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Benzodiazepines are kappa agonist?

The Holy Quadruplty

Bluelighter
Joined
Feb 9, 2022
Messages
660
I was reading that a lot of benzodiazepines are kappa opioid agonist, but I was also reading that they're kappa antagonist which would make more sense. Does anyone have any information on this at all that you could share?
 
The potencies of these benzodizaepines at these receptors is very weak compared to their potencies at GABA A receptors.

The paper even mentions in their discussion that this is not phisiologically relevant except for when high doses of benzos are injected into the spinal cord directly.

I would reccomend reading the discussion sections of papers, as while there is often a tendency to overstate results, papers will usually at least attempt to provide plausible limitations for their findings.

Reading only the abstract of a paper robs you of the context and honestly helps propagate misinformation that is pretty common on forums such as here. This problem is honestly super widespread as it is hard to infer context without experience in a specific field, and requires effort.

If you can't access the papers try Sci-hub (you often have to Google search for mirrors as the site moves quite a bit) or the mutual aid science community. If unable to find papers still, ask here and somebody with access (including myself) can likely help you.

At high enough doses, no drug is selective. The true mark of "selectivity" for a drug is the ratio between it's affinity for the receptor that produces it's main mechanism of action, and a different receptor. You can think of this ratio (x) functionally as "you will need x times an active dose to produce activity at a desired target". Nonselective drugs have these ratios in the ones to tens, ratios over a thousand fold can be considered as selective for one receptor over another, as a dose that would act on a minor binding partner would likely provoke a fatal overdose from the major receptor.
 
The potencies of these benzodizaepines at these receptors is very weak compared to their potencies at GABA A receptors.

The paper even mentions in their discussion that this is not phisiologically relevant except for when high doses of benzos are injected into the spinal cord directly.

I would reccomend reading the discussion sections of papers, as while there is often a tendency to overstate results, papers will usually at least attempt to provide plausible limitations for their findings.

Reading only the abstract of a paper robs you of the context and honestly helps propagate misinformation that is pretty common on forums such as here. This problem is honestly super widespread as it is hard to infer context without experience in a specific field, and requires effort.

If you can't access the papers try Sci-hub (you often have to Google search for mirrors as the site moves quite a bit) or the mutual aid science community. If unable to find papers still, ask here and somebody with access (including myself) can likely help you.

At high enough doses, no drug is selective. The true mark of "selectivity" for a drug is the ratio between it's affinity for the receptor that produces it's main mechanism of action, and a different receptor. You can think of this ratio (x) functionally as "you will need x times an active dose to produce activity at a desired target". Nonselective drugs have these ratios in the ones to tens, ratios over a thousand fold can be considered as selective for one receptor over another, as a dose that would act on a minor binding partner would likely provoke a fatal overdose from the major receptor.
I feel you, but they still do though obviously. I wonder what effects they would have with mixed opioid agonist like Buprenorphine, even if it's a high dose injection into the spine?
 
Btw I looked up Xanax, and it's metabolites on the target predictor and they bind to mu receptors too with some possibility it says. I'm going to look up some other benzos now.
 
never heard of it. this swiss prediction algorithm is not that useful, you need the substance acutally screened against a panel of receptors.

thats how they do it, you can use google translate:

 
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