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Ketamine salts solubility

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So it's phenibut but with the alkyl chain altered to overlay valeric acid? Well the former directly binds to GABAb, the latter is a GABAa PAM.

I would be interested to know your thinking as you designed it. Are their receptor models for the binding sites? Do you have a facile synthesis?

Oh, and it's chiral so which isomer do you think will be active?
 
Fertile said:
So it's phenibut but with the alkyl chain altered to overlay valeric acid? Well the former directly binds to GABAb, the latter is a GABAa PAM.

I would be interested to know your thinking as you designed it. Are their receptor models for the binding sites? Do you have a facile synthesis?

Oh, and it's chiral so which isomer do you think will be active?
Click to expand...

I was Just curious about modifying a valproate in unusial way, because I've seen some works where guys were replacing COOH with amide group. I'm a poor chemist that's why nothing is clear with the synthesis. I dont know which isomer would be more active, because phenibut is produced in a racemat form. More studies are needed.
Btw didnt understand your question about receptor model.
We could also add Br or Cl to the ring as it is done in baclophen in order to increase lipophilicity and overall size of the molecule
 
Baclofen is a dirty, dirty drug. I've not tried phenibut but I've not had much luck with related compounds. Not much fun.

I mean, the compound cited might be of medical utility, but I would need to have more to go on. Drug design is not just the answer, it's 'show your working' and that, that is tedious to do (but vital).
 
Phenibut isn’t also not really useful imo. Ceiling effect from 1g on and I can’t find any use for it, as with gabapentin.
You can make a gaba cocktail out of some gbl, a benzo, some alcohol and a little phenibut, that was nice. But apart from that I find it useless.
 
Things like phenibut are simply a molecule of GABA with a liophhilic groups so it will tend towards fat (like the brain). Baclofen, phenibut, tolybut, baclofen, baflofen (baclofen with Cl --> Cl), gabapentin and so on all seem very similar in action.

The only slightly more interesting example is pregabalin because it's chiral. Now, that isobutyl side-chain would most certainly be something worthy of investigation. I've not looked at the patent so I don't know if they tried many substitution patterns or if the size of the moiety is limited due to biosteric minimum and biosteric conformation but the related GHB receptors clearly do allow for quite a lot of bulk. HOCPA would be an interesting vompound to investigate.
 
Coffee drinking and some other herbal and culinary ingredients protect against damage made by ionizing radiation. People who drink more coffee have demonstrably less side effects from radiation therapy of cancer, and even de-caf coffee seems to have some of this effect if too much caffeine causes anxiety. Could be useful in the case of a nuclear disaster/war.

link.springer.com

Pharmacology of natural radioprotectors - Archives of Pharmacal Research

Radiotherapy is one of the most efficient ways to treat cancer. However, deleterious effects, such as acute and chronic toxicities that reduce the quality of life, may result. Naturally occurring compounds have been shown to be non-toxic over wide dose ranges and are inexpensive and effective...
link.springer.com link.springer.com
 
Don't you just hate when you are trying to read the latest publication in The International Journal of Science and Nature and have to pay for the publication to see it? Me too!

And often the scientists who wrote the paper hate pay walls, because they have to pay to publish it, and then make zero profit (other than reputation, the exposure of the science world). So here are a few ways to steal papers.

First and foremost, Scihub. Formed in 2011 by Kazakh undergrad Alexandra Elbakyan, it collects tokens that allow for journal access (such as a university subscription) and uses these to access articles you query (either with the doi or url). Once it grabs an article it archives it for later access. This is my first choice when trying to hunt down an article due to the ease of access and the relative lack of bullshit hoops you need to jump through

The downside of scihub is that it can often be down and depending on how publishing companies are going after it. Also it can often get taken down by hosting companies so I often Google sci hub and try links rather than just relying on a url as they tend to go bad.

I'll post some of the more niche methods later.
 
Thanks, Skorpio. Paywalls and access to published research is definitely an area I feel needs addressing in academia. Fortunately, some journals (e.g., International Journal of Drug Policy) are committed to being Transformative Journals, however, while this is a positive step in the right direction, there’s still plenty of work to do.

Yes, Sci-Hub can be an invaluable resource. You mentioned you’re going to detail some more niche methods later? It could be useful to link a source where people can find currently active Sci-Hub domains?

In addition, there’s also Library Genesis, which provides access to many scholarly or general interest books and academic journal articles. Much like Sci-Hub, Library Genesis has been an invaluable source to many, despite criticisms of piracy.

