Home
Drugs
Targets
Pathways
Ontologies
Cyp450s
Adv.search
Help/FAQ

Drug-Target Interaction

Drug

show drug details
PubChem ID:4927
Structure:
Synonyms:
(2-Dimethylamino-2-methyl)ethyl-N-dibenzoparathiazine
(Dimethylamino-2-propyl-10-phenothiazine hydrochloride
10-(2-(Dimethylamino)-2-methylethyl)phenothiazine
10-(2-(Dimethylamino)propyl)phenothiazine
10-(2-Dimethylaminopropyl)phenothiazine
10-[2-(Dimethylamino)propyl]phenothiazine
10H-Phenothiazine-10-ethanamine, N,N,.alpha.-trimethyl-
10H-Phenothiazine-10-ethanamine, N,N,alpha-trimethyl-
10H-Phenothiazine-10-ethanamine, N,N,alpha-trimethyl- (9CI)
10h-phenothiazine-10-ethanamine, n,n,alpha-trimethyl-, radical ion(1)
10H-Phenothiazine-10-ethanamine, N,N,alpha-trimethyl-, radical ion(1+)
3277 RP
3389 R.p.
38878-40-9
4-27-00-01253 (Beilstein Handbook Reference)
4182 R.p.
60-87-7
73745-50-3
A-91033
AB00053535
AC-15939
AC1L1J92
AIDS-040817
AIDS040817
Allergan
Antiallersin
Aprobit
Atosil
Avomine
BPBio1_000744
BRN 0088554
BSPBio_000676
BSPBio_002777
C07404
C17H20N2S
Camergan
CCG-109848
CCRIS 7056
CHEBI:8461
CHEMBL643
D00494
DB01069
Dimapp
Dimethylamino-isopropyl-phenthiazin
Dimethylamino-isopropyl-phenthiazin [German]
Diphergan
Diprazin
Diprazine
Diprozin
DivK1c_000005
EINECS 200-489-2
Fargan
Fenazil
Fenergan
Fenetazina
Fenetazine
Genphen
Hiberna
Histargan
HMS2089E08
HSDB 3173
IDI1_000005
Iergigan
Isophenergan
Isopromethazine
KBio1_000005
KBio2_001348
KBio2_003916
KBio2_006484
KBio3_001997
KBioGR_001697
KBioSS_001348
L000495
Lercigan
Lergigan
Lilly 01516
Lilly 1516
Lopac0_000899
LS-264
Metaryl
N,N,alpha-Trimethyl-10H-phenothiazine-10-ethanamine
N,N-dimethyl-1-(10H-phenothiazin-10-yl)propan-2-amine
N,N-dimethyl-1-phenothiazin-10-ylpropan-2-amine
N,N-dimethyl-1-phenothiazin-10-ylpropan-2-amine hydrochloride
N-(2'-Dimethylamino-2'-methyl)ethylphenothiazine
N-Dimethylamino-2-methylethyl thiodiphenylamine
NCGC00015817-03
NCGC00015817-04
NCGC00015817-05
NCGC00015817-06
NCGC00015817-08
NCGC00015817-09
NCGC00015817-10
NCGC00015817-11
NCGC00015817-12
NCGC00089735-02
NCGC00089735-03
NCGC00089735-04
NCI-C60673
NCI60_001878
NINDS_000005
NSC 30321
NSC30321
Oprea1_758749
Pelpica
Phargan
Phenargan
Phenergan
Phenerzine
Phenoject-50
Phenothiazine, 10-(2-dimethylaminopropyl)-
Phenothiazine, 10-[2-(dimethylamino)propyl]-
Phensedyl
Pilothia
Pilpophen
Pipolfen
Pipolphen
Pipolphene
Prestwick0_000888
Prestwick1_000888
Prestwick2_000888
Prestwick3_000888
Pro-50
Proazaimine
Proazamine
Procit
Promacot
Promazinamide
Promergan
Promesan
Promet
Prometasin
Prometazin
Prometazina
Prometazina [INN-Spanish]
Prometazine
Prometh
Promethacon
Promethaine
Promethazin
Promethazine
Promethazine (JAN/INN)
PROMETHAZINE (SEE ALSO PROMETHAZINE HYDROCHLORIDE 58-33-3)
Promethazine Hcl
Promethazine Hydrochloride
Promethazine [INN:BAN]
PromethazineHcl
Promethazinum
Promethazinum [INN-Latin]
Promethegan
Promethiazine
Promezathine
Prorex
Protazine
Prothazin
Prothazine
Provigan
PWWVAXIEGOYWEE-UHFFFAOYSA-
Pyrethia
Pyrethiazine
Remsed
Romergan
RP 3277
Rumergan
SKF 1498
SPBio_000799
SPBio_002895
Spectrum2_000840
Spectrum3_001019
Spectrum4_001149
Spectrum5_000977
Spectrum_000868
Synalgos
Tanidil
Thiergan
UNII-FF28EJQ494
Valergine
Vallergine
WLN: T C666 BN ISJ B1Y1&N1&1
WY 509
Zipan-25
ATC-Codes:
Side-Effects:
Side-EffectFrequency
insomnia0
tinnitus0
thrombophlebitis0
thrombocytopenia0
tachycardia0
syncope0
seizures0
purpura0
phlebitis0
nightmares0
nervousness0
torticollis0
tremor0
paralysis0
bradycardia0
photosensitivity0
blurred vision0
agitation0
dry mouth0
venous thrombosis0
erythema0
loss of consciousness0
unconsciousness0
nasal congestion0
leukopenia0
jaundice0
dermatitis0
delirium0
convulsions0
confusion0
ataxia0
asthma0
asthenia0
apnea0
agranulocytosis0
acidosis0
diplopia0
dizziness0
hypotension0
hallucinations0
gangrene0
flushing0
fatigue0
rash0
euphoria0
edema0
dyskinesia0
somnolence0
abscess0

Target

show target details
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:

11936702
Inhibitory effects of H1-antihistamines on CYP2D6- and CYP2C9-mediated drug metabolic reactions in human liver microsomes.. Nu He; Wen-Qi Zhang; Dolores Shockley; Timi Edeki (2002) European journal of clinical pharmacology display abstract
OBJECTIVE: To screen the inhibitory effects of H1-antihistamines on hepatic bufuralol 1'-hydroxylation and on tolbutamide 4-methylhydroxylation in human liver microsomes. METHODS: Bufuralol 1'-hydroxylation and tolbutamide 4-methylhydroxylation were used as index reactions for CYP2D6 and CYP2C9, respectively. The metabolites of both reactions were measured using high-performance liquid chromatography and were used as indicators of whether CYP2D6 or CYP2C9 activities were inhibited or unaffected by the agents. RESULTS: All five H1-antihistamines studied showed a concentration-dependent inhibition of CYP2D6-mediated bufuralol 1'-hydroxylation with 50% inhibitory concentration (IC50) values of 32-109 microM. Cyclizine and promethazine showed inhibitory effects on tolbutamide 4-methylhydroxylation with IC20 values of 85 microM and 88 microM, respectively. Tripelennamine, chlorpheniramine, and diphenhydramine showed no inhibitory effects on CYP2C9. CONCLUSION: All five H1-antihistamines studied inhibited CYP2D6 markedly, but only cyclizine and promethazine inhibited CYP2C9 at concentrations above that usually seen in plasma. Promethazine and chlorpheniramine inhibited CYP2D6 at concentrations that are very close to their therapeutic plasma concentrations. Further studies in humans, especially in poor metabolizers of CYP2D6, will be required to confirm these findings.