Canrenone: A synthetic pregnadiene compound with anti-aldosterone activity. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 13789 |
| CHEMBL ID | 1463345 |
| CHEBI ID | 135445 |
| SCHEMBL ID | 19560 |
| MeSH ID | M0003283 |
| Synonym |
|---|
| AC-1323 |
| AB00825212-04 |
| 11614 r. p. |
| phanurane |
| nsc-261713 |
| 976-71-6 |
| aldadiene |
| sc-9376 |
| canrenone |
| pregna-4,6-diene-21-carboxylic acid, 17-hydroxy-3-oxo-, .gamma.-lactone (17.alpha.)- |
| canrenone (usan) |
| D03363 |
| luvion |
| 17alpha-pregna-4,6-diene-21-carboxylic acid, 17-hydroxy-3-oxo-, gamma-lactone |
| nsc 261713 |
| 11614 r.p |
| canrenone [usan:inn] |
| einecs 213-554-5 |
| canrenonum [inn-latin] |
| 17-hydroxy-3-oxo-17alpha-pregna-4,6-diene-21-carboxylic acid gamma-lactone |
| 17alpha-(2-carboxyethyl)-17beta-hydroxyandrosta-4,6-dien-3-one lactone |
| canrenona [inn-spanish] |
| pregna-4,6-diene-21-carboxylic acid, 17-hydroxy-3-oxo-, gamma-lactone (17alpha)- |
| brn 0046602 |
| aldadiene (van) |
| NCGC00095148-01 |
| MLS001304014 |
| smr000539206 |
| MLS001163777 |
| CHEBI:135445 |
| HMS2090K21 |
| MLS001304154 |
| (8r,9s,10r,13s,14s,17r)-10,13-dimethylspiro[2,8,9,11,12,14,15,16-octahydro-1h-cyclopenta[a]phenanthrene-17,5'-oxolane]-2',3-dione |
| (10r,13s,17r)-10,13-dimethylspiro[2,8,9,11,12,14,15,16-octahydro-1h-cyclopenta[a]phenanthrene-17,5'-oxolane]-2',3-dione |
| (8r,9s,10r,13s,14s,17r)-10,13-dimethyl-1,8,9,10,11,12,13,14,15,16-decahydro-3'h-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'(2h,4'h)-dione |
| STK801874 |
| AKOS005622473 |
| sc14266 |
| sc9376 |
| canrenona |
| canrenonum |
| 78o20x9j0u , |
| ec 213-554-5 |
| unii-78o20x9j0u |
| 5-17-11-00476 (beilstein handbook reference) |
| HMS2870D16 |
| BBL010921 |
| dtxsid3045930 , |
| tox21_111451 |
| cas-976-71-6 |
| dtxcid1025930 |
| spironolactone impurity f [ep impurity] |
| canrenone [mi] |
| canrenone [who-dd] |
| canrenone [inn] |
| canrenone [usan] |
| canrenone [mart.] |
| 2r)-3,4-dihydro-5h-spiro(androst-4,6-diene-17,2-furan)-3,5-dione |
| CHEMBL1463345 |
| spironolactone metabolite m1 |
| S5273 |
| CCG-220962 |
| AB00825212-06 |
| UJVLDDZCTMKXJK-WNHSNXHDSA-N |
| SCHEMBL19560 |
| tox21_111451_1 |
| NCGC00263479-01 |
| (17?)-17-hydroxy-3-oxopregna-4,6-diene-21-carboxylic acid ?-lactone |
| 20-spiroxa-4,6-diene-3,21-dione |
| mfcd00071735 |
| (1's,2r,2'r,10'r,11's,15's)-2',15'-dimethylspiro[oxolane-2,14'-tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadecane]-6',8'-diene-5,5'-dione |
| canrenone, european pharmacopoeia (ep) reference standard |
| rp-11614 |
| 6,7-dehydro-7a-desthioacetylspironolactone |
| SR-01000813823-2 |
| sr-01000813823 |
| 3-(3-oxo-17b-hydroxy-4,6-androstadien-17a-yl)propionic acid g-lactone |
| 3-(17b-hydroxy-3-oxoandrosta-4,6-dien-17a-yl)propionic acid lactone |
| 17-hydroxy-3-oxo-17a-pregna-4,6-diene-21-carboxylic acid g-lactone |
| 17b-hydroxy-3-oxopregna-4,6-diene-21-carboxylic acid |
| 3-(17b-hydroxy-3-oxoandrosta-4,6-dien-17a-yl)propionic acid g-lactone |
