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Delta opioids

B

bupropion

Bluelighter
Joined
Feb 29, 2008
Messages
373
Has anyone tried selective delta opioid receptor agonists? What affects do they have / are thought to have? Are they less addictive?

Has anyone tried etorphine (which I think is a non-selective agonist)?
 
They cause analgesia but also produce dysphoria and hallucinations.
Salvinorin A is a selective K-opioid agonist.
Interestingly, I think k agonists are the only CNS opioid class that doesn't produce respiratory depresison, but I could be wrong with this - not sure how ORL1/NOP behaves in this respect.
 
A korean friend of mine had once given me some tablets that he claimed to be dihydroetorphine; evidently he used to take these quite often (i think parentally). Dosage of these i am unsure (20-40ug, possibly?) i took it orally, the effects were strange, not unlike levorphanol, but very difficult to discern as i had been taking other compounds at the time.
 
Yes, i'd like to know more about what the effects of agonism at this receptor are. It's very good just to read some article about it but i'd like to do the taste test so I know first-hand what they are like.

There's already alot of mu-agonists and if one wants kappa then salvia can do that. Alot of the pure delta agonists have really weird structures; im keen on Lednicers discovery/ies because of the dual receptorial profile of these ligands.
 
Jamshyd said:
^ We are talking about Delta, not Kappa. Got your greeks mixed up, my friend? ;)

Actually, I am curious about this as well.
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Hahah, oops. I should read more carefully. :! :o
Hmm, I too would like to know more about delta. It's not often discussed.
 
No specifics to offer up, but I read a bit on the delta and epsilon opioid receptors a while ago, and seemingly, many delta agonists were convulsants, some were, some were not, I can't remember much more about it, but a note of caution is advised.
 
Tramadol and pethidine also cause seizures at high doses though, just take a couple of benzos with it and there would be no problem I'm sure!

A selective delta opioid agonist would be very interesting to try, wonder how different it would feel from regular mu agonists. Theres certainly quite a difference between mu agonists and kappa agonists, but I think delta is probably more similar to mu...

Anyway from a quick browse I see suppliers available for both SNC-80 and BW-373U86 so there are certainly selective delta agonists there for the tasting if someone is willing to pay the rather exorbitant price!
 
Hmm, I thought the anticonvulsant benzos didn't cause much respiratory depression?
Feel free to correct me, hehe.
 
More to the point do delta opioid agonists cause respiratory depression, or is it only mu agonists?

2-5mg of lorazepam should be enough to prevent convulsions unless the pro-convulsant effect is really strong, and the respiratory depression from that amount of benzos will be minimal.
 
Benzos increase the respiratory depression caused by opiates/opioids (synergistic effect). Methadone & diazepam or temazepam is a 'popular' way to OD in the N E of England.

Must admit I never thought about whether delta agonists cause resp. depression (just assumed :o ) - if they do, it's not a good combination
 
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.
 
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...

Doctors and nurses usually are pretty careful. And if they fuck up, there is usually some Naltrexone on hand ;)

Anyway from a quick browse I see suppliers available for both SNC-80 and BW-373U86 so there are certainly selective delta agonists there for the tasting if someone is willing to pay the rather exorbitant price!
Click to expand...

As long as I'm guaranteed Customs won't impound it =D
 
Remember that bupreprenorphine and dihydroetorphine are quite similar in structure.
buprenorphinedd0.gif

I've read that DHE is only stable by parenteral administration, meaning that administration through the alimentary canal requires a much higher dose.

Remember that a hardened addict already has a high tolerance, reducing their risk yet further.

Indeed, this is not intended for a person with no tolerance, but it is not so crazily potent to the point that for a human to even contemplate taking it, they should automatically be judged as insane.

Bear in mind that DHE does not have as much euphoria as something like oxycodone. The simple fact of the matter is that it is so strikingly potent that it is cheaper to support a habit of the stuff.
 
^^^That is true, it is not nearly as euphoric as oxycodone/morphone. It may be similar in structure to buprenorphine, but i think that is where the similarities end.

As i mentioned before, it has a strange feeling to it (in the way that levorphanol is strange, but not as euphoric as levorphanol either). The guy i knew was injecting these tablets, which i suppose is even more dangerous (i would assume the bioavailability is not too high)...

Is DHE a schedule I or II drug?
 
Perhaps the strange feeling you mention could be due to epsilon agonism, I know that etorphine itself is an unselective agonist, wouldn't surprise me if dihydroetorphine was also.

Anyone know more about the epsilon receptor? apparently etorphine and b-endorphin are nonselective ligands for the it, are there yet selective ligands, agonists or antagonists available?
 
@riemannzeta:
just consider the following: you put 100 grams of morphine into one liter of water and stir it until it is solute. now, you get pain and you take 0,5ml. fine.
the other time you put 100 milligrams of dihydroetorphine into one liter of water and stir it until it is solute. do you think you would die if you took 0,5ml of this solution? if so, please explain the reasons to me

(edit: for the entire little brainteaser to be assumed that dihydroetorphine is 1000x as strong as morphine)
 
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