DT-Web

DB01134 - Desoxycorticosterone Pivalate


Identification
Name Desoxycorticosterone Pivalate
Accession Number DB01134 (APRD00709)
Type small molecule
Description Desoxycorticosterone Pivalate is a mineralocorticoid hormone and an analog of desoxycorticosterone. It is white, odorless, and stable in air. It is practically insoluble in water, sparingly soluble in acetone, slightly soluble in methanol, ether and vegetable oils. Federal (U.S.A.) law restricts this drug to use by or on the order of a licensed veterinarian.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 414.5775
Groups experimental
Monoisotopic Weight 414.277009704
Pharmacology
Indication Examined for treatment of adrenocortical insufficiency especially in multiple sclerosis, congenital cerebral palsy, polyarteritis nodosa, and rheumatoid arthritis. Currently only approved in treating cats and dogs for the treatment of Addison's disease.
Mechanism of action Desoxycorticosterone Pivalate binds to the mineralocorticoid receptor. Mineralocorticoids are a family of steroids, secreted by the adrenal cortex, necessary for the regulation of a number of metabolic processes including electrolyte regulation. Desoxycorticosterone pivalate exerts its effect through its interaction with the mineralocorticoid receptor (MR), whereby it reacts with the receptor proteins to form a steroid-receptor complex. This complex moves into the nucleus, where it binds to chromatin which results in genetic transcription of cellular DNA to messenger RNA. The steroid hormones appear to induce transcription and synthesis of specific proteins, which produce the physiological effects seen after administration.
Absorption Not Available
Protein binding 90%
Biotransformation Not Available
Route of elimination Not Available
Toxicity Symptoms of overdose include polyuria, polydipsia, increased blood volume, edema, and cardiac enlargement.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


Mineralocorticoid receptor
Name Mineralocorticoid receptor
Gene Name NR3C2
Pharmacological action yes
Actions agonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
  • Beaumont K, Fanestil DD: Characterization of rat brain aldosterone receptors reveals high affinity for corticosterone. Endocrinology. 1983 Dec;113(6):2043-51. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
  • Sekihara H, Island DP, Liddle GW: New mineralocorticoids: 5alpha-dihydroaldosterone and 5alpha-dihydro-11-deoxycorticosterone. Endocrinology. 1978 Oct;103(4):1450-2. - Pubmed
DTHybrid score 0.3906

Predictions


Id Partner name Gene Name Score
146 Androgen receptor AR 0.0588
871 Glucocorticoid receptor NR3C1 0.043
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0405
614 Progesterone receptor PGR 0.0394
364 Corticosteroid 11-beta-dehydrogenase isozyme 1 HSD11B1 0.0327
6228 Nuclear receptor coactivator 1 NCOA1 0.0313
4118 Cytochrome P450 3A5 CYP3A5 0.029
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0275
6107 Cytochrome P450 3A7 CYP3A7 0.0257
4512 Cytochrome P450 3A4 CYP3A4 0.023
380 Cytochrome P450 17A1 CYP17A1 0.0224
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0209
1588 Multidrug resistance protein 1 ABCB1 0.0196
3923 Cholinesterase BCHE 0.014
723 Cytosolic phospholipase A2 PLA2G4A 0.0137
290 Prostaglandin G/H synthase 2 PTGS2 0.0136
232 Corticosteroid-binding globulin SERPINA6 0.0135
4924 Cytochrome P450 2C8 CYP2C8 0.0133
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0129
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0129
4111 Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S 0.0128
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0125
4114 Voltage-dependent L-type calcium channel subunit beta-3 CACNB3 0.0101
4112 Voltage-dependent L-type calcium channel subunit beta-4 CACNB4 0.0101
118 Organic cation/carnitine transporter 2 SLC22A5 0.01
6220 Aryl hydrocarbon receptor AHR 0.0099
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.0096
4113 Voltage-dependent L-type calcium channel subunit alpha-1F CACNA1F 0.0094
333 Voltage-dependent L-type calcium channel subunit beta-1 CACNB1 0.0091
6048 Troponin C, skeletal muscle TNNC2 0.0078
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.0064
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0061
1561 Troponin C, slow skeletal and cardiac muscles TNNC1 0.0056
4160 Voltage-dependent calcium channel subunit alpha-2/delta-2 CACNA2D2 0.0056
964 Voltage-dependent T-type calcium channel subunit alpha-1H CACNA1H 0.005
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.005
4757 Cytochrome P450 2C9 CYP2C9 0.0049
4119 Cytochrome P450 2D6 CYP2D6 0.0048
6141 Sodium/bile acid cotransporter SLC10A1 0.0045
465 Calmodulin CALM1 0.0043
1898 Cytochrome P450 1B1 CYP1B1 0.0037
6147 Solute carrier family 22 member 3 SLC22A3 0.0037
776 Bile salt export pump ABCB11 0.0036
136 Estrogen receptor ESR1 0.0035
862 Multidrug resistance-associated protein 1 ABCC1 0.0032
6144 Solute carrier family 22 member 2 SLC22A2 0.0032
6145 Solute carrier family 22 member 1 SLC22A1 0.0031
5718 Cytochrome P450 2A6 CYP2A6 0.0031
6024 Cytochrome P450 1A1 CYP1A1 0.0029
6016 Cytochrome P450 2C19 CYP2C19 0.0024
4200 Cytochrome P450 1A2 CYP1A2 0.0024
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