| 3'-(3-oxo-17b-hydroxyandrosta-4,6-dien-17a-yl)-propionic acid lactone |
| 17-hydroxy-3-oxo-17a-pregna-4,6-diene-21-carboxylic acid lactone |
| 17a-(2-carboxyethyl)-17b-hydroxyandrosta-4,6-dien-3-one lactone |
| canrenone, >=97% (hplc) |
| HMS3715A05 |
| CS-0013142 |
| HY-B1438 |
| (8r,9s,10r,13s,14s,17r)-10,13-dimethyl-1,3',4',8,9,10,11,12,13,14,15,16-dodecahydro-5'h-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'(2h)-dione |
| DB12221 |
| NCGC00263479-02 |
| Q5033475 |
| AS-13160 |
| BCP10925 |
| aldadiene;sc9376;sc14266 |
| EN300-123063 |
| (1r,3as,3br,9ar,9bs,11as)-9a,11a-dimethyl-2,3,3a,3b,7,8,9,9a,9b,10,11,11a-dodecahydrospiro[cyclopenta[a]phenanthrene-1,2'-oxolane]-5',7-dione |
| NCGC00263479-06 |
| D95826 |
| 3',4'-dihydrospiro[androst-4,6-diene-17,2'(5'h)-furan]-3,5'-dione (canrenone) |
| pregna-4,6-diene-21-carboxylic acid, 17-hydroxy-3-oxo-, g-lactone,(17a)- |
| (17a)-17-hydroxy-3-oxopregna-4 |
| 6-diene-21-carboxylic acid ?-lactone |
| Z1546624239 |
Canrenone is a derivative of spironolactone with lower antiandrogen activity. Canrenone shares with the parent compound the action as a partial agonist with respect to ouabain on the Na+-K+ ATPase.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Canrenone is a derivative of spironolactone with lower antiandrogen activity. " | ( Aldosterone receptor blockers spironolactone and canrenone: two multivalent drugs. Armanini, D; Bordin, L; Clari, G; Donà, G; Sabbadin, C, 2014) | 2.1 |
| "Canrenone is a major active metabolite of spironolactone and, in addition to the antimineralocorticoid effect, shares with the parent compound the action as a partial agonist with respect to ouabain on the Na+-K+ ATPase. " | ( Effects of canrenone on aorta and right ventricle of the rat. Bova, S; Cargnelli, G; Debetto, P; Luciani, S; Trevisi, L, 2001) | 2.14 |
Canrenone has been described as an antihypertensive drug that blocks endogenous ouabain effects in volume-dependent hypertensive models. Canrenone is reported to be a partial agonist of ou abain.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Canrenone has been described as an antihypertensive drug that blocks endogenous ouabain effects in volume-dependent hypertensive models. " | ( Small doses of canrenone block the effects of ouabain on the mechanical activity of the heart and vessels of the rat. França, A; Rossoni, LV; Stefanon, I; Vassallo, DV; Vassallo, PF, 1998) | 2.1 |
| "Canrenone has been reported to be a partial agonist of ouabain." | ( Hypotensive action of canrenone in a model of hypertension where ouabain-like factors are present. De Mendonca, M; Devynck, MA; Garay, R; Grichois, ML; Meyer, P; Pernollet, MG; Thorman, B, 1985) | 1.31 |
Canrenone treatment was associated with a significant attenuation of LV dilation, better LV diastolic and systolic dynamics, and a marked reduction of reactive fibrosis. Treatment with canrenone from the 10th to the 20th day increases Na-K-ATPase.
