You tolerance may have been low if you haven't drank for a while.
Also an empty stomach can make 2 beers feel like 5
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N&PD Moderators: Skorpio | thegreenhand
New secretive "alcohol alternative"
- Thread starter Snafu in the Void
- Start date
Also an empty stomach can make 2 beers feel like 5
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I don't think so, but possible. I'm an alcoholic and used high doses of kratom and alcohol (on the same day, but typically not together) and never really had any major side effects or interaction other than the occasional upset stomach.
Unfortunately I have the alcoholism genetics, it's quite euphoric and also a psychomotor stimulant in me. Still a shit drug, but I get more out of it than most people.
Fertile
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Prenderol (2,2-diethyl-1,3-propanediol) seems to be commercially availale and certain cyclodextrins will absorb up to 60% of the total mass. Of course, it's potency makes it a non-starter.
Id only one could find something similar to methaqualone that was as cheap to produce. Don't forget that for 10 years the US only saw illicit tablets and they still sell in South Africa. But it's dangerous stuff. It's all well and good to make castles in the air, quite another when people are harmed.
Id only one could find something similar to methaqualone that was as cheap to produce. Don't forget that for 10 years the US only saw illicit tablets and they still sell in South Africa. But it's dangerous stuff. It's all well and good to make castles in the air, quite another when people are harmed.
Fertile
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BTW Pyeyzolam is in the process of being patented.
30mg ≈ bottle of vodka.
Non-toxic (no hangover or day after anxiety), T1/2 of 2 hours (so one is sober in 12 hours) and can be made in 2 steps from pyrazolam.
The problem is that it will only emulate 'drunk'. It cannot emulate '2 glasses of wine'. That problem has now been overcome by using a second compound. The mixture (20mg of pyeyzolam + 40mg of the new compound) dissolved into 750mL (i.e. a bottle) of distilled water or a flavouring means one can get the effects of ANY dose of alcohol.
The second compound hasn't been patented yet, so I cannot disclose it's structure.
I might add that the 8 ethynyl (CH≡C-) moiety may be swapped for a trimethylsilyl ((CH3)3SI-) which appears to produce identical effects. We didn't go with the trimethylsilyl because we weren't sure of metasbolism. As it is, pyeyzolam and the new compound are excreted unchanged which makes licencing MUCH easier/cheaper because you don't need to find activity/toxicity of metabolites.
30mg ≈ bottle of vodka.
Non-toxic (no hangover or day after anxiety), T1/2 of 2 hours (so one is sober in 12 hours) and can be made in 2 steps from pyrazolam.
The problem is that it will only emulate 'drunk'. It cannot emulate '2 glasses of wine'. That problem has now been overcome by using a second compound. The mixture (20mg of pyeyzolam + 40mg of the new compound) dissolved into 750mL (i.e. a bottle) of distilled water or a flavouring means one can get the effects of ANY dose of alcohol.
The second compound hasn't been patented yet, so I cannot disclose it's structure.
I might add that the 8 ethynyl (CH≡C-) moiety may be swapped for a trimethylsilyl ((CH3)3SI-) which appears to produce identical effects. We didn't go with the trimethylsilyl because we weren't sure of metasbolism. As it is, pyeyzolam and the new compound are excreted unchanged which makes licencing MUCH easier/cheaper because you don't need to find activity/toxicity of metabolites.
So what's the plan? Market it as a drink and sell it as an alternative to alcohol?BTW Pyeyzolam is in the process of being patented.
30mg ≈ bottle of vodka.
Non-toxic (no hangover or day after anxiety), T1/2 of 2 hours (so one is sober in 12 hours) and can be made in 2 steps from pyrazolam.
The problem is that it will only emulate 'drunk'. It cannot emulate '2 glasses of wine'. That problem has now been overcome by using a second compound. The mixture (20mg of pyeyzolam + 40mg of the new compound) dissolved into 750mL (i.e. a bottle) of distilled water or a flavouring means one can get the effects of ANY dose of alcohol.
The second compound hasn't been patented yet, so I cannot disclose it's structure.
I might add that the 8 ethynyl (CH≡C-) moiety may be swapped for a trimethylsilyl ((CH3)3SI-) which appears to produce identical effects. We didn't go with the trimethylsilyl because we weren't sure of metasbolism. As it is, pyeyzolam and the new compound are excreted unchanged which makes licencing MUCH easier/cheaper because you don't need to find activity/toxicity of metabolites.
