, Volume 180, Issue 4, pp 1-3
Date: 29 Jun 2005

A proof-of-concept study using [11C]flumazenil PET to demonstrate that pagoclone is a partial agonist

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The GABA-ergic system is central to many anxiety disorders and has therefore received much attention. Benzodiazepines are highly effective anxiolytics, leading to their widespread use clinically. However, benzodiazepines often have unwanted side effects, such as sedation, amnesia and ataxia, in the short term. With longer use, tolerance and dependence associated with withdrawal have led to their use being limited or discouraged (NICE 2004).

The benzodiazepine receptor site lies within the GABA-A receptor complex, the activation of which increases chloride channel opening, thus increasing inhibitory neurotransmission. Compounds that bind to the benzodiazepine receptor site such as diazepam or alprazolam are full agonists and increase inhibitory activity in the brain. It has been known for many years that certain compounds are partial agonists at the benzodiazepine receptor site. Such compounds do not fully activate the GABA-A system to the same extent as a full agonist, even when occupyi