Kindling, Gabaergic Substances and NMDA receptor antagonists

[Jabberwocky]

I would like to learn more about the use of NMDAr antagonists in treating gabaergic substance use disorders. The wikipedia entry on kindling has stimulated my curiosity. From the wikipedia page:

Acamprosate, a drug used to promote abstinence from alcohol, an NMDA antagonist drug, reduces excessive glutamate activity in the central nervous system and thereby may reduce excitotoxicity and withdrawal related brain damage.

*[reference]​

Any one have any knowledge or experience in this arena they'd be willing to share? Thank you!

 

[Coolwhip]

Not that NMDA antagonists couldn't be useful in GABAergic WD, but I wouldn't classify Acamprosate as an NMDA antagonist.

 

[Jabberwocky]

Would you mind explaining? I am very interested in them considering how useful they were in getting off heroin and opioids generally back in the day, but I don't really know much about the neuroscience behind how they work.

 

[Limpet_Chicken]

IIRC acamprosate is an NMMDA antagonist selective for the polyamine binding site.

 

[asecin]

i find this interesting as well. toothpastedog which NMDA antagonist did you use to get off opiates? i remember DXM was most effective for me but im curious about acamprosate how it works to stabilize in alcohol withdraws etc.

 

[Limpet_Chicken]

Liker I said acamprosate is an antagonist at the NMDAr polyamine site.

 

[d1nach]

The difference is dxm is metabolized to dxo and acts directly with the nmda receptor as well as dxm activating the sigma receptor and havinf some antgonism of nach receptors I believe . The polyamine site is a distinct receptor located on the nmda channel. And acamprosate has a unclear mechanism of action so is thought to allosterically or indirectly influence the nmda and gaba receptor. Opiate withdrawl might result in a increase in excitation which may involve nmda receptors sending excitatory signals and hving reduced gab acticity from constantly activatingthem with opiates. Some people believe this abnormal activity causes stress to the brain increase risk of relapse as your brain wants to fix things