A class of diuretics which promote aquaresis (the excretion of water without electrolyte loss).
ChEBI ID: 194423
| Member | Definition | Class |
|---|---|---|
| conivaptan | The amide resulting from the formal condensation of 4-[(biphenyl-2-ylcarbonyl)amino]benzoic acid with the benzazepine nitrogen of 2-methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine. It is an antagonist for two of the three types of arginine vasopressin (AVP) receptors, V1a and V2. It is used as its hydrochloride salt for the treatment of hyponatraemia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH). | conivaptan |
| mozavaptan | mozavaptan | |
| tolvaptan | A benzazepine derivative incorporating a benzenedicarboxamide function whch is a selective vasopressin V2 receptor antagonist used to treat euvolemic and hypervolemic hyponatremia. It is also used in the treatment of rapidly progressing autosomal dominant polycystic kidney disease to slow the rate of cyst development and renal insufficiency. Tolvaptan is a racemate consisting of a 1:1 mixture of 5R and 5S stereomers. | tolvaptan |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 1 (0.09) | 18.7374 |
| 1990's | 93 (7.91) | 18.2507 |
| 2000's | 206 (17.52) | 29.6817 |
| 2010's | 627 (53.32) | 24.3611 |
| 2020's | 249 (21.17) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 197 (14.92%) | 5.53% |
| Reviews | 290 (21.97%) | 6.00% |
| Case Studies | 113 (8.56%) | 4.05% |
| Observational | 48 (3.64%) | 0.25% |
| Other | 672 (50.91%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| AR protein | Homo sapiens (human) | Potency | 18.3363 | 4 | 4 |
| caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 3.7578 | 1 | 1 |
| caspase-3 | Homo sapiens (human) | Potency | 3.7578 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 27.5404 | 1 | 1 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 12.1348 | 1 | 2 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 2.4246 | 1 | 3 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 29.8493 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 21.8697 | 3 | 3 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 26.6032 | 1 | 1 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 18.0396 | 3 | 6 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 24.8161 | 3 | 3 |
| G | Vesicular stomatitis virus | Potency | 27.5404 | 1 | 1 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 13.9119 | 2 | 3 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 11.9856 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 27.5404 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 27.5404 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 27.5404 | 1 | 1 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 29.7981 | 2 | 2 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 5.9553 | 1 | 1 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 6.4356 | 2 | 2 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 33.4889 | 1 | 1 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 0.2985 | 1 | 1 |
| progesterone receptor | Homo sapiens (human) | Potency | 21.1317 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 13.3332 | 1 | 1 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 18.9408 | 3 | 5 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 26.8325 | 2 | 2 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 31.0990 | 1 | 2 |
| TDP1 protein | Homo sapiens (human) | Potency | 21.1360 | 2 | 2 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 25.1566 | 2 | 2 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 0.0169 | 1 | 1 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 3.7902 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 9.9900 | 1 | 1 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Oxytocin receptor | Homo sapiens (human) | Ki | 0.6600 | 1 | 1 |
| Oxytocin receptor | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Vasopressin V1a receptor | Homo sapiens (human) | IC50 | 0.6383 | 4 | 7 |
| Vasopressin V1a receptor | Rattus norvegicus (Norway rat) | IC50 | 3.2000 | 2 | 2 |
| Vasopressin V1a receptor | Homo sapiens (human) | Ki | 0.1309 | 4 | 4 |
| Vasopressin V1b receptor | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| Vasopressin V1b receptor | Rattus norvegicus (Norway rat) | IC50 | 5.0000 | 1 | 1 |
| Vasopressin V1b receptor | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| Vasopressin V2 receptor | Homo sapiens (human) | IC50 | 0.3147 | 5 | 8 |
| Vasopressin V2 receptor | Homo sapiens (human) | Ki | 0.0036 | 6 | 7 |
| Vasopressin V2 receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0120 | 1 | 1 |