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Sedatives of the Future

nuke

nuke

Bluelighter
Joined
Nov 7, 2004
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We have plenty of threads on stimulants and psychedelics, but not one for general sedatives. My curiousity lies in new sorts of methaqualones, benzodiazepines, barbiturates, et cetera.

I have no idea how to start the thread, however. I know very little about any new drugs in this field of research, so perhaps someone else could start the discussion.
 
Sorry, I don't really know, but I'm guessing pharm companies are really playing around with anti-histamines. They work (for sedation) pretty good, there is very little abuse potential, benzos have an extremely bad reputation in the pharmaceutical industry and many, many doctors are switching their patients on to less addictive substances to treat insomnia. For anxiety and panic attacks though, I'm sure drugs like Clonazepam and Alprazolam are as effective as they want them to be, respectively. I could be wrong, though...
 
Diacetylus, we're talking about recreational sedatives here. :)

Euphoria. Hopefully something more euphoric than GHB and Quaaludes combined, that's active at microgram doses, and easy to synthesize.
 
Why active at microgram doses if it's easy to synth? All that's going to do is make it exclusively usable by the drug elite with amazing scales... Actually that's a damn good idea! haha

Although I can't comment on Quaaludes, I'd be very suprised to see anything more euphoric than GHB hitting the market any time soon. I'd like to see a substance similar to GHB with a less steep dose response curve so that it's safer :) Also longer acting would be nice too, it gets annoying having to measure out doses every hour or so. I'd also like it if the effects didn't build up over a few doses like it does with G, nothing more annoying than taking a tiny dose after a big night out on it and just falling asleep.
 
Im guessing it might be worth doing a study on any ludes analogs that are a bit more potent. You aint gonna get microgram active but valium led to some pretty strong derivatives nevertheless. I wonder if there is a klonopin equivalent of 'aqualone

methaqualone_2d.jpg
 
Grrr, I wish Methaqualone was still around, I'd give just about ANYTHING to try that shit!
 
The OCDS mentions methaqualone and mecaqualone (sp?), where the ortho methyl has been swapped for a chlorine. Erowid.org lists a threshold dosage of 75 mg and a common dosage of 300 mg. That doesn't sound too potent. Do any of you who know something about pharmacology have any ideas as to why it would require a comparatively high dosage range? Also, are there any significant differences between the chloro and methyl analogs?
If I haven't missed anything, the nitrogen alpha to the carbonyl is sp2 hybridized, making the diazo- ring also aromatic, and rendering the molecule completely planar.
Incidentally, the triazo series of benzodiazepines are also completely planar. However, I have no reason to believe they bind to the same site on the GABA receptor.
 
Concerning sleeping pills, it seems that they try to find some molecules with a very targeted action (drugs that make you sleep without losing your memory, getting high, etc...)

Barbituates are "1st generation sedatives"; benzodiazepines are the 2nd generation, and the 3d generation of sedatives is Zolpidem/Zopiclone/Zaleplon.
(I don't know where the carbamates (Meprobamate, Carisoprodol), the Methaqualone derivatives, Etchlorvynol; Gluthetimide, etc... fit in this classification...)

Zolpidem/Zopiclone/Zaleplon are selective for GABA-A receptors, while benzos (I think) affect all GABA receptors...
And it seems that they want to make sedatives/tranquilizers with a more selective action; Eszopiclone is a good exemple of a new generation sedative.
 
jasoncrest said:
Concerning sleeping pills, it seems that they try to find some molecules with a very targeted action (drugs that make you sleep without losing your memory, getting high, etc...)

Zolpidem/Zopiclone/Zaleplon are selective for GABA-A receptors, while benzos (I think) affect all GABA receptors...
And it seems that they want to make sedatives/tranquilizers with a more selective action; Eszopiclone is a good exemple of a new generation sedative.
Click to expand...

It's strange, because it seems like zolpidem has an abuse potential, with many users reporting hallucinations and memory loss. The addiction potential is lower, but the pharmaceutical industry is still fairly aware that it has its niche of recreational Ambien users now. I've always been curious if zolpidem has some impact on 5HT2A/C, because users often mention serotonergic like hallucinations, and because zolpidem's shape is tryptamine like (but I bet the extra nitrogen would screw up most of the serotonin binding by making it non-planar).
 
mepat1111 said:
Grrr, I wish Methaqualone was still around, I'd give just about ANYTHING to try that shit!
Click to expand...

those are still available in canada... i wonder how hard it is to get some prescribed..
 
In France, a few Quinazoline derivatives were commercialized:

-METHAQUALONE (anxiolytic, muscle-relaxant, sedative, anticonvulsant, antihistaminic....)
-CLOROQUALONE (sedative, antitussive...)
-DIPROQUALONE (analgesic, sedative, anxiolytic, muscle-relaxant, antihistaminic...)
-MECLOQUALONE (hypnotic...)

They were all Methaqualone derivates, and they were all CNS depressants, but they all had their own particular properties: Meclo- was the hypnotic, Cloro- was the antitussive, Dipro- was the analgesic, and Metha- was the anxiolytic & muscle-relaxant....



Concerning the CNS depressants families, I think the Barbituates, the Benzos, the Carbamates are all well-known, and the scientists tried to make many different derivatives of them.
The Quinazoline family seems to be very interesting, and so is the Ethchlorvynol/Gluthetimide family....
(Does anyone know anything about Methyprylon?)
 
Kurv. said:
those are still available in canada... i wonder how hard it is to get some prescribed..
Click to expand...

they're a huge problem in south africa now, from diverted pharmaceutical sources. people smoke the pills, apparently it has a very strong addiction potential.
 
Coolio said:
Diacetylus, we're talking about recreational sedatives here. :)

Euphoria. Hopefully something more euphoric than GHB and Quaaludes combined, that's active at microgram doses, and easy to synthesize.
Click to expand...

U forgot it need to grow on the trees ;)
 
http://www.ncbi.nlm.nih.gov/entrez/..._uids=15769868&query_hl=2&itool=pubmed_DocSum

To the extent that different behavioral effects of GHB are mediated by different mechanisms (e.g., GHB, GABAB, or other receptors), compounds that are selective for GHB receptors might retain some of the therapeutic effects of GHB, while having fewer undesired effects. The present studies have identified UMB86, UMB72, UMB73, and 3-HPA as selective GHB analogs that exhibit some, but not all, of the behavioral effects of GHB and its precursors GBL and 1,4-BDL; these compounds will be helpful tools to investigate the role of GHB receptors in the behavioral profile of GHB.
Click to expand...
 
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Our future direction will consist of follow-up and continuation of present lines of research, taking advantage of research breakthroughs and opportunistic advances in the field. Our lead GABAmimetic therapeutic compound, gamma-vinyl-GABA, has already advanced to clinical trials in human patients with promising initial open-label results.
Click to expand...

http://www.drugabuse.gov/DIR/neuropsycho.html

Therapeutic, eh? Hmm.
 
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