canis lupus familiaris (dog) | IC50 (µMol) | 46.5000 | 0.0001 | 2.4596 | 5.2000 | AID59357 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| beta-adrenergic receptor activity | Beta-1 adrenergic receptor | Homo sapiens (human) |
| beta1-adrenergic receptor activity | Beta-1 adrenergic receptor | Homo sapiens (human) |
| protein binding | Beta-1 adrenergic receptor | Homo sapiens (human) |
| PDZ domain binding | Beta-1 adrenergic receptor | Homo sapiens (human) |
| alpha-2A adrenergic receptor binding | Beta-1 adrenergic receptor | Homo sapiens (human) |
| protein heterodimerization activity | Beta-1 adrenergic receptor | Homo sapiens (human) |
| G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potential | Beta-1 adrenergic receptor | Homo sapiens (human) |
| beta2-adrenergic receptor activity | Beta-2 adrenergic receptor | Canis lupus familiaris (dog) |
| protein homodimerization activity | Beta-2 adrenergic receptor | Canis lupus familiaris (dog) |
| norepinephrine binding | Beta-2 adrenergic receptor | Canis lupus familiaris (dog) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| early endosome | Beta-1 adrenergic receptor | Homo sapiens (human) |
| plasma membrane | Beta-1 adrenergic receptor | Homo sapiens (human) |
| Schaffer collateral - CA1 synapse | Beta-1 adrenergic receptor | Homo sapiens (human) |
| neuronal dense core vesicle | Beta-1 adrenergic receptor | Homo sapiens (human) |
| plasma membrane | Beta-1 adrenergic receptor | Homo sapiens (human) |
| early endosome | Beta-2 adrenergic receptor | Canis lupus familiaris (dog) |
| Golgi apparatus | Beta-2 adrenergic receptor | Canis lupus familiaris (dog) |
| receptor complex | Beta-2 adrenergic receptor | Canis lupus familiaris (dog) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID61258 | Percent change in blood pressure (BP) from control at active dose 0.3-3 mg/kg administered intraperitoneally in anesthetized dogs | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
| AID42031 | Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
| AID59357 | Beta2-receptor selectivity in canine lung tissue in anesthetized dogs | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
| AID61130 | Percent change in FRP from control at active dose 0.3-3 mg/kg administered intraperitoneally | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
| AID230074 | Ratio of number of active animals to number of treated at dose 1.0-10 mg/kg administered intraperitoneally in anesthetized dogs | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
| AID61132 | Percent change in FRP from control at active dose 1.0-10 mg/kg administered intraperitoneally in anesthetized dogs | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
| AID229872 | Ratio of number of active animals to number of treated at dose 0.3-10 mg/kg administered intraperitoneally in Epinephrine-induced model in anesthetized dogs | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
| AID63509 | Concentration at which maximum change in APA95 was observed from control value in anesthetized dogs; The maximum observed change APD95 from control value and concentration at 30 uM when this occurred | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
| AID61276 | Percent change in heart rate (HR) from control at active dose 1.0-10 mg/kg administered intraperitoneally | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
| AID61275 | Percent change in heart rate (HR) from control at active dose 0.3-3 mg/kg administered intraperitoneally in anesthetized dogs | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
| AID63504 | Concentration that causes a 20% increase in APD95 (action potential duration at 95% repolarization) from control value in anesthetized dogs | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
| AID58394 | Ratio of number of active animals to number of treated at dose 0.3-3 mg/kg administered intraperitoneally in PES model in anesthetized dogs; 4/4 | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
| AID61259 | Percent change in blood pressure (BP) from control at active dose 1.0-10 mg/kg administered intraperitoneally in anesthetized dogs | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 9 (100.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 0 (0.00) | 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] | ||
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 (12.15) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 9 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||