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Drug-Target Interaction

Drug

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PubChem ID:34633
Structure:
Synonyms:
31883-05-3
AB00514710
BAS 01947592
BPBio1_001104
BSPBio_001002
C07743
C22H25N3O4S
Carbamic acid,
Carbamic acid, (10-(3-(4-morpholinyl)-1-oxopropyl)-10H-phenothiazin-2-yl)-, ethyl ester
CAS-31883-05-3
CBDivE_008814
CHEBI:6997
D05077
DB00680
EINECS 250-854-5
EN 313
EN-313
Ethmozin
Ethmozine
Ethyl (10-(3-(4-morpholinyl)-1-oxopropyl)-10H-phenothiazin-2-yl)carbamate
Ethyl 10-(3-morpholinopropionyl)phenothiazine-2-carbamate
ethyl N-[10-(3-morpholin-4-ylpropanoyl)phenothiazin-2-yl]carbamate
ethyl [10-(3-morpholin-4-ylpropanoyl)-10H-phenothiazin-2-yl]carbamate
ethyl {10-[3-(morpholin-4-yl)propanoyl]-10H-phenothiazin-2-yl}carbamate
Etmozin
G 214
LS-50419
MLS001201823
Moracizin
Moracizina
Moracizina [INN-Spanish]
Moracizine
Moracizine (INN)
Moracizinum
Moracizinum [INN-Latin]
Moricizine
Moricizine (USAN)
Moricizine [USAN]
NCGC00016809-01
NCGC00074074-03
Oprea1_682904
Oprea1_701257
Phenothiazine-2-carbamic acid, 10-(3-morpholinopropionyl)-, ethyl ester
Prestwick0_001051
Prestwick1_001051
Prestwick2_001051
Prestwick3_001051
SBB005991
SMR000059585
SPBio_002931
STK370502
TimTec1_000772
ZINC19340795
ATC-Codes:
Side-Effects:
Side-EffectFrequency
sleep disorder0
sweating0
sinusitis0
seizures0
pulmonary embolism0
pruritus0
pharyngitis0
paresthesia0
palpitations0
pain0
nystagmus0
nervousness0
nausea0
myocardial infarction0
jaundice0
impotence0
hypothermia0
swelling0
syncope0
thrombocytopenia0
memory loss0
abnormal gait0
kidney pain0
bradycardia0
blurred vision0
dry skin0
eye pain0
agitation0
urinary retention0
dry mouth0
vomiting0
vertigo0
urticaria0
urinary incontinence0
tremor0
tinnitus0
hypotension0
hypertension0
diarrhea0
dysphagia0
decreased libido0
cough0
constipation0
confusion0
coma0
chest pain0
av block0
atrial fibrillation0
ataxia0
asthma0
asthenia0
apnea0
anxiety0
anorexia0
diplopia0
dizziness0
somnolence0
hepatitis0
congestive heart failure0
heart disease0
cardiac arrest0
headache0
hallucinations0
flatulence0
fever0
fatigue0
rash0
euphoria0
edema0
dysuria0
dyspnea0
dyspepsia0
dyskinesia0
abdominal pain0

Target

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Uniprot ID:CP1A1_HUMAN
Synonyms:
CYPIA1
Cytochrome P450 1A1
P450 form 6
P450-C
P450-P1
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

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

References:

12393941
Moricizine, an antiarrhythmic agent, as a potent inhibitor of hepatic microsomal CYP1A.. Hiroki Konishi; Kunihiko Morita; Tokuzo Minouchi; Akira Yamaji (2002) Pharmacology display abstract
We examined the inhibitory effect of moricizine (MOR) on hepatic cytochrome P-450 (CYP) in mice. Spectrophotometric analysis revealed that MOR had a relatively high affinity for CYP molecules. MOR most potently inhibited the CYP1A1-dependent ethoxyresorufin O-deethylation and the CYP1A2-dependent methoxyresorufin O-demethylation, among the metabolic reactions mediated by CYP1A, CYP2A, CYP2B, CYP2C, CYP2D, CYP2E, and CYP3A subfamilies expressed in untreated and CYP-inducer-treated hepatic microsomes. The inhibition constants (K(i)) for ethoxyresorufin and methoxyresorufin O-dealkylations were 0.43 and 0.98 micromol/l, respectively. These K(i) values were one to three orders of magnitude lower than those of cimetidine (CIM) and mexiletine (MEX) that have been accepted as the clinical inhibitors of CYP1A2 and were below the therapeutic serum concentration of MOR. Theophylline 3-demethylation and 8-hydroxylation in untreated hepatic microsomes, clinical probes for CYP1A2 activities, were subjected to marked and competitive inhibition by MOR with K(i) values similar to that of methoxyresorufin O-demethylation, and the inhibitory potency of MOR was much higher than those of CIM and MEX. In addition, the zoxazolamine paralysis time, an in vivo measure of the hepatic CYP1A2 capacity, was markedly prolonged by pretreatment of mice with MOR rather than CIM and MEX, while the prolonging effect of MOR on the pentobarbital sleeping time, an indicator of the metabolic function of phenobarbital-inducible CYP species, was not so pronounced as compared with the zoxazolamine paralysis time. These results indicate that MOR acts as a potent and preferential inhibitor of hepatic CYP1A enzymes in vitro and in vivo.