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.
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- No. CAS: 928046-68-8
- Fòrmula: C16H25Cl2N
- Peso molecular:302.28
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Actividad biológica
Descripciòn
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[1].
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
CTDP-32476 (0.5 mg/kg; i.v.; administered for 3 h daily for 7 consecutive days) fails to maintain program-controlled intravenous self-administration behavior in rats trained to self-administer a Schedule II psychostimulant[1].
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].
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.
Related Protocols :
Chemical Information
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No. CAS 928046-68-8
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Peso molecular 302.28
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
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Pureza:
99.98%
Assay:
99.98%
ee.:
99.98%
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