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gaba a receptor subtypes

markosheehan

Bluelighter
Joined
Sep 17, 2016
Messages
238
which anxiolytic is selective for gaba a alpha 1 and 2 and also has no or very little activity at gaba a alpha 5 and 6 or is a antagonist at this.

thanks in advance
 
As far as benzos go, Temazepam is thought to have more selectivity for a1, it is more similar in that sense to the Z-drugs (which have decent preference for a1).
 
sorry I meant to say selective for alpha 2 and 3 not with little, no or antagonistic activity at a 1,5,6

I know we can all read the wiki page but i will quote some anyway

"Different benzodiazepines have different affinities for GABAA receptors made up of different collection of subunits, and this means that their pharmacological profile varies with subtype selectivity. For instance, benzodiazepine receptor ligands with high activity at the ?1 and/or ?5 tend to be more associated with sedation, ataxia and amnesia, whereas those with higher activity at GABAA receptors containing ?2 and/or ?3 subunits generally have greater anxiolytic activity.[10] Anticonvulsant effects can be produced by agonists acting at any of the GABAA subtypes, but current research in this area is focused mainly on producing ?2-selective agonists as anticonvulsants which lack the side effects of older drugs such as sedation and amnesia."

this is why I am looking for activity at just a 2 and 3.

There are others though. For example etifoxine acts through beta 2 and 3. This is also a good option. I tried it and found it quite good. gave me anxiety relief with out any cognition impairing/amnesia abilities. Unfortunately I am weary about taking it due to it being linked with liver damage in france and there are a number of case reports.


 
If you are looking for drugs that are commercially available, clonazepam is most likely the drug that matches your profile. Clonazepam has a very high affinity for the alpha 2 and alpha 3 subunits. Still, it has some affinity for the alpha 1 and likely also for the alpha 5 subunit.

Its is NOT safe, though !
 
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Clonazepam is pretty bad and only very mildly better than other traditional benzodiazepines in terms of producing less cognitive impairment. I haven't looked into and I can't find clonazepam exact subunit affinitys.
 
on the abstract I can not see anything about its selectivity . do you know if Imidazenil is selective for 2 and 3?

do you know any sources for pyrazolam's selectivity ?
 
It was available a few years ago. dunno why you cant download it anymore. maybe try contacting sci hub ?
 
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