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Improved "benzos"? Options
 
Loveall
#1 Posted : 2/19/2019 7:27:34 AM

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Researches seem to have found how to modify "benzos" to boost therapeutic properties and reduce side effects in clinical pre-trials.

They modified imidazobenzodiaze-pines (e.g. flumazenil) to target only certain GABA receptors. Looks like this was done in modeled simulations first and then they moved to synthesis and in vivo testing.

Paper title (attached): Novel Benzodiazepine-Like Ligands with Various Anxiolytic, Antidepressant, or Pro-Cognitive Profiles

Press release

Interesting and apperently powerful technique. Makes one wonder if any improvements could be done to psychedlic's therapeutic effects (psychoplastogenic and/or cathartic) with a similar technique.
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leratiomyces
#2 Posted : 2/19/2019 10:13:07 AM
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Paper attached appears to be about dmt, not benzos.
 
Loveall
#3 Posted : 2/19/2019 1:52:56 PM

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leratiomyces wrote:
Paper attached appears to be about dmt, not benzos.


My apologies, I selected the wrong paper originally. The correct paper is now attached in the original post above.
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null24
#4 Posted : 2/19/2019 5:24:57 PM

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Wow. They made more addictive drugs to give people when they have a bad day? Confused
They prolly used the same 'breakthrough" hyperbole with valium in the 60s and then xanax in the 90s.

EDIT: obviously a personally informed perspective; it's never the drug, per se, but rather the relationship(s) with it. IN the case of pharms, that is a complex web. I feel that benzos are the invisible quotient of the so-called US 'opioid' epidemic that is seeing overdoses eclipse most other forms of death in this country. Unfortunately, my history includes a intimate knowledge of the destruction that this class of drugs wreaks, and my ire comes from the fact that in every single one of the dozens of overdose deaths I personally know of, I can't think of one in which the deceased wasn't actively using benzos and which they were not a part of. Opiates, other than fent and it's derivatives-which are nothing but weaponized death-rarely kill on their own.

So if my jerking knee caused me to kick you, I apologize, I just really, really hate benzos and yes, there's a big chip on my shoulder. I recall similar language in the 90's around the drugs that are currently sending millions into the hell of addiction and which introduced every addict under 35 I deal with to it.
Sine experientia nihil sufficienter sciri potest -Roger Bacon
*γνῶθι σεαυτόν*
 
Loveall
#5 Posted : 2/19/2019 6:05:35 PM

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null24 wrote:
Wow. They made more addictive drugs to give people when they have a bad day? Confused
They prolly used the same 'breakthrough" hyperbole with valium in the 60s and then xanax in the 90s.


The way I understand it is that they modified benzos to be more specific in their receptor binding so that they are less addictive and more therapeutic with fewer side effects.

This was done by optimizing the molecule's receptor binding profile in a computer model, followed by synthesis and early testing.

If I'm missundertanding the claims in the paper please let me know.

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Th Entity
#6 Posted : 2/19/2019 6:30:25 PM

I can't think of anything important or deep to add here, excuse me!


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Time will tell how effective these amendments are going to be regardig addiction, withdrawals and effectivness for the long term users (patients). I think it will take some time before this sees white world but thats just my opinion.
 
 
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