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Using Naltrexone as KOR Antagonist--with what?

kor kappa opiod kappa antagonist mor mor agonist opioid naltrexone dynorphin depression

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#1 Sygyr

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Posted 12 May 2015 - 08:45 PM


I get occasional very deep bouts of depression that last only a day or so. I experience it as a deep aching pain in the chest--very real physical pain, the feeling of disappointment and despair, magnified--as well as anhedonia. It's brought on and magnified by stress. I have postulated this is the result of dynorphin, since the CRF provokes dynorphin release (CRF is increased by stress).

 

So I have been looking for a strong kappa antagonist, and read the threads on here, the problems with JDTic, etc. I have ordered some amentoflavone in the hopes that might be powerful enough as a kappa antagonist, but I am not super hopeful of it being strong enough.

 

I do have some naltrexone on hand, since I having been experimenting with low dose naltrexone (LDN). On a number of occasions, I have tried a low dose when I am in the midst of one of these episodes. Sometimes it works, and the pain/anhedonia completely lifts. It's like taking a pain medication, it's really amazing--and honestly the way the depression feels, it really does feel completely physical, and something that could be combated with a pain pill of some kind.

 

BUT it certainly doesn't work all the time, and I wonder if it's because naltrexone blocks mu opiods as well as kappa, and indeed kappa to a lesser extent that mu. I am wondering if there is a stack I can engineer that would balance the MOR antagonism while leaving untouched the KOR, without falling into the trap of stimulating the mu opioid system too much. I would also need something that can easily be obtained. Any naturally occurring MOR agonists that would balance out a low dose of naltrexone antagonism, or something I can get somewhere like alldaychemist, and take a small amount of?



#2 vaarmen

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Posted 13 February 2017 - 07:39 PM

You can't obtain a MOR agonist easily. That's basically an opiate. 

I would recommend KOR agonism instead of antagonism to obtain long-term benefits and to heal rather than be sucked in another black hole.

Basically you agonize KOR which leads to downregulation so you get less activity in the long term.

Salvia Divinorum is a potent and selective KOR agonist. As far I remember it's still legal in the US. It's a distinct hallucinogen. You have a 10 minute trip after which your KOR become desensitized and you experience an "antagonist" effect for the rest of the day.


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#3 normalizing

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Posted 16 February 2017 - 02:52 AM

You can't obtain a MOR agonist easily. That's basically an opiate. 

I would recommend KOR agonism instead of antagonism to obtain long-term benefits and to heal rather than be sucked in another black hole.

Basically you agonize KOR which leads to downregulation so you get less activity in the long term.

Salvia Divinorum is a potent and selective KOR agonist. As far I remember it's still legal in the US. It's a distinct hallucinogen. You have a 10 minute trip after which your KOR become desensitized and you experience an "antagonist" effect for the rest of the day.

 

what are you talking about, salvia is illegal in US


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#4 normalizing

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Posted 17 February 2017 - 03:15 AM

any good source for salvia?


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#5 vaarmen

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Posted 18 February 2017 - 11:54 AM

MOR agonism is a more slippery and potentially dangerous and addictive route to take than KOR agonism. KOR agonists, particularly Salvia are actually DYSPHORIC rather than Euphoric.  Salvia is also a very CLEAN drug, it does not touch any other receptors but KOR. Salvia is not allowed in certain states in the USA, but the fact that being a strong hallucinogen it is not federally banned also talks about the physical safety of the drugs, taken together with the fact that it touches only KOR and no other receptors. That said the Salvia trip is weird and can be psychologically frightening. I personally have much intellectual curiosity and fond of the trip since it kind of shows your mind from inside, but in any case I would advise starting very low. On low enough doses you can prevent the hallucinogen effects while still downregulating KOR. In any case once you are done with the trip you don't get a drive or strong desire of repeating, you feel it was enough.

 

You can obtain Salvia legally from various websites. Salviadragon, thebestsalvia, and Arena Ethnobotanicals are some good examples.

MOR agonists, on the other hand will provide temporary relief, but are bad in the long run, as they will downregulate your own MOR receptors as well as endorphin production creating dependence and withdrawal.


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#6 vaarmen

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Posted 18 February 2017 - 11:58 AM

Another good one for KOR downregulation would be Atomoxetine (Strattera) yes! the ADD drug. The primary effect is Noradrenaline Reuptake Inhibitor, but a metabolite is also a KOR agonist. This is the reason the drug is universally disliked, because the KOR agonism creates dysphoria. In the long run however, it could downregulate KOR thus healing the system and providing long term benefits. I have not tried this one. If anyone has tried this long enough I would appreciate any insight.


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Also tagged with one or more of these keywords: kor, kappa opiod, kappa antagonist, mor, mor agonist, opioid, naltrexone, dynorphin, depression

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