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  • EADD Moderators: axe battler | Pissed_and_messed

Professor Nutt's magic jizz (Sentia)

Sunday Reads: SENTIA is the Present. Alcarelle is the Future.

SS
Sentia Spirits
[COLOR=var(--textSecondary,#6e6e6e)]To:
[COLOR=var(--textSecondary,#6e6e6e)]Kevin Orourke
[COLOR=var(--textSecondary,#6e6e6e)]Sun 18/06/2023 07:31[/COLOR][/COLOR]


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Quenching your thirst for knowledge: SENTIA is the Present. Alcarelle is the Future


As you know we love receiving your questions about SENTIA Spirits and how GABA works. So, once again our team of innovators and scientists, led by Professor David Nutt, have picked out another three of our most asked questions for you.

So, keep those questions coming in, and let us quench your thirst for knowledge….

1. What’s the difference between Alcarelle & SENTIA?

If you’ve been following us for a while, you may have heard us talk about ‘Alcarelle’ as well as SENTIA, which is why a few of you have asked us what the difference between them is. You might think you’ve already been drinking Alcarelle, or that it’s the active ingredient in SENTIA!

So, let us clarify: SENTIA is the present, Alcarelle is the future.

In the early 2000’s David Nutt, world-renowned neuropsychopharmacologist, and GABA Lab’s Chief Science Officer was tasked by the UK government to propose a 25-year vision for the future of alcohol and this is where he first introduced the concept of a safer, synthetic alternative.

This is what we call Alcarelle, and our ambition is to have Alcarelle licensed and used by drinks producers as an ingredient in place of Alcohol, and it is on track to be ready for 2027. – Should we add in about going through process to be made safe for human consumption? Or is it better to not even plant the question that safety is an issue?

SENTIA, however, is a ‘proof-of-concept’, a powerful botanical blend proven to target ‘GABA’ – the neurotransmitter responsible for sociable feelings – in the brain. SENTIA’s plant-based ingredients are all ‘GABAergic’, which means that they enhance and activate the pre-existing ‘GABA’ in our bodies. SENTIA gives the same convivial effect as Alcarelle will, but to a lesser degree.

SENTIA is proof that a truly functional alcohol alternative is possible


2027 😎. Received this email today
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Looks like this GP had magic jizz too:

A GP in England has been found guilty of a sexual offence after he deposited his semen into a woman’s coffee. The victim told a trial she would pour ‘salty’ coffee away but always noticed a ‘thick, gloopy’ substance in the sink.

Dr Nicholas Chapman, 55, filled up hundreds of ‘specimen’ samples and was accused of dropping them into his victim’s hot drinks on multiple occasions over the course of a year. The victim - who hasn’t been named for legal reasons - became suspicious when she discovered a collection of the samples a year later
 
Looks like this GP had magic jizz too:

A GP in England has been found guilty of a sexual offence after he deposited his semen into a woman’s coffee. The victim told a trial she would pour ‘salty’ coffee away but always noticed a ‘thick, gloopy’ substance in the sink.

Dr Nicholas Chapman, 55, filled up hundreds of ‘specimen’ samples and was accused of dropping them into his victim’s hot drinks on multiple occasions over the course of a year. The victim - who hasn’t been named for legal reasons - became suspicious when she discovered a collection of the samples a year later
Morning cuppa
 
His defence could be that he did ask her if she wanted cream in her coffee (fnarr fnarr!), and it's all just been a massive misunderstanding.

This would be better than his actual defence, which is claiming that he has a rare medical condition which makes him ejaculate when he takes a shit. Seriously. That is the defence he is going with.

Apparently that disorder is an actual thing, but on the remotest chance that he actually had it, that would mean that he didn't wash his hands after spaffing everywhere whilst having a shit, and / or that he took the coffee cups into the toilet with him. Pretty gross all round whatever the case.

Surely he'll have to prove that he has that disorder for his defence to have any chance.

I'd say he's guilty just because he looks even more of a creepy weasel than Michael Gove, and I'd be surprised if some revelations or other don't come up in connection with him.

That defence is mentioned in this article I posted In gibberings a few days ago, although it now looks he's deciding to use the defence of "it was just a prank"

The phrase 'clutching at straws' springs to mind.