| Excerpt | Reference | Relevance |
|---|---|---|
| " However, since haemodialysis patients are prone to hyperkalaemia, a known side effect of spironolactone, this treatment is not used in this population." | ( Safety of low-dose spironolactone administration in chronic haemodialysis patients. Fumeaux, Z; Mach, F; Martin, PY; Perneger, T; Rossier, M; Saudan, P; Schnetzler, B; Stoermann, C, 2003) | 0.32 |
| " More studies are required, however, before concluding that spironolactone administration is safe in the chronic haemodialysis population." | ( Safety of low-dose spironolactone administration in chronic haemodialysis patients. Fumeaux, Z; Mach, F; Martin, PY; Perneger, T; Rossier, M; Saudan, P; Schnetzler, B; Stoermann, C, 2003) | 0.32 |
The harmonic mean of the distributive half-life (t1/2 alpha) of canrenone was found to be 1. A population pharmacokinetic model has been developed to evaluate the pharmacokinetics ofCanrenone in paediatric patients who received potassium canrenoate as part of their therapy in the intensive care unit.
| Excerpt | Reference | Relevance |
|---|---|---|
| " The interaction study was conducted by collecting urine samples after oral administration of spironolactone alone or in combination with YCHT for 5 days." | ( Preclinical study of simultaneous pharmacokinetic and pharmacodynamic herb-drug interactions between Yin-Chen-Hao-Tang and spironolactone. Hsueh, TP; Tsai, TH, 2020) | 0.56 |
The relative bioavailability of 100 mg canrenone capsules and the commercial 50 mg capsules has been determined in 12 healthy male subjects. The absolute bio availability of a pharmacologically active metabolite, canren one, was 57% in the dog and 48% inthe monkey. The influence of food intake on theBioavailability ofCanrenone was explored in 8 healthy male volu.
| Excerpt | Reference | Relevance |
|---|---|---|
| " The absolute bioavailability of a pharmacologically active metabolite, canrenone, was 57% in the dog and 48% in the monkey." | ( Species differences in the metabolism and disposition of spironolactone. Campion, J; Doherty, M; Karim, A; Kook, C; Zagarella, J; Zitzewitz, DJ, ) | 0.36 |
| "The effect of oral neomycin sulfate on the bioavailability of oral spironolactone in humans was studied." | ( Effect of neomycin on the bioavailability of spironolactone: a single-dose study. Bartle, WR; Coates, PE; Fisher, MM; Louman, FJ, 1979) | 0.26 |
| "The investigations have been performed to determine the relative bioavailability of canrenon from Acelat 100 capsules in comparison with canrenon from a spironolactone standard preparation available on the German market." | ( [Relative bioavailability of a new spironolactone preparation (author's transl)]. Erking, W; Lücker, PW; Stöcker, KP; Wetzelsberger, K, 1979) | 0.26 |
| "The influence of food intake on the bioavailability of canrenone, the major and active metabolite of spironolactone, was explored in 8 healthy male volunteers." | ( Enhancement by food of canrenone bioavailability from spironolactone. Danielson, K; Melander, A; Scherstén, B; Thulin, T; Wåhlin, E, 1977) | 0.81 |
| "Data showing a linear relationship between spironolactone dose and the levels of canrenone in plasma and urine are presented to support the use of canrenone levels as a measure of the bioavailability of spironolactone." | ( Validation of plasma and urinary canrenone for determination of bioavailability of spironolactone--comparison of tablets with solution/suspension. Palmer, RF; Ramsay, LE; Shelton, JR; Tidd, MJ, 1977) | 0.76 |
| "Tablet formulations of spironolactone with hydrochlorothiazide were studied in vitro and in vivo to evaluate the effect of formulation parameters on the bioavailability of spironolactone." | ( In vitro and in vivo availability of spironolactone from oral dosage forms. Chao, AY; Karim, A; Mattes, K; Nicholova, B; Sanvordeker, DR; Zagarella, J, 1976) | 0.26 |
| "The bioavailability of commercial 25-mg spironolactone tablets and a new tablet preparation containing 100 mg of the drug has been determined in 12 healthy male subjects." | ( Spironolactone. II. Bioavailability. Baltes, BJ; Chao, A; Hutsell, TC; Karim, A; Zagarella, J, 1976) | 0.26 |
