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benzodiazepine mechanism

Posted by katekite on May 7, 2002, at 13:15:57

In reply to What about Klonopin, Depakote and GABA..., posted by Janelle on May 6, 2002, at 4:46:05

Hi Janelle,

Ok so here's how it works, read thru to the end for new information:

GABA is a neurotransmitter. GABA is the key, it fits into the GABA receptor (lock). GABA receptors are present on the surface of GABA based neurons.

Most GABA based neurons are inhibitory to other neurons. This means when they are activated by GABA, brain activity is slightly inhibited.

This leads to the results of less anxiety, sleepiness, or decrease in seizure (which is extreme overactivity in some part of the brain).

Benzodiazepines such as klonopin are chemicals that bind to a site on the GABA receptor that is NOT the site where GABA binds. (think of it as a big lock) The sites where GABA and benzodiazepines bind are very close to eachother. It is thought that the benzodiazepine binding changes the conformation of the GABA receptor, and this change in shape actually allows GABA to bind more easily.... ie it changes the shape of the lock to fit the key better.

The analogy is instead of jiggling the key in the lock before it turns, it turns smoothly the first time. So basically benzodiazepines are like oil, they lube up the slot where GABA fits.

So with a benzodiazepine like klonopin attached, GABA binds easier and may stay there longer, all of this makes the GABA neuron more likely to be able to send its inhibitory signal.

Hope that helps.

Not sure how depakote works.





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