[Neuroscience] Re: Is it possible to prevent desensitization of GABA-A receptors?

Matthew Kirkcaldie m.kirkcaldie at removethis.unsw.edu.au
Sat Jan 28 20:39:58 EST 2006


In article <1h9vo38.7xo2e21khgx9cN%usenet02 at out-of-phase.de>,
 usenet02 at out-of-phase.de (Christian Wilms) wrote:

> Something for the inhibition experts out there:
> 
> I'm looking for a drug that will prevent or at least reduce the
> desensitization of GABA-A receptors. Basically a GABAeric version of
> cyclothiazide.

Surely you'd have to find a way to sterically hinder the action of 
whatever is desensitising the receptors?  What's desensitising them?

I can tell you that allopregnanolone is a potent endogenous potentiator 
of the GABA-A receptor, but it would be a pain to deliver in a 
controlled way - it's a steroid so you usually have to use very sticky 
vehicle.


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