GABA antagonist

Overview of GABA antagonists

A GABA antagonist is a type of drug that inhibits the action of GABA, the primary inhibitory neurotransmitter in the central nervous system. These antagonists bind to GABA receptors and block the effects of GABA, leading to increased neuronal excitability.

Mechanism of Action

GABA antagonists work by binding to the GABA receptor and preventing GABA from exerting its inhibitory effects. This can lead to increased neurotransmission and heightened neuronal activity. The primary types of GABA receptors affected by these antagonists are the GABA_A and GABA_B receptors.

Clinical Uses

GABA antagonists are used in research to study the role of GABA in the nervous system. They are also used experimentally to induce seizures in animal models for the study of epilepsy. However, due to their potential to cause seizures, they are not commonly used as therapeutic agents.

Examples of GABA Antagonists

• Bicuculline: A competitive antagonist of the GABA_A receptor, often used in research.
• Gabazine (SR-95531): Another GABA_A receptor antagonist used in scientific studies.
• Picrotoxin: A non-competitive antagonist that blocks the GABA_A receptor channel.

Side Effects

Due to their mechanism of action, GABA antagonists can cause seizures, anxiety, and muscle spasms. These side effects limit their use in clinical settings.

Research Applications

GABA antagonists are valuable tools in neuroscience research. They help scientists understand the role of GABA in synaptic transmission and neural circuits. By blocking GABAergic inhibition, researchers can study the effects of disinhibition on neuronal networks.

See Also

• GABA agonist
• Neurotransmitter
• Inhibitory postsynaptic potential