2. Membrane Transporter/Ion Channel Neuronal Signaling Metabolic Enzyme/Protease
  3. Monoamine Transporter Dopamine Transporter Cytochrome P450
  4. Cilobamine methanesulfonate

Cilobamine methanesulfonate is an orally active antidepressant and a dopamine/norepinephrine reuptake inhibitor. Cilobamine methanesulfonate increases the levels of Aniline hydroxylase and cytochrome P-450 in rat liver. Cilobamine methanesulfonate promotes hypertrophy of the smooth endoplasmic reticulum in rat liver hepatocytes, increases relative liver weight and recoverable microsomal protein. Cilobamine methanesulfonate produces stimulant and anxiogenic effects, and does not inhibit monoamine oxidase. Cilobamine methanesulfonate can be used in the research of depression.

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Cilobamine methanesulfonate

Cilobamine methanesulfonate Chemical Structure

CAS No. : 69429-85-2

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Cilobamine methanesulfonate Related Antibodies

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

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Description

Cilobamine methanesulfonate is an orally active antidepressant and a dopamine/norepinephrine reuptake inhibitor. Cilobamine methanesulfonate increases the levels of Aniline hydroxylase and cytochrome P-450 in rat liver. Cilobamine methanesulfonate promotes hypertrophy of the smooth endoplasmic reticulum in rat liver hepatocytes, increases relative liver weight and recoverable microsomal protein. Cilobamine methanesulfonate produces stimulant and anxiogenic effects, and does not inhibit monoamine oxidase. Cilobamine methanesulfonate can be used in the research of depression.

In Vivo

Cilobamine (3-300 mg/kg; p.o.; daily; 4 days) methanesulfonate dose-dependently induces hepatic drug-metabolizing enzymes in male Charles River CD rats, with significant induction of all measured parameters occurring at 100 and 300 mg/kg, and is approximately 12 times less potent than sodium phenobarbital at achieving 200% of control cytochrome P-450 and ethylmorphine N-demethylase activity levels, and 14 times less potent for aniline hydroxylase activity[1].
Cilobamine (100 mg/kg; p.o.; daily; 4 days) methanesulfonate 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.

Animal Model: Charles River CD (male, 150-210 g)[1]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg; 100 mg/kg; 300 mg/kg; 100 mg/kg (time-course analysis)
Administration: p.o.; daily; 4 days; daily; up to 4 days (time-course analysis)
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.
Animal Model: Charles River CD (female, 150-210 g)[1]
Dosage: 100 mg/kg
Administration: p.o.; daily; 4 days
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.
Molecular Weight

424.38

Formula

C18H27Cl2NO4S
CAS No.
SMILES

O=S(O)(C)=O.ClC1=CC=C(C2(C(C3CCC2CC3)NC(C)C)O)C=C1Cl
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Purity & Documentation
References
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Cilobamine methanesulfonate Related Classifications

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  • Do most proteins show cross-species activity?

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Keywords:

Cilobamine69429-85-2Monoamine TransporterDopamine TransporterCytochrome P450DATSLC6A3CYPsatypical depressiondopamine/norepinephrine reuptake inhibitorcytochrome P-450ethylmorphine N-demethylasehepatic drug-metabolizing enzymesaniline hydroxylasemale Charles River CD ratsdepressionrat liverrat liver hepatocyte smooth endoplasmic reticulumInhibitorinhibitorinhibit

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