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Drug-Target Interaction

Drug

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PubChem ID:4184
Structure:
Synonyms:
1,2,3,4,10,14b-Hexahydro-2-methyldibenzo(c,f)pyrazino(1,2-a)azepine
2-methyl-1,2,3,4,10,14b-hexahydrodibenzo[c,f]pyrazino[1,2-a]azepine
21535-47-7
21535-47-7 (mono-hydrochloride)
24219-97-4
AC-631
AC1L1HLP
AKOS005216268
Biomol-NT_000135
BPBio1_000064
BPBio1_000331
BRD-A19661776-001-01-5
BRD-A19661776-003-05-2
BRN 0755346
BSPBio_000058
BSPBio_003511
C18H20N2
CCG-204829
CHEBI:51137
CHEMBL6437
D08216
DB06148
Dibenzo(c,f)pyrazino(1,2-a)azepine, 1,2,3,4,10,14b-hexahydro-2-methyl-
Dibenzo[c,f]pyrazino[1,2-a]azepine, 1,2,3,4,10,14b-hexahydro-2-methyl-
DivK1c_000844
EINECS 246-088-6
HMS2089A04
HSDB 7182
IDI1_000844
KBio1_000844
KBio2_002301
KBio2_004869
KBio2_007437
KBio3_003016
KBioGR_001820
KBioSS_002303
L000736
Lerivon
Lopac0_000744
LS-61197
MIANSERIN
Mianserin (INN)
Mianserin hydrochloride
Mianserin Monohydrochloride
Mianserin [INN:BAN]
Mianserina
Mianserina [INN-Spanish]
Mianserine
Mianserine [INN-French]
Mianserinum
Mianserinum [INN-Latin]
Mianseryna
Mianseryna [Polish]
NCGC00015656-04
NCGC00015656-05
NCGC00015656-06
NCGC00015656-08
NCGC00015656-09
NCGC00015656-10
NCGC00024926-03
NCGC00024926-04
NINDS_000844
Norval
Oprea1_703627
Org GB 94
PDSP1_001532
PDSP2_001516
Prestwick0_000099
Prestwick1_000099
Prestwick2_000099
Prestwick3_000099
SPBio_000986
SPBio_001997
Spectrum2_001203
Spectrum3_001836
Spectrum4_001260
Spectrum5_001772
Spectrum_001810
Tolvan
Tolvon
Tolvon (TN)
ATC-Codes:

Target

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Uniprot ID:CP2D6_HUMAN
Synonyms:
CYPIID6
Cytochrome P450 2D6
Debrisoquine 4-hydroxylase
P450-DB1
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:2F9Q
Structure:
2F9Q

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----
----
----
----

References:

10497148
15779673
8764331
9352572
Effects of thioridazine, an inhibitor of CYP2D6, on the steady-state plasma concentrations of the enantiomers of mianserin and its active metabolite, desmethylmianserin, in depressed Japanese patients.. N Yasui; G Tybring; K Otani; K Mihara; A Suzuki; J O Svensson; S Kaneko (1997) Pharmacogenetics display abstract
The antidepressant mianserin is administered as a racemate of the S(+)- and R(-)-enantiomers. Previous in-vitro studies have suggested that CYP2D6 is involved in the stereoselective metabolism of mianserin and its active metabolite, desmethylmianserin. To determine a role for CYP2D6 in vivo, the effects of thioridazine, an inhibitor of CYP2D6, on the steady-state plasma concentrations of the enantiomers of mianserin and desmethylmianserin were examined in 13 depressed Japanese patients. All patients were taking 30 mg of racemic mianserin at bedtime for 8-50 days. Thioridazine (40 mg/day) was coadministered for 1 week, and blood samplings were performed before and after thioridazine coadministration, 12 h after bedtime dosing. Plasma concentrations of the enantiomers of mianserin and desmethylmianserin were measured by HPLC, and the CYP2D6 genotype was determined by allele-specific PCR analysis. Thioridazine significantly increased plasma concentration of S(+)-mianserin (mean SD: 78.2 +/- 35.0 vs. 150.8 +/- 48.7 nM, P < 0.001), but not R(-)-mianserin (39.8 +/- 21.2 vs. 39.5 +/- 20.6 nM, NS). Thioridazine also significantly increased plasma concentrations of both S-desmethylmianserin (11.9 +/- 2.8 vs. 24.4 +/- 10.7 nM, P < 0.01) and R-desmethylmianserin (42.6 +/- 28.4 vs. 115.6 +/- 36.9 nM, P < 0.001). One patient homozygous for the defective allele CYP2D6*5 had the second highest and highest plasma concentrations of S(+)-mianserin and R-desmethylmianserin, respectively, before thioridazine coadministration, and exhibited little increase in plasma concentration of the drugs after thioridazine coadministration. These results suggest that thioridazine specifically inhibits the metabolism of S(+)-mianserin and R-desmethylmianserin, probably through inhibition of CYP2D6, but not R(-)-mianserin.