Carvotroline hydrochloride
Carvotroline hydrochloride is an antipsychotic agent and 5-HT2 receptor antagonist, with a Ki value of 211 nM for the 5-HT2 receptor. Carvotroline hydrochloride modulates the activity of the stress-related hypothalamic-pituitary-adrenal axis. Carvotroline hydrochloride exerts a stronger blocking effect on Apomorphine (HY-12723)-induced climbing behavior than on Apomorphine-induced stereotyped behavior. Carvotroline hydrochloride inhibits conditioned avoidance responses in rats and monkeys without inducing catalepsy. Carvotroline hydrochloride can be used in studies related to schizophrenia.
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- CAS No.: 136777-43-0
- Formula: C18H19ClFN3
- Molecular Weight:331.81
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Biological Activity
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5-HT2 Receptor 211 nM (Ki) |
Carvotroline hydrochloride binds to cortical 5-HT2 receptors with high affinity, with a Ki value of 211 nM, which is 10-fold higher than the affinity of Serotonin (HY-B1473A) for these receptors[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Carvotroline (10 mg/kg; i.p.; single dose) hydrochloride significantly reduces rotational stress-induced HPA axis activation in male Long-Evans rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Long-Evans (adult male)[2]
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Dosage:0.1 mg/kg; 1 mg/kg; 10 mg/kg; 50 mg/kg
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Administration:i.p.; single dose
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Result:Increased plasma corticosterone levels in a dose-dependent manner, with doses of 10 mg/kg or more raising levels to near ~50 μg/dl (significantly higher than the saline control mean of 14.6 μg/dl).
Reached an ED50 value of 7.0 mg/kg.
Peaked plasma corticosterone levels at 1 hour and returned to control levels by 2 hours after administration of 10 mg/kg.
Did not produce a significant change in plasma corticosterone levels compared to control at a dose of 1 mg/kg.
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Animal Model:Long-Evans (adult male)[2]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Significantly decreased plasma corticosterone levels below the saline-stress control level (normalized to 100%) when measured 2 hours after administration.
Showed no significant effect on stress-induced corticosterone levels 30 minutes after administration.
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Animal Model:Long-Evans (adult male; HPA axis suppressed by 0.1 mg/kg dexamethasone i.p. 7 hours prior)[2]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Reduced carvotroline-induced HPA axis activity by 95.8% via dexamethasone pretreatment, significantly lowering plasma corticosterone levels from the saline-drug treatment group levels.
Chemical Information
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CAS No. 136777-43-0
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Molecular Weight 331.81
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Formula C18H19ClFN3
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SMILES
FC1=CC2=C(NC3=C2CN(CC3)CCC4=CC=NC=C4)C=C1.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Carvotroline hydrochloride Related Classifications
HY-106898A Related Classifications
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