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Drug-Target Interaction

Drug

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PubChem ID:5360696
Structure:
Synonyms:
(
( )-3-Methoxy-N-methylmorphinon
( )-cis-1,3,4,9,10,10a-Hexahydro-6-methoxy-11-methyl-2H-10,4alpha-iminoethanophenanthren
()-3-methoxy-17-methylmorphinan
(+)-3-Methoxy-17-methylmorphinan
(9alpha,13alpha,14alpha)-17-methyl-3-(methyloxy)morphinan
125-69-9
125-71-3
18046-32-7
18609-21-7
3-Methoxy-17-methyl-9alpha,13alpha,14alpha-morphinan
32062-10-5
4-21-00-01367 (Beilstein Handbook Reference)
6700-34-1
9-alpha,13-alpha,14-alpha-Morphinan, 3-methoxy-17-methyl-
9alpha,13alpha,14alpha-Morphinan, 3-methoxy-17-methyl-
9alpha,13alpha,14alpha-Morphinan, 3-methoxy-17-methyl- (8CI)
BA 2666
Benylin DM
BPBio1_000503
BRN 0088549
BSPBio_000457
C18H25NO
Canfodion
Cosylan
Cough-X
d-Methorphan
D03742
DELSYM
delta-Methorphan
Demorphan hydrobromide
Demorphine
Destrometerfano [DCIT]
DEX
Dextromethorfan [Czech]
DEXTROMETHORPHAN
Dextromethorphan (USP)
DEXTROMETHORPHAN POLISTIREX
Dextromethorphan [BAN:INN]
Dextromethorphan [USP:INN:BAN]
Dextromethorphane [INN-French]
Dextromethorphanum [INN-Latin]
Dextrometorfano [INN-Spanish]
Dextromorphan
DIMETANE-DX
Dormetan
EINECS 204-752-2
Hihustan M.
HSDB 3056
l-Methorphan
Levomethorphan
Lopac-D-2531
LS-91838
MLS000758303
Morphinan, 3-methoxy-17-methyl-, (9-alpha,13-alpha,14-alpha)-
Morphinan, 3-methoxy-17-methyl-, (9-alpha,13-alpha,14-alpha)- (9CI)
Morphinan, 3-methoxy-17-methyl-, (9alpha,13alpha,14alpha)-
NCGC00015333-01
NCGC00015333-02
Prestwick0_000359
Prestwick1_000359
Prestwick2_000359
Prestwick3_000359
Racemethorphan
SMR000326694
SPBio_002378
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:

10223772
Comparative in vitro and in vivo inhibition of cytochrome P450 CYP1A2, CYP2D6, and CYP3A by H2-receptor antagonists.. C Martínez; C Albet; J A Agúndez; E Herrero; J A Carrillo; M Márquez; J Benítez; J A Ortiz (1999) Clinical pharmacology and therapeutics display abstract
The isozymes CYP1A2, CYP2D6, and CYP3A4/5 are involved in the majority of all cytochrome P450-mediated drug biotransformations. In this study we investigated the inhibition profiles of CYP1A2 (substrate: caffeine) CYP2D6 (substrate: dextromethorphan), and CYP3A4/5 (substrate: dextrorphan) by cimetidine, ranitidine, and the novel H2-receptor antagonist ebrotidine in human liver microsomes. The inhibitory effect of the drugs on the enzymes activities were as follows: CYP1A2: cimetidine >> ranitidine = ebrotidine; CYP2D6: cimetidine >>> ranitidine = ebrotidine; CYP3A4/5: ebrotidine > cimetidine >>> ranitidine. The inhibition of CYP3A4/5 enzyme activity by ebrotidine was competitive. To test whether the inhibitory effect of ebrotidine in CYP3A activity was also found in vivo, we analyzed the biodisposition of midazolam in 8 healthy volunteers. Midazolam biodisposition was significantly reduced when administered together with cimetidine (P < .05), whereas no significant inhibition was observed with ebrotidine or ranitidine compared with placebo. Psychomotor performance analysis revealed no significant effect of the observed reduction on midazolam biodisposition. We concluded that patients who are receiving treatment with drugs metabolized through CYP3A may experience enhanced drug effects as a result of pharmacokinetic interaction when treated concomitantly with cimetidine. In contrast, the effect of ranitidine or ebrotidine on CYP3A activity in vivo seems to have little clinical significance.
18362694
Pharmacokinetic effect of AMD070, an Oral CXCR4 antagonist, on CYP3A4 and CYP2D6 substrates midazolam and dextromethorphan in healthy volunteers.. Myaing M Nyunt; Stephen Becker; Ron T MacFarland; Priscilla Chee; Robert Scarborough; Stephanie Everts; Gary B Calandra; Craig W Hendrix (2008) Journal of acquired immune deficiency syndromes (1999) display abstract
BACKGROUND: Many antiretroviral drugs used in HIV care involve complex drug metabolism by CYP3A4 and CYP2D6 enzymes, and drug interactions are problematic clinically. AMD070, a novel entry inhibitor, is an inhibitor of X4-tropic HIV virus. In vitro data suggested that it is a CYP3A4 substrate and may inhibit CYP2D6 and CYP3A4. METHODS: Twelve healthy subjects were given a single oral dose of 5 mg of midazolam and 30 mg of dextromethorphan on day 1 and 9, and 200 mg of AMD070 twice daily on days 2 through 9 (inclusive). Pharmacokinetic parameters of midazolam and dextromethorphan were assessed alone and in the presence of AMD070. RESULTS: The mean AUC0-24 and Cmax of dextromethorphan increased 2.86-fold (2.20 to 5.10, 90% confidence interval [CI]) and 2.52-fold (1.99 to 4.24, 90% CI), respectively, in the presence of AMD070. Plasma AUC0-12 of midazolam increased 1.33-fold (1.15 to 1.61, 90% CI) without change in Cmax. The half-life did not change for both drugs, but significant, parallel decrease in apparent oral clearance and volume of distribution was observed. CONCLUSIONS: The data support an alteration in bioavailability due to an AMD070-mediated inhibition of presystemic metabolism, though an intestinal P-glycoprotein effect could also be contributing. Interactions between AMD070 with CYP3A4 and, especially, 2D6 substrates of clinical importance in HIV care should be further explored.