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Delta opioids

^^^^Yea that suggests a very low affinity to the delta/kappa receptors, so i would assume etorphine has a similarly low affinity for these receptors as well?
 
^A medical book gave etorphine a rating of "+++" for all 3 subtypes (?).

What is the epsilon receptor? Was it relatively recently discsovered?
 
This file is fairly good for outlining the antidepressant effects of DOR agonists. i havent actually read it myself yet, although I included a link to it in an earlier thread several weeks ago.

Yes I have a direct link to the article which I mentioned earlier.

Just reading stuff is pretty sick though, and some of the structures in that document are weird.

It's be cool if a salvia for the delta receptor appeared. That'd be like totally bogus, mang!
 
Is this stuff readily available on the market or one of those lurking in the background opiates? Sounds like it would be resonable to take.

Likely as addictive as morphine too.
 
Was just going to point that out. But it also has some pronounced adrenergic ativity and a decent affinity for mu opiod receptors. A very odd drug in my opinion and quite psychedelic for me as an individual.

I think this discussion pertains more to pure delta agonists. Conventional wisdom tells me if they were worthwhile then big pharma would have already exploited this option for pain mangagement. However that does not mean they wont be fun as trippy or dissociative chemicals, or simple potentiators for other psychedelics.
 
That's not true. Mitragyninine is selective for the mu opioid receptor.

Aged or improperly stored kratom will contain the primary oxidation product, mitragynine-pseudoindoxyl, which is indeed a delta selective opioid.

So, for the most part, there is not a commonly available DOR agonist.
 
I'd like to make it clear that delta opioid agonists are definitely addictive and definitely cause tolerance. I've read somewhere that they're more coupled with the inhibition of GABA on dopaminergic neurons, and they might cause more dopamine release than selective mu agonists. Maybe a more stimulating effect, then? What do you guys know about that?
 
^ That is assuming that the inhibit-GABA-to-increase-DA hypothesis stands true as far as opioid action goes.

Last I heard, that hypothesis is shaky at best.
 
Riemann Zeta said:
I can't believe that dihydroetorphine is used clinically. The therapeutic dose is around 20 mcg!? Couldn't this lead to a whole lot of overdoses and deaths if people are not extremely careful.
Click to expand...
I'm with morphiquet on this one. How would using a substance that is active at 20 µg be more dangerous than a substance active at 20 mg? I understand the dangers for the chemists working in the synthesis lab, but for doctors who have pre-made doses of the drug I can't see what the difference is (provided the two drugs have the same therapeutic index).
 
^ Yeah, that "argument" really gets me sometimes.
"OMG supadupa-fentanyl-analogue is so strong! Its the best because a dose is 1 microgram!"

But 1 microgram costs 10 dollars, while 100mg of high quality heroin also costs 10 dollars (lets say those two amounts are equipotent).

Eh, whatchugonnado?
 
Generally speaking, provided your dosing is accurate, more potent drugs are safer than their less-potent counterparts. This is because there is less of the drug in your body to do things other than its intended purpose.
 
This may not be the case with opioids however as receptor internalisation is observed more frequently with superpotent opioids.
Although this isn't so much "safety" as it is practicality (a lack of thereof) or good practice!

Indeed that is correct though. More potent drugs are likely to be that way because they fit the target site better - hence, they are less promiscuous.
 
Ham-milton said:
That's not true. Mitragyninine is selective for the mu opioid receptor.

Aged or improperly stored kratom will contain the primary oxidation product, mitragynine-pseudoindoxyl, which is indeed a delta selective opioid.

So, for the most part, there is not a commonly available DOR agonist.
Click to expand...

I've read that too, but are you sure of that?
Even that beeing the case you should oxidize mytragine for obtaining a DOR selective agonist.
 
Wait, delta selective? Does that translate to salvia-like effects?
 
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