Cilobamine
Cilobamine is an orally active antidepressant and a dopamine/norepinephrine reuptake inhibitor. Cilobamine increases the levels of Aniline hydroxylase and cytochrome P-450 in rat liver. Cilobamine promotes hypertrophy of the smooth endoplasmic reticulum in rat liver hepatocytes, increases relative liver weight and recoverable microsomal protein. Cilobamine produces stimulant and anxiogenic effects, and does not inhibit monoamine oxidase. Cilobamine can be used in the research of depression.
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- CAS No.: 69429-84-1
- Formule: C17H23Cl2NO
- Masse moléculaire:328.28
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
In Vivo
Cilobamine (100 mg/kg; p.o.; daily; 4 days) induces hepatic drug-metabolizing enzymes and increases relative liver weight in female Charles River CD rats without altering recoverable microsomal protein[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Charles River CD (male, 150-210 g)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg; 100 mg/kg; 300 mg/kg; 100 mg/kg (time-course analysis)
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Administration:p.o.; daily; 4 days; daily; up to 4 days (time-course analysis)
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Result:Showed no significant changes in ethylmorphine N-demethylase activity, aniline hydroxylase activity, cytochrome P-450 content, relative liver weight, or recoverable microsomal protein compared to controls at 3 mg/kg.
Significantly increased ethylmorphine N-demethylase activity; showed no significant changes in aniline hydroxylase activity, cytochrome P-450 content, relative liver weight, or recoverable microsomal protein compared to controls at 10 mg/kg.
Significantly increased ethylmorphine N-demethylase and aniline hydroxylase activities; showed no significant changes in cytochrome P-450 content or relative liver weight; decreased recoverable microsomal protein compared to controls at 30 mg/kg.
Significantly increased ethylmorphine N-demethylase activity (8.43 nmol HCHO/min/mg microsomal protein), aniline hydroxylase activity (25.94 nmol p-aminophenol/hr/mg microsomal protein), cytochrome P-450 content (0.96 nmol/mg microsomal protein), and relative liver weight (5.25 g/100 g body weight; control: 4.40 g/100 g body weight) compared to controls; showed no change in recoverable microsomal protein compared to controls at 100 mg/kg.
Revealed prominent hypertrophy of the smooth endoplasmic reticulum in hepatocytes at 100 mg/kg.
Showed ethylmorphine N-demethylase activity peaked after 3 doses, aniline hydroxylase activity peaked after 2 doses, and cytochrome P-450 content plateaued after 2 doses, with slight declines in enzyme activities after subsequent doses during time-course analysis at 100 mg/kg.
Significantly increased ethylmorphine N-demethylase activity, aniline hydroxylase activity, cytochrome P-450 content, relative liver weight (5.63 g/100 g body weight), and recoverable microsomal protein (34.97 mg/g liver wet weight) compared to controls at 300 mg/kg.
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Animal Model:Charles River CD (female, 150-210 g)[1]
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Dosage:100 mg/kg
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Administration:p.o.; daily; 4 days
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Result:Significantly increased ethylmorphine N-demethylase activity (3.35 nmol HCHO/min/mg microsomal protein), aniline hydroxylase activity (16.39 nmol p-aminophenol/hr/mg microsomal protein), cytochrome P-450 content (0.67 nmol/mg microsomal protein), and relative liver weight (4.06 g/100 g body weight) compared to controls.
Showed no change in recoverable microsomal protein compared to controls.
Chemical Information
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CAS No. 69429-84-1
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Masse moléculaire 328.28
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Formule C17H23Cl2NO
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SMILES
ClC1=CC=C(C2(C(C3CCC2CC3)NC(C)C)O)C=C1Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Cilobamine Related Classifications
HY-183457 Related Classifications
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Keywords
- Cilobamine
- 69429-84-1
- Monoamine Transporter
- Dopamine Transporter
- Cytochrome P450
- DAT
- SLC6A3
- CYPs
- atypical depression
- dopamine/norepinephrine reuptake inhibitor
- cytochrome P-450
- ethylmorphine N-demethylase
- hepatic drug-metabolizing enzymes
- aniline hydroxylase
- male Charles River CD rats
- depression
- rat liver
- rat liver hepatocyte smooth endoplasmic reticulum
- Inhibitor
- inhibitor
- inhibit