Fertile
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I'm in the UK and so the Psychoactive Substance Act makes further research very difficult. But the above was not perfect. The dose-response curve is not linear. Up to 20mg it does NOTHING and then between 20mg & 30mg one goes from 'merry' to 'drunk;' very quickly.
It turns out it's because at low doses, alcohol primarily binds to the a1b1y1 GABA subtype and only at higher doses does it affect the a5b1y1 subunit. It's hugely important to be able to emulate the positive effects of alcohol perfectly. It doesn't emulate the negative effects i.e.
-Mood Lability
-Loss of Judgement
-anterograde amnesia
-hyperphagia
-Aggression
-Loss of balance
-Retrograde amnesia
-Nausea/emesis
-dehydration
-Disturbed sleep
And so, no hang-over next day (thirst, headache, anxiety, nausea, hyperacusis and so on). It's calorie-free and it's effects can be reversed in an emergency.
BTW we discovered that all of the negative mental effects of alcohol are due to ethanol's affinity to the a1b1y1 subtype. That is why their are news stories of famous people getting on a plane, taking a sleeper (usually a Z-drug i.e. zopiclone, zolpidem or zimovane) and behaving in a bizarre manner, The Z drugs are a1b1y1 selective so these people act crazy and cannot remember it - it's not an excuse, Z-drugs really do this. If nothing else, we proved Z-drugs are a BAD idea. 2mg of alprazolam is a MUCH better option (no a1b1y2 affinity).
But as I said, the compound I specify will emulate 'drunk' but not 2 bottles of beer. It needs a compound that is selective to a second GABA receptor subtype. Specifically it needs an a5b2y1 PAM and I have one. I have to synthesis worked out. It's not cheap to have samples made but the team who does our lab-work calculated that at scale, the cost of each would be be $1400/Kg. So a 750mL bottle with 40:20mg would mean >16 bottle per gram i.e. 17¢ each. A lot CHEAPER than distilling mash.
But how does one introduce it? It's not a medicine so it cannot be licenced (although we did consider going down that route to get it accepted - as a treatment for alcoholics initially) and THEN suggest a GSL (general sales licence).
Sorry to bang on, but I di all of this work 10 years ago but I'm purely a technical guy. I wouldn't know how to steer this through trials, to deal with the UK government and HMCE (because I am guessing the government would want to add tax and duty).
Last point - since it has no a1b1y1 affinity, it's dependence liability is much lower than most benzodiazepines. I'm pretty sure it has SOME dependence liability but other than 'low' I cannot specify it.
So 50,000 people a year die because of alcohol while I'm sat here unable to do anything to help.
BTW the BEST alcohol-like medicine on the market is without a doubt chlormethiazole (Heminevrin/Nevrin) that was discovered in 1932. It comes as 192mg capsules (192mg = 3 grains... THAT is how old it is!) or a a solution of the ethanedisulfonate salt. If you can get it, it's well worth tryting/ Just don't mix it with any other CNS depressant. Only take 1. As a friend said 'take 2 and you just wake up 6 hours later wondering where you are). Now THAT is possible to get.
I'm also in UK. I wonder if David Nutt has the patient?
Fertile
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He bought it from me - BUT he didn't buy the patent for the second compound thus I can patent the mixture AND the second compound, I can mention it now because Alcorette has patented it.
I should add that we also found an even more euphoric compound. It's a benzo that is also a potent serotonin-releaser and serotonin-reuptake inhibitor and people who know have told me that subjectively, it's identical to methaqualone. The difference is that one needs to take 300-600mg of methaqualone and only 3-6mg of my compound.
The lab synthesis was tricky BUT if scaled, an appropriate precursor would be produced and so estimated cost is $1600/Kg.
All I can tell you is that EVERYONE who tried the stuff asked me if I had any more. If you haven't tried methaqualone, it's hard to describe but HIGHLY EUPHORIC covers it. Once again, I ensured it has no a1b1y1 affinity so no amnesia, mood lability, aggression, loss of balance or loss of judgement.
It lasts about 6 hours and believe me - just lying on your bed staring at the ceiling on the stuff is more euphoric than anything you could possibly do WITHOUT the drug.
And once again, it's very non-toxic, doesn't undergo metabolism and thus is excreted unchanged. I really did meet people who stored their own urine with a view to drinking it again to get another hit.
