acetyl-hydromorphone

[chemchem]

So my understanding is hydromorphone is stronger than M because it can pass through the BBB better do to being less polar. Now H is better than M for the same reason.

Is it possible to add an acetyl group to hydromorphone and make it pass through faster?

Now you might be thinking that oxymorphone is still more potent, yet it contains that 14hydroxy making it more polar, however I believe there is another pocket that fits the hydroxy in there. This would make sense since larger substituents on the 14 position provide better potency.

We need a comp chemist to check out the docking of these molecules, maybe we can improve the design or find a simpler molecule to use, or make it more selective for different opioid receptors.
I should learn comp chem soon, should be fun playing around with those receptors and molecules.

[Papa Verine]

I don't know...

I enjoy reading all these posts about opiates that increase in potency by x number of times and all that. But where can I get them??? That's what I want to know. If only I could get some damn Acetyl-Hydromorphone... you know? I'd make a big chart with all these different chemicals, and how much potency I percieved them to have through self-experimentation.

I should've been a chemist... and had a V-8.

[Paregoric Kid]

yes, basically, it is called acetylmorphone. also, look into metopon, a methylated analogue of hydromorphone. also methyldihydromorphine and some of the dihydromorphine analogues are interesting.

[jonny-5]

hydromorphone already passes through pretty damn quick. if anything id want to find a way to keep dilaudids awesome rush, but add some legs to it so it would last longer, kinda like the heroin i get. its tar, and i can tell that it has something besides just diacetylmorphine that gives it legs, like probably 6-monoacetylmorphine or just morphine itself. it has a good rush and then the high lasts a pretty damn long time, like a few hours and then i dont get sick for somewhere around 12 hours after IVing an issue.

so what im thinking is what would be more valuable to me would be to find a way to give hydromorphone legs, instead of just a really quick good rush. ya know?

[chemchem]

well thats where the comp chemistry should come in. should be able to fit something into a pocket increasing the time it produces the analgesic effect.

but i'm still a beginner

need to study the longer acting opes and see what they have or what they interact with

[chemchem]

so what im thinking is what would be more valuable to me would be to find a way to give hydromorphone legs, instead of just a really quick good rush. ya know?

I just fully read this... well this is my logic behind it.
When the compound can cross the BBB very rapidly, the receptors get activated faster producing that rush, from so much activation in a short amount of time. The affinity and how long it can bind, or how long it can stay with out being degraded, effect the "legs".

So what you want is something that crosses fast, for the rush, and stays in the synaptic cleft, or bound to the receptor, for a longer duration.

Does anyone know of a variable that effects "rush"? I imagine its the time it takes to get into the brain, I don't know how this would be measured though.