GBR-12935

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GBR-12935[edit | edit source]

Chemical structure of GBR-12935

GBR-12935 is a chemical compound that acts as a potent and selective dopamine reuptake inhibitor. It is primarily used in scientific research to study the dopaminergic system and its role in various neurological disorders.

Chemical Properties[edit | edit source]

GBR-12935 is a piperazine derivative, and its chemical structure is characterized by a piperazine ring linked to a phenyl group and a tropane moiety. The compound is known for its high affinity for the dopamine transporter (DAT), which it inhibits, leading to increased levels of dopamine in the synaptic cleft.

Mechanism of Action[edit | edit source]

GBR-12935 functions by binding to the dopamine transporter, thereby blocking the reuptake of dopamine into the presynaptic neuron. This inhibition results in elevated extracellular concentrations of dopamine, enhancing dopaminergic neurotransmission. This mechanism is similar to that of other dopamine reuptake inhibitors, such as cocaine, but GBR-12935 is more selective and is primarily used in research settings.

Research Applications[edit | edit source]

GBR-12935 is extensively used in neuroscience research to investigate the role of dopamine in the brain. It is particularly useful in studies related to Parkinson's disease, schizophrenia, and addiction. By modulating dopamine levels, researchers can better understand the pathophysiology of these conditions and evaluate potential therapeutic interventions.

Pharmacological Effects[edit | edit source]

The pharmacological effects of GBR-12935 are primarily related to its action on the dopaminergic system. In animal models, it has been shown to increase locomotor activity and produce behavioral effects similar to those of psychostimulants. These effects are valuable for studying the behavioral and neurochemical consequences of altered dopamine transmission.

Safety and Toxicity[edit | edit source]

As a research chemical, GBR-12935 is not intended for human consumption, and its safety profile in humans is not well-established. In laboratory settings, it is handled with care to avoid exposure, and its use is typically restricted to controlled environments.

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Contributors: Prab R. Tumpati, MD