I also found a much more potent and SAFE methaqualone homologue:
The above is active at 15-30mg and it's effects are identical to methaqualone.... but the other thing I developed costs significantly less per dose and the all-important precursor is commercially available. This requires some unusual materials. That chloromethyl doubles potency, the o-nitro increases potency x10. The p-Me is required partly for metabolism and partly to make the active conformation the lowest energy conformation. Doesn't alter potency but makes onset slower, duration longer (and I think 8 hours is as long as you want).
I like thinks that come on fast and end quickly. This goes from 'full on' to almost nothing in 30 minutes - their isn't a 4 hour period of it wearing off.
Wow David Nutt bought it? Alcarelle hopefully coming..or something similarHe bought it from me - BUT he didn't buy the patent for the second compound thus I can patent the mixture AND the second compound, I can mention it now because Alcorette has patented it.
I should add that we also found an even more euphoric compound. It's a benzo that is also a potent serotonin-releaser and serotonin-reuptake inhibitor and people who know have told me that subjectively, it's identical to methaqualone. The difference is that one needs to take 300-600mg of methaqualone and only 3-6mg of my compound.
The lab synthesis was tricky BUT if scaled, an appropriate precursor would be produced and so estimated cost is $1600/Kg.
All I can tell you is that EVERYONE who tried the stuff asked me if I had any more. If you haven't tried methaqualone, it's hard to describe but HIGHLY EUPHORIC covers it. Once again, I ensured it has no a1b1y1 affinity so no amnesia, mood lability, aggression, loss of balance or loss of judgement.
It lasts about 6 hours and believe me - just lying on your bed staring at the ceiling on the stuff is more euphoric than anything you could possibly do WITHOUT the drug.
And once again, it's very non-toxic, doesn't undergo metabolism and thus is excreted unchanged. I really did meet people who stored their own urine with a view to drinking it again to get another hit.
I also found a much more potent and SAFE methaqualone homologue:
The above is active at 15-30mg and it's effects are identical to methaqualone.... but the other thing I developed costs significantly less per dose and the all-important precursor is commercially available. This requires some unusual materials. That chloromethyl doubles potency, the o-nitro increases potency x10. The p-Me is required partly for metabolism and partly to make the active conformation the lowest energy conformation. Doesn't alter potency but makes onset slower, duration longer (and I think 8 hours is as long as you want).
I like thinks that come on fast and end quickly. This goes from 'full on' to almost nothing in 30 minutes - their isn't a 4 hour period of it wearing off.
As a drinker who likes both drinking loads but also just a few pints with a mate, I'm looking for something that is a good alternative to alcohol. Doesn't have to be strong. Just need something to give an effect.
Will watch the next few years closely.
Will watch the next few years closely.
Fertile
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Well, it turned out that in the 1970s, when Jackson B. Hester was working on the triazolo class of benzodiazepines, he did, in fact, produce pyrazolam. He didn't even test it, it's just one of the several hundred compounds listed in his patent, so the compound itself couldn't be patented although it's selectivity - an idea not known in the 70s MIGHT allow it to be used in an SR formulation for GAD as it's much, much less dependence-forming (something else he missed.... in fact in the 1970s people were denying that benzos WERE addictive).
Then, in the 1980s James Cook (considered world expert in designing selective benzodiazepines) made pyeyzolam BUT because it was unexpectedly INACTIVE (nothing happens until you reach 0.4mg/Kg), he just added it to HIS patent. So it's action was never characterised. Nutt bought the patent rights off me, showed them to Cook and THEN discovered he couldn't patent it!
But as I have said, pyeyzolam alone will emulate 'drunk' wonderfully. Better than alcohol itself. The problem is that it cannot emulate low doses of alcohol so you cannot get '2 glasses of wine merry' with the stuff. I discovered this problem and I then found an answer to it. Nutt KNOWS I have the answer BUT he has formed a company with Cook and evidently they think they can find it without me. As it goes, I have slightly modified pyeyzolam so I CAN patent this one (currently named Hanazepam). I have had made and tested the mixture so I can now emulate 1 glass of wine right up to 2 bottles of vodka. The second compound is currently named Hanazolam).
I THINK I can obtain a sample of pyeyzolam from the people who made if for me but it would be expensive. It would be 0.5-1g which at 30mg = bottle of vodka, it's still 33 bottles-worth and proves that I am not just making this up OR seeking to cheat you (since I never have possession of it - it's sent from them to you). This IS a potential commercial venture. The biggest hurdle is that the alcohol industry will do their very best to put a stop to it as it would destroy them. If they were smart, they would just dissolve 30mg Hanazepam &75mg of Hanazolam into a 750mL bottle of liquid - a very nicely flavoured liquid (both compounds are sufficiently water soluble for 1 gram to dissolve in 1L of water at STP).
