OPC 51803: a nonpeptide vasopressin V(2)-agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 3038506 |
| CHEMBL ID | 332447 |
| SCHEMBL ID | 1943632 |
| MeSH ID | M0364950 |
| Synonym |
|---|
| 1igv6wtk9i , |
| 1h-1-benzazepine-5-acetamide, 1-(2-chloro-4-(1-pyrrolidinyl)benzoyl)-2,3,4,5-tetrahydro-n-(1-methylethyl)-, (r)- |
| 192514-54-8 |
| unii-1igv6wtk9i |
| gtpl2173 |
| sou-003 |
| opc-51803 |
| opc51803 |
| opc 51803 |
| 2-[(r)-1-(2-chloro-4-pyrrolidin-1-yl-benzoyl)-2,3,4,5-tetrahydro-1h-benzo[b]azepin-5-yl]-n-isopropyl-acetamide |
| bdbm50117486 |
| 2-[1-(2-chloro-4-pyrrolidin-1-yl-benzoyl)-2,3,4,5-tetrahydro-1h-benzo[b]azepin-5-yl]-n-isopropyl-acetamide |
| CHEMBL332447 , |
| 2-[(5r)-1-(2-chloro-4-pyrrolidin-1-ylbenzoyl)-2,3,4,5-tetrahydro-1-benzazepin-5-yl]-n-propan-2-ylacetamide |
| DB05838 |
| (5r)-5-isopropylaminocarbonylmethyl-1-[4-(1-pyrrolidinyl)-2-chlorobenzoyl]-2,3,4,5-tetrahydro-1h-benzazepine |
| INGXCNVWWKKWOO-LJQANCHMSA-N , |
| SCHEMBL1943632 |
| DTXSID50172847 |
| 1h-1-benzazepine-5-acetamide, 1-(2-chloro-4-(1-pyrrolidinyl)benzoyl)-2,3,4,5-tetrahydro-n-(1-methylethyl)-, (5r)- |
| (-)-opc-51803 |
| Q27088207 |
| AKOS040749086 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " These results demonstrate that OPC-51803 is a V(2)-selective agonist that produces a significant antidiuretic action after single and multiple oral dosing in AVP-deficient and normal AVP states." | ( Antidiuretic effects of a nonpeptide vasopressin V(2)-receptor agonist, OPC-51803, administered orally to rats. Aoyama, M; Hirano, T; Kondo, K; Mori, T; Nakamura, S; Tominaga, M; Tsujimae, K; Yamamura, Y, 2000) | 0.31 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Vasopressin V2 receptor | Homo sapiens (human) | IC50 (µMol) | 0.3300 | 0.0000 | 1.1213 | 7.0000 | AID217372 |
| Vasopressin V2 receptor | Homo sapiens (human) | Ki | 0.0919 | 0.0004 | 0.4345 | 3.9811 | AID1386896 |
| Vasopressin V1a receptor | Homo sapiens (human) | Ki | 0.8190 | 0.0002 | 0.6235 | 7.0300 | AID1386894 |
| Vasopressin V1b receptor | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 2.0000 | 2.0000 | 2.0000 | AID1386895 |
| Vasopressin V2 receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.2300 | 0.0005 | 0.0638 | 0.5700 | AID217549 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Vasopressin V2 receptor | Homo sapiens (human) | EC50 (µMol) | 0.1890 | 0.0000 | 0.5506 | 6.7000 | AID1386897 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| vasopressin receptor activity | Vasopressin V2 receptor | Homo sapiens (human) |
| protein binding | Vasopressin V2 receptor | Homo sapiens (human) |
| peptide binding | Vasopressin V2 receptor | Homo sapiens (human) |
| vasopressin receptor activity | Vasopressin V1a receptor | Homo sapiens (human) |
| protein kinase C binding | Vasopressin V1a receptor | Homo sapiens (human) |
| protein binding | Vasopressin V1a receptor | Homo sapiens (human) |
| peptide hormone binding | Vasopressin V1a receptor | Homo sapiens (human) |
| V1A vasopressin receptor binding | Vasopressin V1a receptor | Homo sapiens (human) |
| peptide binding | Vasopressin V1a receptor | Homo sapiens (human) |
| vasopressin receptor activity | Vasopressin V1b receptor | Homo sapiens (human) |
| protein kinase C binding | Vasopressin V1b receptor | Homo sapiens (human) |
| peptide binding | Vasopressin V1b receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1386897 | Agonist activity at human V2 receptor expressed in human HeLa cells assessed as stimulation of cAMP accumulation by radioimmunoassay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism. |
| AID217367 | Percentage of maximal cAMP accumulation at a concentration of 10e-6 M was done in HeLa cells expressing the human Vasopressin V2 receptor | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17 | Characterization of orally active nonpeptide vasopressin V(2) receptor agonist. Synthesis and biological evaluation of both the (5R)- and (5S)-enantioisomers of 2-[1-(2-Chloro-4-pyrrolidin-1-yl-benzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin- 5-yl]-N-isopropy |
| AID1386896 | Displacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting method | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism. |
| AID1386894 | Displacement of [3H]-AVP from human V1A receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting method | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism. |
| AID244068 | Agonist activity against Vasopressin V2 receptor relative to Oxytocin receptor at 3 uM | 2004 | Bioorganic & medicinal chemistry letters, Sep-06, Volume: 14, Issue:17 | Non-peptide oxytocin agonists. |
| AID1386895 | Displacement of [3H]-AVP from human V1B receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting method | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism. |
| AID217372 | Binding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determined | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17 | Characterization of orally active nonpeptide vasopressin V(2) receptor agonist. Synthesis and biological evaluation of both the (5R)- and (5S)-enantioisomers of 2-[1-(2-Chloro-4-pyrrolidin-1-yl-benzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin- 5-yl]-N-isopropy |
| AID217549 | Binding affinity against Vasopressin V2 receptor was determined in Brattleboro rats | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17 | Characterization of orally active nonpeptide vasopressin V(2) receptor agonist. Synthesis and biological evaluation of both the (5R)- and (5S)-enantioisomers of 2-[1-(2-Chloro-4-pyrrolidin-1-yl-benzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin- 5-yl]-N-isopropy |
| AID1346432 | Human V1A receptor (Vasopressin and oxytocin receptors) | 2000 | British journal of pharmacology, Apr, Volume: 129, Issue:8 | Characterization of a novel nonpeptide vasopressin V(2)-agonist, OPC-51803, in cells transfected human vasopressin receptor subtypes. |
| AID1346453 | Human V2 receptor (Vasopressin and oxytocin receptors) | 2000 | British journal of pharmacology, Apr, Volume: 129, Issue:8 | Characterization of a novel nonpeptide vasopressin V(2)-agonist, OPC-51803, in cells transfected human vasopressin receptor subtypes. |
| [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 | 0 (0.00) | 18.2507 |
| 2000's | 7 (77.78) | 29.6817 |
| 2010's | 2 (22.22) | 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 (12.30) 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] | ||