| "An intraindividual comparative multiple-dose study (6 days) was carried out under controlled conditions on 10 healthy volunteers in order to establish the bioavailability of bendroflumethiazide (Bft; 3-benzyl-6-trifluoromethyl-7-sulfamyl-3,4-dihydro-1,2,4-benzoth iad iazine-1, 1-oxide), the sum of the fluorogenic metabolites of spironolactone (3-[3-oxo-7-alpha-acetylthio-17 beta-hydroxy-4-androstene-17-alpha-yl]-propionic acid-gamma-lactone) and canrenone, the main spironolactone metabolite from a fixed combination of Bft with spironolactone vs." | ( [Pharmacokinetic studies and bioavailability of bendroflumethiazide in combination with spironolactone]. Nuss, U; Strobel, K; Vergin, H, 1986) | 0.43 |
| "The relative bioavailability of 100 mg canrenone capsules and the commercial 50 mg capsules has been determined in 12 healthy male subjects." | ( [Relative bioavailability in man of 2 pharmaceutical forms of canrenone]. Bres, J; Bressolle, F; Faure, A; Pistre, MC, ) | 0.64 |
| " The absolute bioavailability of canrenone was 25 +/- 9%." | ( Pharmacokinetics of canrenone after oral administration of spironolactone and intravenous injection of canrenoate-K in healthy man. Karras, J; Krause, W; Seifert, W, 1983) | 0.87 |
| "The mean (95% confidence limits) relative bioavailability for SP-COMP (compared with ALD) from steady state serum concentrations of canrenone, 6beta-hydroxyl 7alpha-thiomethyl spironolactone and 7alpha-thiomethyl spironolactone was 310." | ( Improved bioavailability and clinical response in patients with chronic liver disease following the administration of a spironolactone: beta-cyclodextrin complex. Abosehmah-Albidy, AZ; Chrystyn, H; Losowsky, MS; Wong, V; York, P, 1997) | 0.5 |
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
Multiple dosing of 100 mg spironolactone with tau = 12 h, Study II can lead to slightly increased t 1/2 values for both canrenone (18) and canrenoate. Peak levels and areas under the curve forCanrenone in plasma were significantly lower than those for spironOLactone.
| Excerpt | Relevance | Reference |
|---|---|---|
| " Applying a fluorimetric method to both canrenone and canrenoate--the major biologically active metabolites of spironolactone--the two brands were compared in 11 volunteers for the 50 mg, and in 10 volunteers for the 100 mg dosage form." | ( [Comparative study of relative biovailability of several spironolactone formulations in a steady-state test (author's transl)]. Jaeger, H; Rosenthal, J; Specker, M, 1979) | 0.53 |
| "Canrenone can be determined by high-speed liquid chromatography in pharmaceutical dosage forms without interference from common excipients or degradation products." | ( High-speed liquid chromatographic determination of canrenone in pharmaceutical dosage forms. Williamson, DE, 1976) | 1.95 |
| " A therapeutically satisfactory result has been reached with the administered dosage of both Canrenon and the comparison group." | ( [Studies on the bioequivalence of canrenone using pharmacokinetic data and clinical effects]. Gopold, B; Schneider, J; Wallnöfer, H, 1987) | 0.55 |
| " Our findings are contrary to the widely accepted belief that spironolactone is metabolized too rapidly to be detected in serum after oral dosing and that canrenone is the principal metabolite of spironolactone." | ( New insights into the pharmacokinetics of spironolactone. Hermens, WA; Merkus, FW; Overdiek, HW, 1985) | 0.47 |
| " However, these differences between the two age groups diminished after multiple dosing on Day 8, and the steady state pre-dose plasma levels of canrenone and 'total metabolites' were significantly higher in the elderly subjects." | ( Comparison of plasma levels of canrenone and metabolites after base hydrolysis in young and elderly subjects following single and multiple doses of spironolactone. Bourne, DW; Ho, PC; Smithurst, BA; Triggs, EJ, 1984) | 0.75 |
| " multiple dosing of 100 mg spironolactone with tau = 12 h, Study II) can lead to slightly increased t 1/2 values for both canrenone (18." | ( [Bioavailability studies of two spironolactone-preparations (author's transl)]. Hitzenberger, G; Nuss, U; Schwarzländer, F; Strobel, K; Vergin, H; Weigand, W, 1981) | 0.47 |
