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Opiates and stimulant effect

The Monkey Mantra said:
What I'd be looking for if I were you is delta opioid receptor activity (DOR). I believe the DOR is more tied into the inhibition of the GABAergic activity which suppressed dopamine release. Morphine, one of the LEAST stimulating opioids IMO, is basically pure MOR. Stuff like levorphanol was always rather stimulating to me, and I've had friends who ate large doses of my prescription and had sleepless nights because of it.
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From what i have read, DOR agonists inhibit Acetylchloline release in the Basal Ganglia. Acetylcholine normallys inhibits dopamine release in the Basal Ganglia, so a DOR agonist will indirectly increase dopamine release.

KOR agonists inhibit Dopamine, and they are very sedating.

and MOR agonists inhibit GABA, which indirectly increases dopamine.

KOR and MOR also inhibit Glutamate release which dampens down neurons, and stops burst firing.

There are also DOR/MOR hetro-dimer receptors (the receptors are joined together, and when both activated synergise) and drugs that 'hit' them (like herion and M6G) will be more stimulating than a pure MOR agonist, and MOR/DOR agonists are alot more EURPHORIC. I suspect that Oxycodone hits this DOR/MOR hetro-dimer receptor (from the way people talk about it) but i have never read anything about this - just guessing.
 
How can you possibly "find buprenorphine stimulating due to kappa antagonism?" How exactly do you pretend to discern between kappa antagonism, delta antagonism, mu agonism, dopamine release, and all the other effects?

Simply put, without testing a variety of single-action drugs (ie, pure DOR-antagonists, KOR-antagonists, etc) there's simply no way to make these sorts of claims with any degree of credibility.
 
Ham-milton said:
How can you possibly "find buprenorphine stimulating due to kappa antagonism?" How exactly do you pretend to discern between kappa antagonism, delta antagonism, mu agonism, dopamine release, and all the other effects?

Simply put, without testing a variety of single-action drugs (ie, pure DOR-antagonists, KOR-antagonists, etc) there's simply no way to make these sorts of claims with any degree of credibility.
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Cause i have tried lots of other different opiates with no Kappa antagonism, and i find them more sedating.

Buprenorphine is the only stimulating opiate i have found.

There are SO MANY articles on the net talking about which opiate receptor is stimulating, and which opiate receptors are not. If you bothered looking around you would find them easily.

here are some articles for you:

http://jpet.aspetjournals.org/cgi/content/abstract/290/3/1307

http://www.aapsj.org/view.asp?art=aapsj070371
http://www.aapsj.org/articles/aapsj0703/aapsj070371/aapsj070371.pdf

http://www.jneurosci.org/cgi/content/full/23/13/5674

http://molinterv.aspetjournals.org/cgi/content/abstract/6/3/162

There are lots of articles on the net regarding this - go find them if you can be bothered.
 
Mitragynine->7 Hyrdoxy is a pretty simple 1 stepper. I wonder if those people selling the pure 7-hydroxy are extracting it or making it?
 
Ham-milton said:
Yeah, that's true, but pure mitragynine is available, and has a similar effect. the 7-hydroxy derivative is more potent, but from my personal tests, there effects aren't that different.

I always wonder about the "true opiate" idea. I tend to consider anything that binds to MOR an opiate, and those partial agonists opioids. Obviously not the official or common understanding, but it makes more sense in my mind.

But from what I've seen, (go figure) F&B is dead on. The more stimulating opioids tend to have of a dopaminergic effect. I think this is related to why some opioids are more addictive than others- hydrocodone isn't as stimulating, less addictive. Oxycodone is more, more dopamine, a better agonist and way more addictive.

That probably won't prove true, but I'm gonna stick to it for a while.
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unfortunately i have a strong tolerance to opiates from years of use. i've found hydrocodone to be much MORE stimulating than oxycodone although i do find both stimulating and keeps me from sleep. hydrocodone makes me incredibly stimulated and motivated. some friends of mine agree with my experiences on hydrocodone vs oxycodone. i will agree hydrocodone is much less addictive and withdrawals exponentially easier from hydrocodone than oxycodone. my statement about hydrocodone being much more stimulating than oxycodone but less addictive goes entirely against the dopamine agonist theories i know. i'm just stating from my experience and from my friends' experiences. i think the dopamine release that FAB said as the first reply in this thread makes perfect sense but i don't know that hydrocodone fits that role b/c to me it's more stimulating AND less addicting. the latter part shows that it fucks with the reward system a bit less than oxycodone, something else must be going on with hydrocodone that's not dopaminergic that would explain this added stimulation. unless my friends and i are alone in saying that hydrocodone is more stimulating than oxycodone.
 
The more directly the opiate is derived from thebaine the more stimulating it will be, its that simple.....
 
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