Target intelligence / Profile preview

Cocaine- and amphetamine-regulated transcript prepropeptide (CART)

Target
CART
Molecular classification
Neuropeptide, Other (precursor protein), Neurotransmitter
01

Overview

Cocaine- and amphetamine-regulated transcript prepropeptide (CART) is a neuropeptide encoded by the CARTPT gene, expressed widely in the central and peripheral nervous systems. It functions as a neurotransmitter or neuromodulator involved in the regulation of reward, feeding, stress, and mood. CART has been found to block the effects of psychostimulants like cocaine and amphetamine when co-administered, and plays a role in energy balance via hypothalamic circuits. Additional functions include neuroprotection—especially against oxidative stress, regulation of cardiovascular function, antinociception (pain modulation), bone remodeling, and CNS development. Preclinical research implicates CART in the pathophysiology or modulation of conditions such as obesity, addiction, neurodegenerative diseases, and mood disorders. While no CART-targeting drugs are clinically available, its role as a functional neuropeptide and its distribution make it a potential target for future therapies and a possible biomarker for certain diseases.

Other names
CART prepropeptideCARTCocaine- and amphetamine-regulated transcript proteinCARTPTCART peptide
02

Mechanism of action

Modulation of neurotransmitter pathways (dopamine, serotonin, GABA, glutamate), endogenous inhibition/augmentation of psychostimulant effects, energy homeostasis regulation (via hypothalamic circuits), antioxidant/mitochondrial protection

03

Biological functions

Regulation of appetite and energy homeostasisReward and addiction circuitryStress responseNeuroprotection and antioxidationRegulation of cardiovascular functionPain modulation (antinociception)Bone remodeling (neuroskeletal biology)CNS developmentMood and emotion regulation (antidepressant/anxiolytic effects)
04

Disease associations

Neurodegenerative disease (e.g., Parkinson's disease)Obesity/metabolic disordersPsychiatric disorders (addiction, depression, anxiety)Cardiovascular disease (potential links)
05

Safety considerations

No major safety data available for clinical usepotential challenges include non-specific CNS effects (arousal, mood modulation, feeding behavior)
06

Interacting drugs

Amphetamine

3 more in the full profile.

07

Biomarkers

Reduced CART peptide levels in cerebrospinal fluid proposed as a potential biomarker for some neurodegenerative diseases (e.g., dementia with Lewy bodies)

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