If you are seriously thinking of investing, I can even give you their name, address and contact details BUT unless they know I sent you, they won't even admit to having ever produced it).
I should add that all of this is 100% LEGAL. I am a technical person. I know nothing about business, nothing about tax or duty or shipping, wholesale, retail or any of those things. I can design a compound to produce a specific effect (I was asked to make an 'alcohol pill'), deal with the toxicology, trials and licencing (and for the latter you have to fill in 2 documents. The first is 1194 pages long, the latter 914 pages long) so it's a lot of work... but I've done it before, I've worked with Huntingdon Life Sciences and understand these initial steps.... but anything beyond the output of a V-mixer (where the Hanazolam and Hanazepam are mixed) is a mystery to me.
I suggested to Nutt that he get Pyeyzolam licenced as a medicine to treat alcoholism (we tried it, it works a lot better than chlorodiazepoxide and better than chlormethiazole. The latter being considered a DLR (drug of last resort). Obviously now it would be getting Hanazepam and Hanazolam licenced in a similar manner. Once it's truly massive therapeutic index and low-toxicity are proven, a GSL (general sales licence) could be applied for.
BTW Anybody got thoughts on what the stuff should be called (the mixture of the 2 compounds)? In this world, the guy who came up with the name Xanax earnt more than the guy who invented alprazolam. I know this because Dan Lednicer was a close friend and told me all about Upjohn's development lab. They has:
-Dan Lednicer (who developed BDPC and the much better MDPC)
-Philip Voigtlander (who further developed work by lead chemists)
-Jackson B. Hester (developed alprazolam, ketazolam and adinazolam)
-Jacob Szmuszkovicz (developed U-47700, U-77891 and a series of kappa ligands)
-Robert C. Kelly (developed a technique to separate the endo and exo forms of drugs like 4MAR)
-Verlan H. Van Rheenen (developed the field of steroid chemistry HUGELY)
-Walter Morozowich (developed formulations for insoluble or unstable drugs)
-Donald W. DuCharme (developed a new class of antiarrhythmics.
-William P. Schneider (who developed the method to humanise immunobulins)
-Charles M. Hall (who developed treatment for skin conditions)
-Milton E. Herr (who invented anti inflammatory drugs)
-Gabriel Kornis (who developed antibiotics - especially prodrugs to widen the utility of existing, proven agents).
They were termed 'Upjohn's Dream Team'.
Sadly, I think the only one left is Philip Voigtlander. I know he kept in touch with Dan and worked on several projects with Dan. Somewhere their is an amazing picture of them both stood next to a plastic model of the BDPC molecule in it's minimum-energy conformation. They had to calculate the minimum-energy by hand so what you see is about 10 days work. Dan was astonished to discover than BDPC and fentanyl overlay perfectly.
That is why I recommend people spend £120 on an old version of ChemOffice off Ebay. As long as it is sealed and the serial number hasn't been used, you get arguably the best organic chemistry software on the planet. It performs energy minimisation in 10-20 seconds and I discovered (for example) that U-47700 & (3R,4S) prodine overlay perfectly. The N-methyl of U4 overlays the methyl side-chain on the poperidine ring.!
Then, in the 1980s James Cook (considered world expert in designing selective benzodiazepines) made pyeyzolam BUT because it was unexpectedly INACTIVE (nothing happens until you reach 0.4mg/Kg), he just added it to HIS patent. So it's action was never characterised. Nutt bought the patent rights off me, showed them to Cook and THEN discovered he couldn't patent it!
But as I have said, pyeyzolam alone will emulate 'drunk' wonderfully. Better than alcohol itself. The problem is that it cannot emulate low doses of alcohol so you cannot get '2 glasses of wine merry' with the stuff. I discovered this problem and I then found an answer to it. Nutt KNOWS I have the answer BUT he has formed a company with Cook and evidently they think they can find it without me. As it goes, I have slightly modified pyeyzolam so I CAN patent this one (currently named Hanazepam). I have had made and tested the mixture so I can now emulate 1 glass of wine right up to 2 bottles of vodka. The second compound is currently named Hanazolam).
