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Drug-Target Interaction

Drug

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PubChem ID:2966
Structure:
Synonyms:
)-isoquinoline carboxamidine sulfate;
1,2,3, 4-Tetrahydro-isoquinoline-2-carboxamidine sulfate
1131-64-2
2(1H)-Isoquinolinecarboxamidine, 3,4-dihydro- (7CI,8CI)
2(1H)-Isoquinolinecarboxamidine, 3,4-dihydro-, sulfate (2:1)
2(1H)-Isoquinolinecarboximidamide, 3,4-dihydro-
2(1H)-Isoquinolinecarboximidamide, 3,4-dihydro-, sulfate (2:1)
2-Amidino-1,2,3,4-tetrahydroisoquinoline
3,4-dihydro-1H-isoquinoline-2-carboximidamide
3,4-Dihydro-2(1H)-isoquinoline carboxamidine sulfate
3,4-Dihydro-2(1H)-isoquinolinecarboxamidine
3,4-Dihydro-2(1H)-isoquinolinecarboxamidine sulfate (2:1)
3,4-Dihydro-2(1H)-isoquinolinecarboximidamide
3,4-dihydroisoquinoline-2(1H)-carboximidamide
581-88-4 (SULFATE SALT)
AC1L1EVE
AIDS-156089
AIDS156089
AKOS000225362
BPBio1_000577
BSPBio_000523
C10H13N3
C13650
CAS-581-88-4
CHEBI:34665
CHEMBL169901
D003647
DB04840
Debrisochinum
DEBRISOQUIN
Debrisoquin hemisulfate
Debrisoquin Sulfate
Debrisoquina
Debrisoquina [INN-Spanish]
Debrisoquine
Debrisoquine sulfate
Debrisoquine [INN:BAN]
Debrisoquinum
Debrisoquinum [INN-Latin]
Declinax
EINECS 214-470-1
Equitonil
HMS2089P09
Isocaramidine
Isocaramidine sulfate
Lopac0_000326
LS-172212
NCGC00016513-01
NCGC00016513-02
NCGC00016513-03
NSC139330
NSC139330 (SULFATE SALT)
Prestwick0_000372
Prestwick1_000372
Prestwick2_000372
Prestwick3_000372
RO 5-3307/1
SPBio_002444
STK232096
STOCK5S-37991
Sulfuric acid compound with 3,4-dihydro-2(1H)-isoquinolinecarboximidamide (1:1)
Tendor
UNII-X31CDK040E
ATC-Codes:

Target

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Uniprot ID:Q38LG2_HUMAN
Synonyms:
Cytochrome P450 2D6
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

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

References:

12597994
Interaction of serum proteins with CYP isoforms in human liver microsomes: inhibitory effects of human and bovine albumin, alpha-globulins, alpha-1-acid glycoproteins and gamma-globulins on CYP2C19 and CYP2D6.. Bang Qian Xu; Mikio Ishii; Li Rong Ding; Nancy E Fischer; Tadanobu Inaba (2003) Life sciences display abstract
The effects of serum proteins on the in vitro hydroxylation pathways of mephenytoin (CYP2C19) and debrisoquine (CYP2D6) were studied to enhance the predictability of in vivo drug metabolism from in vitro assays. Both CYP substrates are known to be weakly bound to albumin and the applicability of the free drug hypothesis was further appraised. Since bovine serum albumin (BSA) is used widely in in vitro assays, a comparison between human and bovine proteins was made. Four major serum proteins were studied: albumin, alpha1-acid glycoprotein (AGP), alpha- and gamma-globulins. Human serum albumin (HSA) inhibited both CYP activities about 20% more than BSA. The addition of human alpha-globulins, but not the bovine protein, resulted in marked reduction of 86% and 41% in CYP2C19 and CYP2D6 activities, respectively. This reduction of activity was strikingly greater than the fraction bound (14 and 22%, respectively). The inhibition was of the competitive type and the Ki values of human alpha-globulins on CYP2C19 and CYP2D6 were found to be 0.45% (4.5 mg/ml) and 3.5% (35 mg/ml), respectively. The effect of both human and bovine gamma-globulins on CYP isoforms was negligible. The Ki values of human and bovine AGP for CYP2C19 were 1.84% (420 microM) and 0.93% (210 microM), respectively. For HSA, human alpha-globulins and human and bovine AGP, the strongly decreased CYP activities in vitro cannot be explained by the free drug hypothesis. A direct interaction of these serum proteins with CYP enzymes is postulated. Differential effects of bovine and human serum proteins and CYP specific inhibition were observed.