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4-methyl-GHB

Haha wow, old thread!

I'm also curious... GHB is probably tied for my favorite pleasure drug.
 
Interesting, never heard of the compound before.
And I declare you, muie, the Necro King.
 
On a similar note without hijacking has anyone tried 4-methylpregabalin
 
It's been a long time since I've been really involved in OD so if I could get some help from my compatriots here regarding philosophy. Is this a typical thing over here, sort of, open ended questions regarding the entirety of a drug's character. I'm definitely curious about some of these analogs. As many of us know, the majority of Pregabalin (Lyrica) is excreted unchanged, but a very small portion is metabolized into 4-Methylpregabalin.

I'm very curious though. There are some other Gabapentinoids that are allegedly under development that I'm sure are going to be quite interesting. The patent on Lyrica finally ran out this year so you can only imagine they're scrambling to raise another prize pig as fast as they can. I've never used GHB :(
 
absinthe6669 said:
Has anyone outhere tried 4-methyl-GHB or 4-pentanolide ( Tranquili-G )?
Click to expand...

"4-pentanolide" is probably better known under the term gamma-Valerolactone ("GVL").

It has seen some use as a GBL replacement, although it seems to be less potent, yet somehow more toxic. The same presumably applies to 4-methyl-GHB ("gamma hydroxy valeric acid"), seeing as how both GBL and GVL are pro-drugs for the corresponding gamma-hydroxy acid (i.e. GHB and GVB).
en.wikipedia.org

gamma-Hydroxyvaleric acid - Wikipedia

en.wikipedia.org en.wikipedia.org
en.wikipedia.org

γ-Valerolactone - Wikipedia

en.wikipedia.org en.wikipedia.org
 
Keif' Richards said:
As many of us know, the majority of Pregabalin (Lyrica) is excreted unchanged, but a very small portion is metabolized into 4-Methylpregabalin.
Click to expand...

This is false. A very minor portion of pregabalin is metabolized into N-methyl pregabalin, not 4-methyl-pregabalin.

I'm very curious though. There are some other Gabapentinoids that are allegedly under development that I'm sure are going to be quite interesting. The patent on Lyrica finally ran out this year so you can only imagine they're scrambling to raise another prize pig as fast as they can. I've never used GHB :(
Click to expand...

Weirdly enough, the search for a successor to pregabalin hasn't been all that fruitful for Pfizer.
While they were quick to discover a number of analogues that had a much higher affinity for the target ion channels in-vitro, this didn't translate into increased in-vivo potency. This is because the drug is too polar to enter the brain on its own, so it has to rely on certain transporter proteins, which are normally responsible for the uptake of the amino acid leucine. This naturally complicates the development of such a drug, since it has to be designed to fit into not one, but two different pharmacophores.

A few drug candidates (atagabalin, imagabalin, 4-methylpregabalin) apparently made it into clinical trials, but it looks like Pfizer eventually shelved them all after failing to demonstrate any additional therapeutic benefits when compared to pregabalin itself. Mirogabalin (which was developed by Daiichi-Sankyo, not Pfizer) recently got approved for neuropathic pain in Japan, but as far as I've read that's it for novel gabapentinoids.
 
Oh jeez. My bad guys, I should've been a little more careful. Thanks for the correction Hodor. I actually knew about the failure of some of these other guys, but I did hear about the Mirogabalin and that was actually the one I was most curious about. I'm kind of blown away that there is a novel, potentially abusable drug that wasn't unleashed upon the barefoot hordes of America first.

Should I move to Japan? I think I would fit in pretty well.

"Hey Toji! More of that wicked fucking pissa Sake down here. You guys wanna smoke DMT on top of a moving bullet train? You guys like this Manga shit at all?"
 
4methylpregabalin is readily available and supposedly 5 times more potent.

It might be more cost effective. I'd like to gwt a lot tof use to come off methadone and possible benzos. Gabaergic withdrawal or taper seems to be manageable for me
I feel at this stage opioid withdrawal is almost beyond me and the thought of bEnzo sickness frightens me.
 
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