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Gabapentin binds to the alpha 2 delta 1 subunit. Question

Kdem

Bluelighter
Joined
Mar 14, 2015
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Is that subunit in any way related to the GABAA receptor ? I once read that benzodiazepines (at high doses) bind to calcium channels.

Quote from wiki: https://en.wikipedia.org/wiki/GABRD

'(GABA) is the major inhibitory neurotransmitter in the mammalian brain where it acts at GABAA receptors, which are ligand-gated chloride channels. The GABAA receptor is generally pentameric. Its five subunits are alpha, beta, gamma, delta, and rho. The GABRD gene encodes the delta subunit'

Alpha2, delta 1 looks like GABA ...

But then this: https://en.wikipedia.org/wiki/CACNA2D1 ...

Has that subunit nothing to do with gaba ?
 
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As far as I know gabapentin binds primarily to the a2d calcium ion channels and block them. Iirc this translates to less excitatory action because of less activation in calcium channels. So while the effects of gabapentin may look like GABA related reductions in excitatory action (e.g. inhibition from benzos) I think they have little to do with GABA.
 
alpha delta and etc are greek lettering systems used to denote protein subunits. So a gaba receptor may have an alpha component, but that is not the same alpha component on a calcium channel. Or a sodium channel or whatever.
 
Sekio, got it, thanks !

It's odd that in older literature it is stated that benzodiazepines at higher doses bind to calcium channels. I guess that's just outdated theory ?
 
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