DT-Web

DB00288 - Amcinonide


Identification
Name Amcinonide
Accession Number DB00288 (APRD00788)
Type small molecule
Description Amcinonide is a corticosteroid. [Wikipedia]
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 502.5717
Groups approved
Monoisotopic Weight 502.236681679
Pharmacology
Indication For the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.
Mechanism of action The mechanism of the anti-inflammatory activity of the topical steroids, in general, is unclear. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2. Amcinonide has affinity for the glucocorticoid receptor. It has weak affinity for the progesterone receptor, and virtually no affinity for the mineralocorticoid, estrogen, or androgen receptors.
Absorption Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin increase percutaneous absorption.
Protein binding Not Available
Biotransformation Once absorbed through the skin, topical corticosteroids are handled through pharmacokinetic pathways similar to systemically administered corticosteroids. Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys.
Route of elimination Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys. Some of the topical corticosteroids and their metabolites are also excreted into the bile.
Toxicity Results from acute toxicity studies do not indicate that any risk of acute intoxication is to be expected following a single dermal application of an overdose (application over a large area under conditions favorable to absorption) or inadvertent oral ingestion.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


Glucocorticoid receptor
Name Glucocorticoid receptor
Gene Name NR3C1
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
  • Grossman R, Yehuda R, Golier J, McEwen B, Harvey P, Maria NS: Cognitive effects of intravenous hydrocortisone in subjects with PTSD and healthy control subjects. Ann N Y Acad Sci. 2006 Jul;1071:410-21. - Pubmed
  • Rautanen A, Eriksson JG, Kere J, Andersson S, Osmond C, Tienari P, Sairanen H, Barker DJ, Phillips DI, Forsen T, Kajantie E: Associations of body size at birth with late-life cortisol concentrations and glucose tolerance are modified by haplotypes of the glucocorticoid receptor gene. J Clin Endocrinol Metab. 2006 Nov;91(11):4544-51. Epub 2006 Aug 8. - Pubmed
  • Hammer F, Stewart PM: Cortisol metabolism in hypertension. Best Pract Res Clin Endocrinol Metab. 2006 Sep;20(3):337-53. - Pubmed
  • Shaw JR, Gabor K, Hand E, Lankowski A, Durant L, Thibodeau R, Stanton CR, Barnaby R, Coutermarsh B, Karlson KH, Sato JD, Hamilton JW, Stanton BA: Role of glucocorticoid receptor in acclimation of killifish (Fundulus heteroclitus) to seawater and effects of arsenic. Am J Physiol Regul Integr Comp Physiol. 2007 Feb;292(2):R1052-60. Epub 2006 Oct 12. - Pubmed
  • Sher L: Combined dexamethasone suppression-corticotropin-releasing hormone stimulation test in studies of depression, alcoholism, and suicidal behavior. ScientificWorldJournal. 2006 Oct 31;6:1398-404. - Pubmed
DTHybrid score 0.9602
Annexin A1
Name Annexin A1
Gene Name ANXA1
Pharmacological action unknown
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
  • Serres M, Comera C, Schmitt D: Annexin 1 regulation in human epidermal cells. Cell Mol Biol (Noisy-le-grand). 1994 Jul;40(5):701-6. - Pubmed
DTHybrid score 0.4198

Predictions


Id Partner name Gene Name Score
232 Corticosteroid-binding globulin SERPINA6 0.2409
4512 Cytochrome P450 3A4 CYP3A4 0.0929
1588 Multidrug resistance protein 1 ABCB1 0.05
756 Sex hormone-binding globulin SHBG 0.0383
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0364
4118 Cytochrome P450 3A5 CYP3A5 0.034
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0319
4924 Cytochrome P450 2C8 CYP2C8 0.0311
6107 Cytochrome P450 3A7 CYP3A7 0.029
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0255
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0249
614 Progesterone receptor PGR 0.0223
84 Nuclear receptor 0B1 NR0B1 0.0209
737 Mineralocorticoid receptor NR3C2 0.0198
723 Cytosolic phospholipase A2 PLA2G4A 0.0179
3811 Cytochrome P450 19A1 CYP19A1 0.0171
146 Androgen receptor AR 0.0161
6024 Cytochrome P450 1A1 CYP1A1 0.0153
380 Cytochrome P450 17A1 CYP17A1 0.0149
381 Prolactin receptor PRLR 0.0142
6031 Cytochrome P450 3A43 CYP3A43 0.0128
468 Cytochrome P450 4A11 CYP4A11 0.0125
5718 Cytochrome P450 2A6 CYP2A6 0.012
6017 Cholesterol side-chain cleavage enzyme, mitochondrial CYP11A1 0.0118
4119 Cytochrome P450 2D6 CYP2D6 0.0116
2751 Holliday junction ATP-dependent DNA helicase ruvB ruvB 0.0105
4755 Holliday junction ATP-dependent DNA helicase ruvB ruvB 0.0105
1898 Cytochrome P450 1B1 CYP1B1 0.0099
776 Bile salt export pump ABCB11 0.0097
4615 Chain A, Red Copper Protein Nitrosocyanin NE0143 0.0093
7 Nitric oxide synthase, inducible NOS2 0.0092
6016 Cytochrome P450 2C19 CYP2C19 0.0092
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.0081
6030 Cytochrome P450 2B6 CYP2B6 0.0072
6013 Cytochrome P450 2E1 CYP2E1 0.0071
1758 GTPase HRas HRAS 0.0068
4604 Liver carboxylesterase 1 CES1 0.0061
4200 Cytochrome P450 1A2 CYP1A2 0.0061
4757 Cytochrome P450 2C9 CYP2C9 0.0061
6500 Phospholipase A2 PLA2G1B 0.006
136 Estrogen receptor ESR1 0.0052
3923 Cholinesterase BCHE 0.0049
364 Corticosteroid 11-beta-dehydrogenase isozyme 1 HSD11B1 0.0048
290 Prostaglandin G/H synthase 2 PTGS2 0.0048
2300 Lysozyme E 0.0047
3633 Lysozyme R 0.0047
5597 Lysozyme 17 0.0047
862 Multidrug resistance-associated protein 1 ABCC1 0.0031
587 Serum albumin ALB 0.003
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