If you’re not having any luck with the above, you could always:
  1. Contact the corresponding or co-authors of your paper of interest. Most (almost all) journals will have the email address of the corresponding author for the paper - which may not be the first or last author - and it‘s possible to just reach out and express your interest in their work/paper. Sharing a .pdf of the published version of the manuscript is classified as “fair use” and many authors are happy to provide a copy of the manuscript you’re interested in. Often, published papers are shared in good-faith that the recipient will use the file for the own private purposes and not share with authors. If you don’t hear back from the corresponding author, don’t stress, you can simply move on to the next co-author or utilize another approach.

  2. Utilize ArXiv.org. Although, primarily used by researchers in Maths, Physics, Astronomy and Computer Science, the platform now includes researcher from other disciplines. ArXiv is a platform where pre-prints (i.e., often before having undergone peer-review) are made freely available for others to comments on. If authors make changes to the manuscript in response to one of the comments, it must be reflected on the original version.

  3. 3. Install and explore Unpaywall, which is a browser extension for Chrome and Firefox that allows access to a repository of harvested links to Open Acess Peer-reviewed journal articles from around the world.
 
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Sci-Hub is an amazing site, but it seems like over the past couple years it's unable to access a lot of newer papers. In cases where I can't find a paper on Sci-Hub I've always been able to get it on /r/scholar. I miss having a university account though, it was so much easier.
 
One of the chemicals in this one (N-phenethyl-N'-(3-chlorophenyl)piperazine)) is said to have an unbelievably good 0.04 nanomolar affinity for DAT.

www.sciencedirect.com

Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands

Selective σ2 ligands continue to be an active target for medications to attenuate the effects of psychostimulants. In the course of our studies to det…
www.sciencedirect.com www.sciencedirect.com

Edit: it looks like this one has been discussed before: https://bluelight.org/xf/threads/3c-pep-powerful-selective-da-stim-v-close-to-opioids.775533/
 
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Skorpio seems able to get specific articles if asked nicely, but I note he has to be convinced that their is a specific aim and the person isn't just browsing. For browsing, Sci Hub is enough.
 
Science hub mutual aid group

Science hub Mutual Aid community

Mutual Aid Community Committed to:free papers,download research papers for free,free scientific articles,doi unlocker,free scientific papers,scientific articles free,
www.wosonhj.com
This is a site where users post requests, and users with access fill the requests for points. It isn't as likely to have some rare article that you want, but putting a request could get that article acquired for you. I've successfully used it once or twice for things I couldn't sci-hub.
 
Thank you so much for this! One of the main reasons I came back on the site was because I am writing a paper for grad school on the use of psychedelics in a therapeutic setting (such as ketamine) so this is EXTREMELY helpful, thank you!!!
 
Mate - you found me one of the hardest articles to acquire bar none. I hope I explained WHY it was important. Look at 'Opioid Analgesics - Chemistry and Receptors' by Casy et al. Chapter 8 Page 296. Those spirane opioids. I was able to divine QSAR. The p-Me makes it bind to NOP and the N-methyl of the amide overlays the 4 position of the fentanyl class opioids so the methoxymethyl (-CH2OCH3) or carbamate ester (-COOCH3) act like sufentanil or carfentanil analogues.

One of them is x15000 M.

But your paper had one compound with a MOP Ki of 0.0034!!!!!!!!
 
1-phenyl-(1S)-1-methoxy-(2S)-2-ethylaminopropane.png


WOKE
1-phenyl-(1S)-1-methoxy-(2S)-2-ethylaminopropane

Although I am not 100% certain this is the right diastereoisomer, being chiral minded and ending up doing only a single drug rather than a mix of 4 in this case at the same time, may pay off big time.

This issue was brought to my attention after trying racemic ethylamphetamine first and then the pure dextro, single isomer d-NICE.
 
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N-tert-butyl-1-(3-chlorophenyl)-1-oxo-2-aminopropane.png


WELLBUTRIN
N-tert-butyl-1-(3-chlorophenyl)-1-oxo-2-aminopropane

Works surprisingly well when insuffulated.
Mild stimulation, color enhancement, redosable, lasts 2 or 3 hours.
 
N-isopropyl-1-methoxy-1-phenyl-(2S)-2-aminopropane.png


PERPLEX
N-isopropyl-1-methoxy-1-phenyl-(2S)-2-aminopropane

No tengo ningun idea.
 
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