| "Better absorption of spironolactone from the spironolactone: beta-cyclodextrin complex formulation should lead to a reduction in dosage and perhaps a more consistent effect in patients with chronic liver disease." | ( Improved bioavailability and clinical response in patients with chronic liver disease following the administration of a spironolactone: beta-cyclodextrin complex. Abosehmah-Albidy, AZ; Chrystyn, H; Losowsky, MS; Wong, V; York, P, 1997) | 0.3 |
| " For investigation of bioequivalence of 2 oral spironolactone formulations, Spironolacton 50 Heumann and Aldactone 50, the pharmacokinetics and bioequivalence of the parent drug and 2 predominant active metabolites, canrenone and 7 alpha-thiomethylspirolactone, were determined in a 2-way crossover study in 24 young healthy male volunteers after multiple oral dosing of 100 mg once daily." | ( Analysis of metabolites--a new approach to bioequivalence studies of spironolactone formulations. Eichinger, A; Mahr, G; Martens, H; Metz, R; Nitsche, V; Vergin, H, 1997) | 0.48 |
| " Misleading subtarget concentrations were repeatedly reported, and falsely guided drug dosing resulted in a case of digoxin intoxication." | ( Intoxication due to negative canrenone interference in digoxin drug monitoring. Eber, B; Emmanuilidis, K; Müller, C; Steimer, W, 1999) | 0.59 |
| " Not only may toxic concentrations remain unidentified, but intoxication could occur should dosage be increased because of falsely low results." | ( Digoxin assays: frequent, substantial, and potentially dangerous interference by spironolactone, canrenone, and other steroids. Eber, B; Müller, C; Steimer, W, 2002) | 0.53 |
| " At equal dosage by weight potassium canrenoate yielded peak levels and areas under the curve for canrenone in plasma which were significantly lower than those for spironolactone, and the peak level of canrenone was reached significantly later." | ( Canrenone--the principal active metabolite of spironolactone? Ramsay, LE; Shelton, JR; Tidd, MJ; Wilkinson, D, 1976) | 1.92 |
| " The data suggest that adjustment of K-canrenoate dosage according to body weight is appropriate in paediatric patients." | ( Population pharmacokinetic model of canrenone after intravenous administration of potassium canrenoate to paediatric patients. Collier, PS; Halliday, HL; Hawwa, AF; Kole, P; McElnay, JC; Millar, M; Millership, JS; Shields, MD; Suyagh, M, 2012) | 0.65 |
| "To evaluate the effects of canrenone as add-on therapy in patients already treated with angiotensin-converting enzyme inhibitors (ACE-I) or angiotensin II receptor blockers (ARBs) and hydrochlorothiazide at the maximum dosage (25 mg/d)." | ( Efficacy and safety of two dosages of canrenone as add-on therapy in hypertensive patients taking ace-inhibitors or angiotensin II receptor blockers and hydrochlorothiazide at maximum dosage in a randomized clinical trial: The ESCAPE-IT trial. Bestetti, A; D'Avino, M; Derosa, G; Felis, S; Gaudio, G; Guasti, L; Maffioli, P; Mugellini, A; Sala, C; Sarzani, R; Vanasia, M; Vulpis, V, 2017) | 1.02 |
| Class | Description |
|---|---|
| steroid lactone | |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 28.1838 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 30.0474 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 21.3138 | 0.1737 | 34.3047 | 61.8120 | AID1346859 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 21.3138 | 0.1737 | 34.3047 | 61.8120 | AID1346859 |
| TDP1 protein | Homo sapiens (human) | Potency | 19.0362 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 6.4029 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
| AR protein | Homo sapiens (human) | Potency | 7.7680 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID1259381; AID743036; AID743040; AID743042; AID743053; AID743054 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 2.6603 | 0.0010 | 22.6508 | 76.6163 | AID1224838 |
| progesterone receptor | Homo sapiens (human) | Potency | 1.7455 | 0.0004 | 17.9460 | 75.1148 | AID1346784; AID1347036 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 10.9640 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 10.6822 | 0.0002 | 14.3764 | 60.0339 | AID720692 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 27.3914 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159555 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 19.1679 | 0.0015 | 30.6073 | 15,848.9004 | AID1224848; AID1224849; AID1259403 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 28.8666 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID743069; AID743075; AID743079 |
