N&PD Moderators: Skorpio
Possible ultra potent GHB analog
Synaps3
Bluelighter
I've been researching GABAb agonists and found the most potent to be SKF-97,541. Now what if you just replaced that amino with a hydroxy? Super potent GHB? If it works, it would be active with a few mgs like a benzo. Could the same be done to baclofen?
SKF-97541:
Holy crap it looks like a chemical weapon. Sorry, not really, bore slight reseblance to VX minus the sulfur
GHB not only acts at GABAB but also on GHB receptors, that is I guess what makes drugs like GHB / GHV etc kind of unique from other sedatives besides the steep dose-response curve. So question becomes whether your proposed compound binds to GHB receptors. If it is just about GABAB binding, the above parent compound does that already.
And it might be less unsafe to just at some point use that parent compound if it passes the BBB as it apparently does, since at least this one has some animal testing being performed.
I'd personally not fuck with Baclofen, but the gamma-hydroxy version of phenibut seems pretty yummy to me, I think I thought about that quite some time ago and recently someone else brought it up again independently.
rakketakke
Bluelighter
HOCPCA with an affinity 39x as high as GHB.
sekio
Bluelight Crew
I have a feeling you need both GABA-B agonism and GHBr agonism to get a good GHB like drug.
http://jpet.aspetjournals.org/content/313/3/1314.full - there is this but it's 4-hydroxy-4-phenylbutyric acid
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=38719 - and this
Yeah I've also seen 4-hydroxy-2-phenylbutyric acid before, but we need the beta / 3
Possibly this contains good info:
Analogues of gamma-hydroxybutyric acid. Synthesis and binding studies.
Bourguignon JJ1, Schoenfelder A, Schmitt M, Wermuth CG, Hechler V, Charlier B, Maitre M.
But I don't have uni credentials anymore. <<< sad panda
Synaps3
Bluelighter
Those listed appear to be GHB receptor only agonists. I think the hydroxy phenibut as well as the phosphinic acid molecule I proposed would work, but I'm not very experienced. Does anyone with more experience know of any reason why the first molecule replaced with a hydroxy wouldn't hit the GHB receptor?
BTW: I talked to some research chem companies and it sounds like the guy with the weirdest collection is interested in the first molecule. He said he added it to his get synthed list and we may see it in a few months. It would be the amino version though (like posted above) so most likely, no GHB receptor action. If it works as is, then I may try to get the hydroxy version. AFAIK it hasn't been tested in humans before, but has been used extensively for GABA research with no adverse effects.
Well let's hope for the nootropic kind of cholinesterase inhibitor, not the chemical weapon kind...
or better yet, just stay the fuck away from it?
Side-question: when an Alzheimer's patient is exposed to something like VX, is the disease instantly cured before he dies? 
WSH
Bluelighter
Side-question: when an Alzheimer's patient is exposed to something like VX, is the disease instantly cured before he dies?
Certainly, and if the dose is low enough, you can even treat him WITHOUT him dying.
But REVERSIBLE acetylcholinesterase inhibitors are obviously preferable for Alzheimer treatment.
blueberries
Bluelighter
HOCPrCA looks like a thong!
A couple of things I don't get about that molecule (HOCPrCA):
- is it a double radical, cause if those are two free adjacent electrons, isn't that just a bond? Is there like a chaperone molecule to stablize it normally, otherwise it all seems ridiculously reactive.
- its R,R-isomer is stereochemically made .. selectively, but how is it even a chiral molecule cause it looks planar trigonal?
Yes definatly, its limited with GHB as gabab agonism has the opposite effect on glutamate release in contrast to GHB agonism.
[morals off]Idk, man.... perhaps there's some money to be made in nerve gases[/morals off]
Well let's hope for the nootropic kind of cholinesterase inhibitor, not the chemical weapon kind...
or better yet, just stay the fuck away from it?
Side-question: when an Alzheimer's patient is exposed to something like VX, is the disease instantly cured before he dies?
If I get Alzheimer's please expose me to VX in the later stages. It's one of the worst ways to die.
