Opioids Vote for your favorite Opiate (in terms of warmth, Euphoria, bliss, etc.)

[Northwesternparacelsus]

Oxymorphone slams
Panda is very real my DOC

Very interesting will watch thread. We were overdue for a vote here!

Heroin 3) close

 

[4DQSAR]

@Northwesternparacelsus - WSB infamously wrote "Letter from a master addict to dangerous drugs" to the British Journal of addiction in 1956 and I may be wrong but I don't think oxymorphone had been used medically at that point BUT he suggested it would be the most euphoric opioid.

In fact his understanding of QSAR was probably better than most doctors and while now we know some of the ideas were wrong, with the information to hand, he had good reason to list things like diacetyloxymorphone and diacetyldihydromorphine.

Even now we only have a small number of animal models which purely measure analgesic activity to guesstimate if he was right or wrong since as far as I know none of the other things he suggested had ever undergone human trials.

 

[RUC4]

i've never heard of or tried tilidine. it has piqued my curiosity.

 

[DeathIndustrial88]

i've never heard of or tried tilidine. it has piqued my curiosity.

I think it's more commonly used in Europe.

I believe @Hexenstahl wrote a whole post about this opioid & it being their favorite. At least I think it was tilidine. It has some unique properties, I believe dopamine reuptake inhibitor properties, which occurs because of it's metabolite nortilidine.

I'd love to try it myself too, personally. It's basically an opioid & a stimulant in one.

 

[DeathIndustrial88]

There's so many opioids out there, rare or just not used much that I will probably never get to try & it just makes me sad. lol

People think an opioid is an opioid is an opioid.... but every opioid has it's own unique feel & energy to it. And everyone's bodily chemistry is different, so what might be boring for one person is gonna be fun for another. There's so many variables & experiences to be had.

I'd love to try tilidine, dilaudid, opana, levomethadone, O-desmethyltramadol (in it's pure form). There's just so much.

 

[4DQSAR]

I believe dopamine reuptake inhibitor properties, which occurs because of it's metabolite nortilidine.

Dinortilidine overlays cypenamine.

Now I don't know if nortilidine is in effect 'methylcypenamine/methcypenamine' although it IS flagged as a drug of abuse in some databases.

 

[DeathIndustrial88]

Dinortilidine overlays cypenamine.

Now I don't know if nortilidine is in effect 'methylcypenamine/methcypenamine' although it IS flagged as a drug of abuse in some databases.

Not sure myself. Never heard of cypenamine til now. Sounds like an experimental psychostimulant drug.

But Googles AI overview definitely says it has dopamine reuptake inhibitor properties. Along with NMDA antagonists properties.

Yes, Tilidine possesses dopamine reuptake inhibitor (DRI) properties, but this activity is exclusively attributed to its primary active metabolite, nortilidine. [1, 2]
While the parent drug tilidine itself is a weak prodrug with minimal pharmacological activity, it undergoes rapid first-pass metabolism in the liver to form nortilidine. Nortilidine functions as a dual-action compound: [1, 2]

• • Mu-Opioid Receptor Agonist: It binds strongly to μ-opioid receptors to provide morphine-equivalent pain relief.
  • Dopamine Reuptake Inhibitor: It blocks the dopamine transporter (DAT), preventing the reabsorption of dopamine and increasing extracellular concentrations of the neurotransmitter in the brain. [1, 2, 3]

Additionally, specific isolated isomers of nortilidine exhibit NMDA antagonist properties. This diverse pharmacological profile contributes to both its effective pain-blocking capabilities and its high potential for misuse, which is why medical preparations of the drug (such as Valoron N) frequently combine tilidine with the opioid antagonist naloxone to deter intravenous abuse.


That last part is confusing, because why would anyone wanna abuse IV Tilidine if it needs to undergo first-pass metabolism in the liver into it's active metabolite?

 

[4DQSAR]

I wrote and deleted the apart about NMDA activity because it's another example of papers woozing from a study in which EVERY class of receptor tilidine had even slight affinity for and it's only their we see it mentioned. I am guessing somewhere along the line it was seen as useful to someone to suggest tilidine MAY be able to treat pain that a pure opioid could not. I believe levodromoran and ketobemidone are examples of where those specific medications have significant NMDA activity therefore are better able to treat certain types of pain.

As for addition of naloxone, I strongly suspect political reasons. Same as saying something is a 'mixed agonist' or 'partial agonist'. Both terms are so opaque as to be meaningless.