Gabazine

Gabazine (also known as SR-95531) is a drug that acts as an antagonist at GABA_A receptors. It is used in scientific research to discriminate between GABA_A receptors and GABA_B receptors, and has also been used to study the shape of the GABA_A receptor protein. Gabazine has been found to have a high affinity for the GABA_A receptor, which means it binds strongly to the receptor and blocks the action of GABA, the main inhibitory neurotransmitter in the brain.

Pharmacology

Gabazine is a competitive antagonist for the GABA_A receptor. This means it competes with GABA for the same binding site on the receptor. When gabazine binds to the GABA_A receptor, it prevents GABA from binding to the receptor and thus inhibits the action of GABA. This results in an increase in neuronal activity, as the inhibitory effects of GABA are blocked.

Uses in Research

Gabazine is commonly used in neuroscience research to study the function and structure of the GABA_A receptor. It is particularly useful in this regard because it is a selective antagonist for the GABA_A receptor, meaning it does not affect other types of GABA receptors. This allows researchers to study the GABA_A receptor in isolation, without the effects of other receptors confounding the results.

Side Effects

As a GABA_A receptor antagonist, gabazine can increase neuronal activity and potentially cause seizures. However, it is generally considered safe for use in research settings under controlled conditions.

See Also

• GABA_A receptor
• GABA_B receptor
• Neurotransmitter
• Seizure

References

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