CTDP-32476
CTDP-32476 is a dopamine transporter (DAT) inhibitor with antidepressant activity, exhibiting a Ki value of 12 nM for human DAT and moderate affinity for the norepinephrine transporter (NET). CTDP-32476 blocks DAT to increase extracellular dopamine levels, and induces locomotor stimulation and brain-stimulation reward effects in rats. CTDP-32476 is used in research related to drug addiction.
For research use only. We do not sell to patients.
- CAS No.: 928046-68-8
- Formula: C16H25Cl2N
- Molecular Weight:302.28
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
CTDP-32476 (10 nM-100 μM; 60 min) potently binds human DAT expressed in HEK293 cells with a Ki value of 12 nM[1].
CTDP-32476 (10 pM-100 μM; 60 min) is a potent competitive inhibitor of human DAT expressed in HEK293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
CTDP-32476 (0.25-1.0 mg/kg; intravenous injection; daily administration for 3 consecutive days) shows significantly lower rewarding efficacy than psychostimulants[1].
CTDP-32476 (3-20 mg/kg; i.p.; single administration) dose-dependently inhibits schedule-controlled self-administration behavior under a fixed-ratio 2 reinforcement schedule in rats with a history of stimulant exposure[1].
CTDP-32476 (3-20 mg/kg; i.p.; single administration) pretreatment reduces the rewarding efficacy of psychostimulants, with a significant effect at the 20 mg/kg dose[1].
CTDP-32476 (10-20 mg/kg; i.p.; single administration) pretreatment dose-dependently reduces psychostimulant self-administration behavior and total intake in rats with a history of psychostimulant exposure within a certain dose range[1].
CTDP-32476 (10-20 mg/kg; i.p.; once daily for 7 consecutive days) administered chronically during extinction training significantly reduces cue-induced reinstatement of controlled stimulant-seeking behavior in rats with a history of controlled stimulant exposure[1].
CTDP-32476 (10-20 mg/kg; i.p.; single administration or 30 μM; local perfusion into the nucleus accumbens; single administration) systemically induces a slow-onset and sustained elevation of dopamine (DA) levels in the nucleus accumbens[1].
CTDP-32476 (3-10 mg/kg; i.p.; single administration) produces a slow-onset, long-lasting, and dose-dependent increase in locomotor activity in rats following systemic administration[1].
Systemic administration of CTDP-32476 (3-10 mg/kg; i.p.; single dose) produces a slow-onset, long-lasting, and dose-dependent enhancement of brain stimulation reward in rats, which differs from the rapid-onset effect of methylbenzoylecgonine[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Long-Evans (male, initial weight 250-300 g, schedule-controlled intravenous self-administration-trained, tested for substitution under fixed-ratio 2 reinforcement)[1]
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Dosage:0.5 mg/kg
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Administration:i.v.; 3-hour sessions for 7 days
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Result:Did not sustain stable self-administration.
Revealed a statistically significant treatment main effect and time main effect.
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Animal Model:Long-Evans (male, initial weight 250-300 g, psychostimulant self-administration-trained, tested for substitution under progressive-ratio reinforcement)[1]
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Dosage:0.25, 0.5, 1.0 mg/kg
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Administration:i.v.; daily sessions for 3 days
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Result:Produced significantly lower progressive-ratio break points than equivalent doses of psychostimulant at 0.5 mg/kg and 1.0 mg/kg/infusion.
Showed a progressive reduction in break points over the 3 sessions of CTDP-32476 substitution.
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Animal Model:Long-Evans (male, initial weight 250-300 g, schedule-controlled self-administration-trained, tested for pretreatment effects under fixed-ratio 2 reinforcement)[1]
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Dosage:3, 10, 20 mg/kg
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Administration:i.p.; single dose
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Result:Dose-dependently inhibited schedule-controlled self-administration with 10 mg/kg and 20 mg/kg producing statistically significant reductions in target infusions relative to vehicle controls.
Showed no effect on inactive lever responding.
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Animal Model:Long-Evans (male, initial weight 250-300 g, psychostimulant self-administration-trained, tested for pretreatment effects under progressive-ratio reinforcement)[1]
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Dosage:3, 10, 20 mg/kg
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Administration:i.p.; single dose
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Result:Dose-dependently lowered the progressive-ratio break point for psychostimulant self-administration, with 20 mg/kg producing a statistically significant reduction relative to vehicle controls.
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Animal Model:Long-Evans (male, initial weight 250-300 g, psychostimulant self-administration-trained, tested for pretreatment effects on multiple-dose psychostimulant self-administration)[1]
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Dosage:10, 20 mg/kg
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Administration:i.p.; single dose
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Result:Dose-dependently shifted the psychostimulant self-administration dose-response curve downward and shifted the psychostimulant intake dose-response curve downward and to the right, with significant reductions in infusions and intake across all tested psychostimulant doses relative to vehicle controls.
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Animal Model:Long-Evans (male, initial weight 250-300 g, controlled stimulant self-administration-trained, extinguished controlled stimulant-seeking, tested for cue-induced reinstatement after chronic pretreatment)[1]
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Dosage:10, 20 mg/kg
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Administration:i.p.; once daily for 7 days
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Result:Significantly attenuated cue-induced reinstatement of drug-seeking behavior, while a single pretreatment dose did not alter controlled stimulant-primed reinstatement.
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Animal Model:Long-Evans (male, initial weight 250-300 g, drug-naive, tested for locomotor activity)[1]
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Dosage:3, 10 mg/kg
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Administration:i.p.; single dose
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Result:Revealed a statistically significant treatment main effect and time main effect.
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Animal Model:Long-Evans (male, initial weight 250-300 g, implanted with medial forebrain bundle electrodes, trained for brain-stimulation reward)[1]
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Dosage:3, 10 mg/kg
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Administration:i.p.; single dose
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Result:Produced a slow-onset (20-60 min), long-duration (up to 9 h) dose-dependent decrease in brain-stimulation reward thresholds.
Revealed a statistically significant treatment main effect and time main effect.
Chemical Information
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CAS No. 928046-68-8
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Molecular Weight 302.28
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Formula C16H25Cl2N
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SMILES
[C@@H](CC(C)C)(C1=CC=C(Cl)C=C1)[C@]2(CCCCN2)[H].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.
Protocols
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Protocol for Tail Suspension Test (TST)
The Tail Suspension Test is a mouse behavioral assay in which an animal is suspended by the tail in an inescapable position, causing alternating escape-directed activity and immobility; the main readout is immobility time, and antidepressant-like treatments generally reduce immobility compared with vehicle controls. The assay detects behavioral response to acute inescapable stress rather than a molecular event; immobility is interpreted as passive stress-coping behavior, while reduced immobility is used as a predictive screen for antidepressant-like activity, with important limitations related to strain, locomotor activity, and tail-climbing behavior.
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Protocol for Forced Swim Test (FST)
The Forced Swim Test is a rodent behavioral assay in which a mouse or rat is placed in an inescapable cylinder of water, and the main readout is the time spent immobile versus active escape-related behaviors such as swimming or climbing. Reduced immobility after treatment has historically been interpreted as antidepressant-like activity, but the assay should be interpreted as a behavioral response to acute inescapable stress rather than a complete model of human depression.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CTDP-32476 Related Classifications
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