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Cholinergics + Sigma 1 receptor

M

Mask0ff

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Joined
Apr 21, 2021
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Is anyone aware of any cholinergic drugs besides donepezil (ache inhibitors or otherwise) that also potently agonise the sigma 1 receptor to nearly the same degree?

Cheers & Tanks (and treads)
 
What is the purpose of the compounds you see interested in? Only thing I can think of is cognition enhancemebt maybe.
 
ibtisam midlet said:
i have reviewed thousands of meds and never found cholinergic drugs besides donepezil that also potently agonise the sigma 1 receptor
but in other type of meds there is Opipramol (selective) and Fluvoxamine
en.wikipedia.org

Opipramol - Wikipedia

en.wikipedia.org en.wikipedia.org
en.wikipedia.org

Fluvoxamine - Wikipedia

en.wikipedia.org en.wikipedia.org
Click to expand...

Oof, a TCA. Fluvoxamine i'm also looking at but would be combining an SSRI with ache inhibitor, want a second option on ACHE inhibitor. Any idea on if you can combine 2 sigma-1 agonists?
 
Mask0ff said:
Oof, a TCA. Fluvoxamine i'm also looking at but would be combining an SSRI with ache inhibitor, want a second option on ACHE inhibitor. Any idea on if you can combine 2 sigma-1 agonists?
Click to expand...
I have biases against ache inhibitors after reading too many toxicology papers on low level organophosphate exposure in agricultural workers and the increase in neurodegeneration. This may very well not carry over to non-covalent inhibitors, but the fear has been planted in me.
 
Skorpio said:
I have biases against ache inhibitors after reading too many toxicology papers on low level organophosphate exposure in agricultural workers and the increase in neurodegeneration. This may very well not carry over to non-covalent inhibitors, but the fear has been planted in me.
Click to expand...
Make sense, every exogenous ligand has it's side effects just about. Could you provide a link? It can't be all that bad.

Just found this: https://pubmed.ncbi.nlm.nih.gov/32798937/
 
Here's one: https://www.sciencedirect.com/science/article/pii/S0160412017305822#bb0110

I like this more than pure epidemiological stuff because they not only tie risk to organophosphate exposure, but they look into paroxonase1 (PON1) functional polymorphisms. PON1 breaks down organophosphates, so the finding that the slow metabolism phenotypes increase Parkinson's risk when around organophosphates strengthens the argument that they are causitive.
 
Check. Out my latest invention. Sigma 1 with m1-5 cholinergic agonism, together with d and s activity
 
opipramol seems to be the widest sold antidepressant in germany. i found it to be ok. you have to take many times the dosage that it recommended. i took it rectally once and it produced a certain taste in the mouth, something that seems to be the case with sigma ligands.
 
in higher doses it calms you down, thats all i remember.
 
For me opipramol did nothing, literally nothing and I ended up taking whole blisters in search for just something. Might have been just me tho.

But there's certainly something about sigma, just look @ DXM or ibogaine, for example.
 
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