Nabazenil

Nabazenil is a benzodiazepine derivative drug that was developed in the 1980s. It is most commonly used as an antagonist for the GABA receptor, which is the primary inhibitory neurotransmitter in the human brain. Nabazenil is structurally similar to the benzodiazepine antagonist flumazenil, but has a different mechanism of action and a different spectrum of effects.

Pharmacology

Nabazenil acts as a partial inverse agonist of the benzodiazepine receptor, which means it reduces the activity of the receptor below its normal baseline level. This is in contrast to a full inverse agonist, which would completely inhibit the receptor, and an antagonist, which would simply block the effects of other drugs without affecting the receptor's baseline activity.

Clinical Use

Nabazenil has been studied for potential use in the treatment of epilepsy and anxiety disorders, but has not been widely adopted for these purposes. It has also been investigated as a potential antidote for benzodiazepine overdose, but again, it has not been widely adopted for this use.

Side Effects

The side effects of nabazenil are similar to those of other benzodiazepine antagonists, and can include insomnia, anxiety, agitation, and seizures. These side effects are more likely to occur in individuals who are dependent on benzodiazepines or who have been taking them for a long period of time.

See Also

• Benzodiazepine
• GABA receptor
• Flumazenil
• Epilepsy
• Anxiety disorders

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