| G | Vesicular stomatitis virus | Potency | 27.5404 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 26.8325 | 0.0010 | 19.4141 | 70.9645 | AID743094 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 1.3332 | 0.0237 | 23.2282 | 63.5986 | AID743222 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 18.8336 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 25.1567 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 12.8680 | 0.0006 | 27.2152 | 1,122.0200 | AID743202; AID743219 |
| Vpr | Human immunodeficiency virus 1 | Potency | 63.0957 | 1.5849 | 19.6264 | 63.0957 | AID651644 |
| muscleblind-like protein 1 isoform 1 | Homo sapiens (human) | Potency | 19.9526 | 0.0041 | 9.9625 | 28.1838 | AID2675 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 33.4915 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
| Interferon beta | Homo sapiens (human) | Potency | 27.5404 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 27.5404 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 33.4915 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 27.5404 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 27.5404 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1133846 | Antimineralocorticoid activity in po dosed adrenalectomized rat assessed as urinary log (Na X 10)/K administered post deoxycorticosterone acetate treatment relative to spironolactone | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | Ring D oxygenated Spirolactones. Characterization of human metabolic product of spironolactone. |
| AID74244 | Displacement of [3H]dexamethasone from Glucocorticoid receptor of rabbit kidney | 1993 | Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16 | Synthesis of new 11 beta-substituted spirolactone derivatives. Relationship with affinity for mineralocorticoid and glucocorticoid receptors. |
| AID977599 | Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
| AID126437 | Ratio of [3H]aldosterone binding with 8*10e-8 M aldosterone to [3H]aldosterone binding with 8*10e-8 M competitor at Mineralocorticoid receptor | 1981 | Journal of medicinal chemistry, Sep, Volume: 24, Issue:9 | A structure-activity relationship study of spirolactones. Contribution of the cyclopropane ring to antimineralocorticoid activity. |
| AID126290 | Antagonist activity against Mineralocorticoid receptor after oral administration in Male Sprague Dawley rats; (-) = negative | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | Aldosterone antagonists. 2. Synthesis and biological activities of 11,12-dehydropregnane derivatives. |
| AID126297 | Displacement of [3H]aldosterone from mineralocorticoid receptor | 1981 | Journal of medicinal chemistry, Sep, Volume: 24, Issue:9 | A structure-activity relationship study of spirolactones. Contribution of the cyclopropane ring to antimineralocorticoid activity. |
| AID197642 | Relative anti-androgenic activity as suppressive effect on weight increase of ventral prostate in castrated immature rats given testosterone propionate | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | Aldosterone antagonists. 2. Synthesis and biological activities of 11,12-dehydropregnane derivatives. |
| AID1133847 | Antimineralocorticoid activity in sc dosed adrenalectomized rat assessed as urinary log (Na X 10)/K administered post deoxycorticosterone acetate treatment relative to spironolactone | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | Ring D oxygenated Spirolactones. Characterization of human metabolic product of spironolactone. |
| AID197654 | Relative anti-mineralocorticoid potency compared to Spironolactone after oral administration | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | Aldosterone antagonists. 2. Synthesis and biological activities of 11,12-dehydropregnane derivatives. |
| AID39315 | Relative binding affinity against the androgen receptor in rat renal cytosol using [3H]DHT as ligand | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | Aldosterone antagonists. 2. Synthesis and biological activities of 11,12-dehydropregnane derivatives. |
