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Drug-Target Interaction

Drug

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PubChem ID:2145
Structure:
Synonyms:
( inverted question mark)-p-Aminoglutethimide
(+-)-3-(p-Aminophenyl)-3-ethyl-2,6-piperidinedione
(+/-)-p-AMINOGLUTETHIMIDE
(?)-p-Aminoglutethimide
.alpha.-(p-Aminophenyl)-.alpha.-ethylglutarimide
125-84-8
2,6-Piperidinedione, 3-(4-aminophenyl)-3-ethyl-
2-(p-Aminophenyl)-2-ethylglutarimide
3-(4-Aminophenyl)-3-ethyl-2,6-piperidindion
3-(4-Aminophenyl)-3-ethyl-2,6-piperidinedione
3-(4-aminophenyl)-3-ethylpiperidine-2,6-dione
3-(p-Aminophenyl)-3-ethylpiperidine-2,6-dione
3-Ethyl-3-(p-aminophenyl)-2,6-dioxopiperidine
5-22-13-00297 (Beilstein Handbook Reference)
A 9657
A1947
A9657_SIGMA
AB00051935
AC-12456
AC1L1D0R
AC1Q2SPJ
AG-1
AKOS004120070
alpha-(p-Aminophenyl)-alpha-ethylglutarimide
Aminoglutethimide
aminoglutethimide (AG)
Aminoglutethimide (USP/INN)
Aminoglutethimide [BAN:INN]
Aminoglutethimide [INN:BAN]
Aminoglutethimidum
Aminoglutethimidum [INN-Latin]
Aminoglutetimida
Aminoglutetimida [INN-Spanish]
Ba 16038
Ba-16038
BB_SC-1153
BPBio1_000032
BRD-A25234499-001-05-0
BRN 0210656
BSPBio_000028
BSPBio_001832
C 16038-BA
C07617
C13H16N2O2
CCG-38911
CCRIS 7562
CHEBI:2654
CHEMBL488
Ciba Vision Brand of Aminoglutethimide
CPD-10532
CPD000326785
Cytadren
Cytadren (TN)
D000616
D00574
DB00357
DivK1c_000884
DL-AMINOGLUTETHIMIDE
EINECS 204-756-4
Elipten
EU-0100124
Glutarimide, 2-(p-aminophenyl)-2-ethyl-
Glutethimide, para-amino
HMS1568B10
HMS1920C09
HMS2090I05
HMS2091I09
HMS2095B10
HMS2231M19
HMS3259H10
HMS3260I10
HMS502M06
HSDB 7494
IDI1_000884
KBio1_000884
KBio2_000400
KBio2_002968
KBio2_005536
KBio3_001332
KBioGR_000588
KBioSS_000400
Lopac0_000124
LS-72014
MLS000859924
MLS001213216
NCGC00015110-02
NCGC00015110-03
NCGC00015110-04
NCGC00015110-05
NCGC00015110-06
NCGC00015110-07
NCGC00093615-01
NCGC00093615-02
NCGC00093615-03
NCGC00093615-04
NCGC00093615-05
NCI60_002900
NINDS_000884
Novartis Brand of Aminoglutethimide
NSC330915
Orimeten
p-Aminoglutethimide
Prestwick0_000244
Prestwick1_000244
Prestwick2_000244
Prestwick3_000244
Prestwick_243
S1672_Selleck
SAM002589964
SBB000711
SMP1_000017
SMR000326785
SPBio_000046
SPBio_002247
SPECTRUM1500115
Spectrum2_000093
Spectrum3_000296
Spectrum4_000144
Spectrum5_000802
Spectrum_000040
STK802074
UNII-0O54ZQ14I9
VU0243029-3
ATC-Codes:
Side-Effects:
Side-EffectFrequency
rash0
vomiting0
somnolence0
allergic alveolitis0
orthostasis0
pancytopenia0
hirsutism0
nausea0
anorexia0
adrenal insufficiency0
myalgia0
hypotension0
leukopenia0
cancer0
tachycardia0
urticaria0
fever0
hypersensitivity0
neutropenia0
dizziness0
pruritus0
hemolytic anemia0
agranulocytosis0
goiter0
anemia0
hypothyroidism0
masculinization0
headache0

Target

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Uniprot ID:CP19A_RAT
Synonyms:
Aromatase
CYPXIX
Cytochrome P450 19A1
Estrogen synthetase
P-450AROM
EC-Numbers:1.14.14.1
Organism:Rat
Rattus norvegicus
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----
--6200-
---260
--34000-

References:

8142297
Effect of aromatase inhibitors on estrogen 2-hydroxylase in rat liver.. H S Purba; E J King; P Richert; A S Bhatnagar (1994) The Journal of steroid biochemistry and molecular biology display abstract
The effect of aromatase inhibitors, 4-hydroxyandrostenedione, CGS 16949A and aminoglutethimide on the inhibition of estrogen 2-hydroxylase activity in rat liver microsomes in vitro and on its induction in vivo has been examined. Estrogen 2-hydroxylase was found to have over twice the affinity for estradiol compared to estrone. Using high pressure liquid chromatography and employing estradiol as a substrate, the IC50 values were 2.2, 98, 110 and 908 microM for the reference compound ketoconazole and the aromatase inhibitors, 4-hydroxyandrostenedione, CGS 16949A and aminoglutethimide, respectively. Similar IC50 values were obtained using estrone as a substrate and by a tritiated water method employing estradiol as a substrate. The Km value for estrogen 2-hydroxylase with estradiol as a substrate using a tritiated water method was 4.3 microM with a Vmax of 11.89 nmol/h/mg. Ketoconazole, CGS 16949A and aminoglutethimide exhibited non-competitive inhibition whereas 4-hydroxyandrostenedione appeared to be a competitive inhibitor of estrogen 2-hydroxylase. The Ki values were 2.6, 72, 114 and 958 microM for ketoconazole, 4-hydroxyandrostenedione, CGS 16949A and aminoglutethimide, respectively. All three aromatase inhibitors were weak inhibitors of estrogen 2-hydroxylase as compared to the reference drug, ketoconazole. Following treatment of rats with aminoglutethimide (40 mg/kg/day; i.p.; for 3 days), estrogen 2-hydroxylase activity was increased by 28 and 30% using estradiol and estrone as substrates, respectively. Following treatment of rats with CGS 16949A (2 mg/kg/day; p.o.; for 3 days), the corresponding increase in estrogen 2-hydroxylase activity was 48 and 44%. The results of this study indicate that the aromatase inhibitors, aminoglutethimide and CGS 16949A are only weak inhibitors of estrogen 2-hydroxylase activity in vitro and show no evidence of inhibition in vivo. On the contrary, there was some evidence to suggest that both aminoglutethimide and CGS 16949A induce estrogen metabolism following repeated administration. Therefore, aminoglutethimide and CGS 16949A may lower estrogen levels not only by primarily inhibiting their synthesis but also by inducing the metabolism of estrogens.