• N&PD Moderators: Skorpio | thegreenhand

Endogenous antagonists of the opioid receptors

Nagelfar

Bluelight Crew
Joined
Nov 23, 2007
Messages
2,527
It appears, from what I've seen of the literature, that there isn't the narcan equivalent of endorphins found to exist as made by the body (endorcans?).

Any papers with titles like "endogenous opioid antagonism" regard exogenous ligand antagonism of endogenous opioids.

Now I am well aware subjective experiences, cited as to what mechanism is truly taking place with regard to their own neurotransmitters, is the bane of subforums such as ours here. Scientifically unsound to say the least.

However as I am basing my following accordingly, I have little other recourse than the familiarity in these shared experiences: I myself have had information hit me, feelings of shame, more than simple embarrassment; those immediate moments of being told off or shot down, where a chill goes down my spine, I get cold and feel nauseated, in fact get goosebumps. A hot flush comes over me; very similar to many experiences being resuscitated with naloxone (once five times repeatedly in a single overdose scenario), post acute withdrawal, precipitated withdrawal especially. These are exaggerated when I have been in such a state and have felt any of the above.

Am I alone in presuming there is some manner wherein opioid receptors are naturally antagonized (inverse agonists to be more precise), is there any reason as to why not? Is there a specific scaffold of the G-coupled protein site, for mu particularly, which allows for inverse agonism that might then rightly be called an orphan receptor sub-complex of some kind, by that rationale?

I'm honestly perplexed as to why I cannot find more attempts at discovering such compounds in the body, are so many reactions, subjective feelings, explained away by other neuro-transmitters that interest has not been piqued to search for and isolate such a potential natural mechanism?
 
I'll raise you an i don't know.

Do you know if there are any endogenous antagonists of gcprs that function as antagonists at the level found in the human body? I can't really think of any off top.
 
Its probably more of matter of things that limit the conversion of precursor peptides like PMOC to beta-endorphin, or things that lead to beta-endorphin degradation.

Who knows maybe there is some endogenous neuroactive steroid with antagonistic action on opioid receptors (sort of like dhea's antagonistic action on GABA-A).
 
negrogesic, whats with that comment, dhea has antagonistic effect on GABA-A?? I was taking it for a while, for libido. But would it be detrimental for someone who drinks or take benzos?
 
negrogesic, whats with that comment, dhea has antagonistic effect on GABA-A?? I was taking it for a while, for libido. But would it be detrimental for someone who drinks or take benzos?


Yes i would probably avoid it while taking benzos.

However perhaps in theory its antagonistic action on GABA-A could upregulate GABA-A and help repair the system after discontinuing benzos in a fashion similar to flumazenil. Who knows though.

Its worth noting that some fragments of beta-endorphin (like beta-endorphin 1-27) effectively act as antagonists to beta-endorphin and could be considered endogenous antagonists. Its probably a high affinity low efficacy partial agonist more than true antagonist is my guess.
 
Last edited:

Yes i would probably avoid it while taking benzos.

However perhaps in theory its antagonistic action on GABA-A could upregulate GABA-A and help repair the system after discontinuing benzos in a fashion similar to flumazenil. Who knows though.

Its worth noting that some fragments of beta-endorphin (like beta-endorphin 1-27) effectively act as antagonists to beta-endorphin and could be considered endogenous antagonists. Its probably a high affinity low efficacy partial agonist more than true antagonist is my guess.


thats very very interesting. i have this kind of a weird seizure disorder.... while not crazy ass epilepsy shit, i do get severely disoriented and completely lost and confused for few seconds a minute at time, especially driving a car, which is stupid and dangerous. BUT anyway, yesterday i drank a whole bottle of Cognac and I knew with my disorder I will in fact get the seizures next day but what does my stupid ass do? I pump up myself with vitamins and herbals , including high doses of DHEA because it usually helps my libido and I needed it that day, and I end up having some severe crazy mental breakdowns or if you wish yo call it siezures. Shit was nuts and I am still trying to recover... I am still shaking actually typing this. I just wonder, whats a high dose of DHEA anyway?? I read some studies DHEA helps with addiction with crazy doses of up to 100mg https://www.ergo-log.com/break-addiction-dhea.html

but anyway, im just rambling i guess.... super stimulated...
 
yeh supposedly by literature that changes all the time. as if i ever got one single correct statement ever from science....

today we are sponsored by starbucks so coffee is good for you. tomorrow we are sponsored by lipton so tea is better.
 
Last edited by a moderator:
It's modulated by the sert mélatonine for sleep, how? Lights. Think of open eyes when drunk against closed. I think
 
Top