I THINK I can obtain a sample of pyeyzolam from the people who made if for me but it would be expensive. It would be 0.5-1g which at 30mg = bottle of vodka, it's still 33 bottles-worth and proves that I am not just making this up OR seeking to cheat you (since I never have possession of it - it's sent from them to you). This IS a potential commercial venture. The biggest hurdle is that the alcohol industry will do their very best to put a stop to it as it would destroy them. If they were smart, they would just dissolve 30mg Hanazepam &75mg of Hanazolam into a 750mL bottle of liquid - a very nicely flavoured liquid (both compounds are sufficiently water soluble for 1 gram to dissolve in 1L of water at STP).
If you are seriously thinking of investing, I can even give you their name, address and contact details BUT unless they know I sent you, they won't even admit to having ever produced it).
I should add that all of this is 100% LEGAL. I am a technical person. I know nothing about business, nothing about tax or duty or shipping, wholesale, retail or any of those things. I can design a compound to produce a specific effect (I was asked to make an 'alcohol pill'), deal with the toxicology, trials and licencing (and for the latter you have to fill in 2 documents. The first is 1194 pages long, the latter 914 pages long) so it's a lot of work... but I've done it before, I've worked with Huntingdon Life Sciences and understand these initial steps.... but anything beyond the output of a V-mixer (where the Hanazolam and Hanazepam are mixed) is a mystery to me.
I suggested to Nutt that he get Pyeyzolam licenced as a medicine to treat alcoholism (we tried it, it works a lot better than chlorodiazepoxide and better than chlormethiazole. The latter being considered a DLR (drug of last resort). Obviously now it would be getting Hanazepam and Hanazolam licenced in a similar manner. Once it's truly massive therapeutic index and low-toxicity are proven, a GSL (general sales licence) could be applied for.
BTW Anybody got thoughts on what the stuff should be called (the mixture of the 2 compounds)? In this world, the guy who came up with the name Xanax earnt more than the guy who invented alprazolam. I know this because Dan Lednicer was a close friend and told me all about Upjohn's development lab. They has:
-Dan Lednicer (who developed BDPC and the much better MDPC)
-Philip Voigtlander (who further developed work by lead chemists)
-Jackson B. Hester (developed alprazolam, ketazolam and adinazolam)
-Jacob Szmuszkovicz (developed U-47700, U-77891 and a series of kappa ligands)
-Robert C. Kelly (developed a technique to separate the endo and exo forms of drugs like 4MAR)
-Verlan H. Van Rheenen (developed the field of steroid chemistry HUGELY)
-Walter Morozowich (developed formulations for insoluble or unstable drugs)
-Donald W. DuCharme (developed a new class of antiarrhythmics.
-William P. Schneider (who developed the method to humanise immunobulins)
-Charles M. Hall (who developed treatment for skin conditions)
-Milton E. Herr (who invented anti inflammatory drugs)
-Gabriel Kornis (who developed antibiotics - especially prodrugs to widen the utility of existing, proven agents).
They were termed 'Upjohn's Dream Team'.
Sadly, I think the only one left is Philip Voigtlander. I know he kept in touch with Dan and worked on several projects with Dan. Somewhere their is an amazing picture of them both stood next to a plastic model of the BDPC molecule in it's minimum-energy conformation. They had to calculate the minimum-energy by hand so what you see is about 10 days work. Dan was astonished to discover than BDPC and fentanyl overlay perfectly.
That is why I recommend people spend £120 on an old version of ChemOffice off Ebay. As long as it is sealed and the serial number hasn't been used, you get arguably the best organic chemistry software on the planet. It performs energy minimisation in 10-20 seconds and I discovered (for example) that U-47700 & (3R,4S) prodine overlay perfectly. The N-methyl of U4 overlays the methyl side-chain on the poperidine ring.!
You should work with Nutt I'd say.
Is this alcarelle sounding promising?
You seen this from 2010 by the way??
While ago now.
Fertile
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I hadn't seen this - I think that it IS pyeyzolam. He calls ALL of his drugs 'alcosynth', it's a marketing thing i.e. not my realm. Before pyeyzolam he tried pagoclone. The problem is that pagoclone has a1 affinity so it CAN cause many of the negative effects of alcohol and is dependence-forming.
-Labile mood
-Loss of judgement
-retrograde & anterograde amnesia
-Loss of balance
An altered sleep - it suppresses stage 4 slow-wave sleep.
Now Nutt reckons to have a herbal alternative to alcohol in 5 years and a synthetic alternative to alcohol in 10 years. Well, we have all seen numerous 'herbal alternatives' and none of them are much cop. I think he's doing it JUST to keep a media profile.