 
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It will be interesting to read any GABA labs patents BECAUSE I sent the QSAR for both 1,4-benzodiazepines and 1,5-benzodiazepines that are a5 selective... and Nutt replied to my E-mails. So IF they attempt to patent any of the compounds I designed, I actually have proof that they are not novel (so cannot be patented.

I've mentioned pyeyzolam which was my first design and GABA labs (under it's previous name 'Alcorette') paid me for the rights (and I have copies of said sale) BUT it only covers 3 specific compounds i.e.

Pyeyzolam - a5-selective benzo that emulates 'drunk' but cannot emulate '2 glasses of wine' i.e. I discovered the receptor that high doses of ethanol bind to.

Pynazolam - a benzo that is actually a selective serotonin releaser which emulated the relaxation and euphoria ethanol produces.

Pynazolam - which the above were both made from.

But I later figured out that lower doses of alcohol preferentially bind to the a5b2y2 receptor and sent Nutt the design for Pyeybazam which has been made and tested and DOES emulate lower doses of ethanol.

So to emulate alcohol from 1 glass of wine to a bottle of vodka actually required 2 different compounds, specifically a 3:1 mixture of Pyeybazam:pyeyzolam. Now, getting a marketing licence when their are 2 actives is just HUGELY costly.

So what did I do next? I found a compound that acted at both the a5b1y2 AND a5b2y2 GABA receptors. Now THAT they do not have. It took the team a fair old while to figure out how to produce an asymmetrical dimer (so technically not a dimer but chemists will know what I mean). It required an unusual synthetic technique and even then the product wasn't pure and required biocatalytic resolution (the impurities cannot be removed using HPLC or any other purely chemical technique).

I should add we didn't DISCOVER this method or resolving mixtures but knowing the appropriate biocatalyst and conditions resulted in a LOT of trial end error. But if people wish to see pyeyzolam, pynazolam and pyeybazam, here they are:


So the only things I'm not showing is the single chiral compound that is a5b1y2/a5b2y2 selective and which about 5mg equals 1 UK unit of alcohol.

Of course it's quite possible that GABA Labs are working with an entirely new scaffold. The most obvious one to me is those found in Kava, specifically kavain, dihydrokavain and methysticin although out limited studies showed that the natural compounds are VERY costly to extract so they would have to produce them synthetically and the law is much laxer on natural compounds as compared to synthetics. We did briefly think that it's impossible to tell if a given compound was produced by a plant or by synthesis but that IS dubious legal ground and if anyone remembers tryptophan being banned. The Chinese were CLAIMING to have extracted it from plants but were in fact making it synthetically and as it turned out, their was an impurity that turned out to be chronically toxic.. so we gave up on that one.
 
Well, the compounds I've shown were the ones sold to Nutt (Alcorette) and patented so yes, they are in the public domain.
If they are not patented then can anyone use them?

I thought it you sold them then only the buyer could use them.
 
Yes - you asked if they were in the public domain which they are. All patents are in the public domain BUT ownership of the intellectual property is in the hands of Alcorette AKA GABA Labs.

But since it's very specifically JUST those 3 compounds, one can easily develop an analogue that isn't patented. If you want a legal-to-produce pyeyzolam homologue, just add a 4-methyl thus:


Call it mepyeyzolam or something.

You see the thing is that it wasn't so much the specific compound, it was IDENTIFYING that the a5b1y2 subtype is responsible for all of the positive effects of alcohol.

Oh, and MOST of the negative effects (all the emotional and behavioral ones) are mediated by the a1b1y2 subtype.
 
Yes - you asked if they were in the public domain which they are. All patents are in the public domain BUT ownership of the intellectual property is in the hands of Alcorette AKA GABA Labs.

But since it's very specifically JUST those 3 compounds, one can easily develop an analogue that isn't patented. If you want a legal-to-produce pyeyzolam homologue, just add a 4-methyl thus:


Call it mepyeyzolam or something.

You see the thing is that it wasn't so much the specific compound, it was IDENTIFYING that the a5b1y2 subtype is responsible for all of the positive effects of alcohol.

Oh, and MOST of the negative effects (all the emotional and behavioral ones) are mediated by the a1b1y2 subtype.
Bottom line.. does this help the cause to release this alcarelle, or add another hurdle?
 
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