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Drugs acting on the 'opiate system' other than opiates

serotonin-system

serotonin-system

Ex-Bluelighter
Joined
Mar 24, 2008
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672
Hi all,

So, I'm more familiar with 5-HT pharmacology and in this field we have several different ways of activating 5-HT receptors. For example: SSRI's, MAOI's, 5-HT receptor agonists. All of which have shown promise as antidepressants. It seems that when it comes to opiate receptors, drugs are limited to receptor agonists and that's it. Is this the case? Are there endorphin transporters that could thereotically be blocked? Enzymes that break down endorphins that could be inhibited? Any other ways of potentiating opiate receptor activation other than administering agonists?

Discuss :)

SS
 
Cannabinoids such as THC indirectly activate opioid receptors.

Nicotine stimulates b-endorphin release.
 
Tianeptine has some opioidergic mecahnism. There's literature about it out there, but I can tell you from my experience that when I was using it regularly and took an abnormally high dose (3x my normal dose) I'd feel a good, painkilling opiate buzz that I *really* liked. You can also pop some D-Phenylalanine, which is apparently an enkephalinase inhibitor. I've found it to be helpful.

My personal favorite, however, is cardiovascular exercise and yoga, both of which have opioidergic (and in the case of cardio, phenethylamine-based) components that can get you *really* high if you push yourself hard. Great side-effects, too.
 
Some types of meditation are known to release beta endorphin and dopamine.
 
If talking about the "opiate system" and not just the opiate receptors themselves, I would say: Antihistaminics. They are well known to potentiate other opiates through indirect coupling to the opioid-receptors (to put it in short terms). There are several threads about this here at BL, so I won't elaborate this...

Peace! Murphy
 
I cant believe no one mentioned Salvia D. yet. It is apparently a kappa opioid agonist but does not have affinity for mu receptors which cause most of the 'desirable' effects of opioids. The kappa agonism is what causes the hallucinations and is why they are so much different than effects caused by other hallucinogens.
 
Ketamine has mu agonist activity (that's why the ortho-chloro group is included) although to maximize the mu agonist activiy, the most useful substitution is 3-methoxy/hydroxy - corresponds to the phenolic OH group in morphine
 
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^ Yea, it's a full mu agonist.

Also, Sophora Subprostata or Shan Dou Zeng, a chinese medicinal herb is a kappa and mu agonist.
 
^ DXM, although closely related to morphine does not act on any opiate receptors. Though it is a sigma 1 and sigma 2 receptor agonist, and they were once thought to be a type of opioid receptor, but later found they weren't related in any way, because opiate antagonists failed to block the effects of sigmaergic drugs.
 
If I remember correctly, thiorphin is a beta-enkephalinase inhibitor and because of that exerts opioid activity by a different route (best check the info though as it was a long time ago that I read that and I've killed a lot of brain cells since then!)

Actually it's thiorphan (my piss poor spelling!) and there's a bit of info here
 
Thymoquinone, from the seed oil of Nigella Sativa, I read a while ago that it is noncrosstolerant with morphine, but morphine is crosstolerant to it, it acts, anecdotally, as quite a potent potentiator of opioids, but doesn't seem to get one high on its own.

I think that likely could be an enkephalinase inhibitor, or inhibit breakdown of other endogenous opioids going from that.


http://www.ncbi.nlm.nih.gov/pubmed/12722128?dopt=Abstract Anyone got access to the full paper?


Theres another enkephalinsase inhibitor in the wild lettuce if I remember right, although I'm not sure which compound is responsible, for the so called 'lettuce opium'
 
What about such as california poppies, and other poppye types? Also apomorphine and amorphine; are they not resent in some lotus species?
 
swilow said:
What about such as california poppies, and other poppye types? Also apomorphine and amorphine; are they not resent in some lotus species?
Click to expand...

^ Nope. california poppies only have alkaloids like noscapine and papaverine. Even if they did have narcotic alkaloids they would be like codeine, morphine, and thebain which are actual opiates, which OP said substances otherwise.
Lotus does not contain any opioids either.

Apomorphine and amorphine aren't opioid agonists, they are dopamine agonists unrelated to morphine or heroin.
 
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