| AID126421 | Relative binding affinity to the rat mineralocorticoid receptor determined in rat renal cytosol using [3]Ald as ligand | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | Aldosterone antagonists. 2. Synthesis and biological activities of 11,12-dehydropregnane derivatives. |
| AID126299 | Relative binding affinity against mineralocorticoid receptor determined in rat renal cytosol using [3]Ald as ligand | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | Aldosterone antagonists. 2. Synthesis and biological activities of 11,12-dehydropregnane derivatives. |
| AID162616 | Displacement of [3H]promegestone from progestin receptor of rat uterine cytosol at 0 degree Centigrade | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | Aldosterone antagonists. 2. Synthesis and biological activities of 11,12-dehydropregnane derivatives. |
| AID977602 | Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
| AID126285 | Displacement of [3H]aldosterone from mineralocorticoid receptor of rabbit kidney | 1993 | Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16 | Synthesis of new 11 beta-substituted spirolactone derivatives. Relationship with affinity for mineralocorticoid and glucocorticoid receptors. |
| AID126293 | Antagonist activity against Mineralocorticoid receptor after subcutaneous administration in Male Sprague Dawley rats; (+) =positive | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | Aldosterone antagonists. 2. Synthesis and biological activities of 11,12-dehydropregnane derivatives. |
| AID197507 | Relative anti-androgenic activity as suppressive effect on weight increase of seminal vesicle in castrated immature rats given testosterone propionate | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | Aldosterone antagonists. 2. Synthesis and biological activities of 11,12-dehydropregnane derivatives. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1159550 | Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening | 2015 | Nature cell biology, Nov, Volume: 17, Issue:11 | 6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 115 (46.75) | 18.7374 |
| 1990's | 31 (12.60) | 18.2507 |
| 2000's | 33 (13.41) | 29.6817 |
| 2010's | 50 (20.33) | 24.3611 |
| 2020's | 17 (6.91) | 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 very strong demand-to-supply ratio for research on this compound.
| This Compound (57.77) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 39 (14.55%) | 5.53% |
| Reviews | 13 (4.85%) | 6.00% |
| Case Studies | 6 (2.24%) | 4.05% |
| Observational | 1 (0.37%) | 0.25% |
| Other | 209 (77.99%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| Canrenone Effects on Cardiovascular Mortality in Patients With Congestive Heart Failure: the Coffee-it Study [NCT03263962] | 502 participants (Actual) | Observational | 2017-07-13 | Completed | |||
| Clinical Efficacy of Potassium Canrenoate - Canrenone in Sinus Rhythm Restoration Among Patients With Atrial Fibrillation and Elevated Blood Pressure - a Pilot Randomized Controlled Trial. [NCT03536806] | Phase 4 | 80 participants (Anticipated) | Interventional | 2018-06-30 | Not yet recruiting | ||
| Efficacy and Safety of Canrenone as Add-on in Patients With Essential Hypertension-Italy (ESCAPE-IT) [NCT02687178] | Phase 4 | 180 participants (Actual) | Interventional | 2010-10-31 | Completed | ||
| Effects of Mineralocorticoid and AT-1 Receptor Antagonism on the Aldosterone-Renin Ratio (ARR) In Primary Aldosteronism Patients (EMIRA Study): Rationale and Design [NCT04185857] | 50 participants (Actual) | Observational | 2018-01-01 | Completed | |||
| MINECRAFT Study: MINEralcorticoid Receptor Antagonism With CanRenone As eFfective Treatment in Moderate to Severe ARDS in COVID-19, a Phase 2 Clinical Trial. [NCT04977960] | Phase 2 | 180 participants (Anticipated) | Interventional | 2022-09-30 | Not yet recruiting | ||
| Phase 3 Study Of Antiremodeling Effect Of Aldosterone Receptors Blockade With Canrenone In Mild Chronic Heart Failure [NCT00403910] | Phase 3 | 500 participants | Interventional | 2002-09-30 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||