I much prefer the opposite approach - a fait accompli with my name never even surfacing. Not because I'm a criminal or because I worry people will think I'm rich but because I don't believe that 1 or 2 names on a patent anywhere nearly matches the number of hours put in by the scores of people involved in making a new drug.
I should add that I know how to make related compounds that are much more potent (like x10 more potent). This, for example, would be much like pyeyzolam but would only need 3mg.... but the dose/response curve would be even steeper, duration longer, it would produce negative effects and be dependence-forming. But I want it to be identical to alcohol, not 'kind of similar'.
Of course, the money men don't REALLY care about the end users. As long as it's well established, shares have been sold at a huge profit and the design licenced out for an even huger profit BEFORE questions are asked. But I wouldn't want to be famous for making a drug that destroyed lived.
Thus I will remain poor.
-Labile mood
-Loss of judgement
-retrograde & anterograde amnesia
-Loss of balance
An altered sleep - it suppresses stage 4 slow-wave sleep.
Now Nutt reckons to have a herbal alternative to alcohol in 5 years and a synthetic alternative to alcohol in 10 years. Well, we have all seen numerous 'herbal alternatives' and none of them are much cop. I think he's doing it JUST to keep a media profile.
I much prefer the opposite approach - a fait accompli with my name never even surfacing. Not because I'm a criminal or because I worry people will think I'm rich but because I don't believe that 1 or 2 names on a patent anywhere nearly matches the number of hours put in by the scores of people involved in making a new drug.
I should add that I know how to make related compounds that are much more potent (like x10 more potent). This, for example, would be much like pyeyzolam but would only need 3mg.... but the dose/response curve would be even steeper, duration longer, it would produce negative effects and be dependence-forming. But I want it to be identical to alcohol, not 'kind of similar'.
Of course, the money men don't REALLY care about the end users. As long as it's well established, shares have been sold at a huge profit and the design licenced out for an even huger profit BEFORE questions are asked. But I wouldn't want to be famous for making a drug that destroyed lived.
Thus I will remain poor.
Nutt's herbal one is the sentia and nothing happens when you drink it that I can feel. I did feel something once but can't seem to repeat this mild feeling.
But he has the real synthetic alcohol ready and reckons the key year will be 2025.
I reckon he consumers it himself at the Nutt dinner table or family picnic.
Do your compounds also have maximum dosage?
But he has the real synthetic alcohol ready and reckons the key year will be 2025.
I reckon he consumers it himself at the Nutt dinner table or family picnic.
Do your compounds also have maximum dosage?
Fertile
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Well - it's TI is well over 200 which is HUGE and if it were dissolved in water to make it as potent as vodka, it would be like drinking 200 bottles of vodka with no toxic effects - you just fall asleep.
But I'm not convinced Nutt HAS got an alternative, or at least not one that really does an exact job of emulating alcohol. I'm quite sure my new compounds aren't patented nor will he nor James Cook find them.... because I kind of didn't tell them the WHOLE truth. There is a trick in which one can form a dimer of a benzodiazepine. It's just as active per mole, but of course each mole weighs over twice as much. Cook has made a number of these dimers.... BUT he has missed out on what is, well, an obvious trick BUT not one seen in any of his papers.
It would mean that 1 compound could bind to both sites so rather than having to get a licence for 2 drugs, you only need to get a licence for 1 which halves the cost at a stroke.
But isn't that the way? Cook and his team like to show their genius - how complex and difficult that THEY can make things (i.e. others cannot) but it's one of the very simple things.
But I'm not convinced Nutt HAS got an alternative, or at least not one that really does an exact job of emulating alcohol. I'm quite sure my new compounds aren't patented nor will he nor James Cook find them.... because I kind of didn't tell them the WHOLE truth. There is a trick in which one can form a dimer of a benzodiazepine. It's just as active per mole, but of course each mole weighs over twice as much. Cook has made a number of these dimers.... BUT he has missed out on what is, well, an obvious trick BUT not one seen in any of his papers.
It would mean that 1 compound could bind to both sites so rather than having to get a licence for 2 drugs, you only need to get a licence for 1 which halves the cost at a stroke.
But isn't that the way? Cook and his team like to show their genius - how complex and difficult that THEY can make things (i.e. others cannot) but it's one of the very simple things.
Thanks. Guess we have to wait and see what happens this decade.
One thing is for sure is alcohol consumption is falling with the young. The drinks companies will be interested in anything that works. Every brand is bringing out its own non alcoholic one.
Fertile
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Well, it turns out that the subjective effects of alcohol are due to the relative PAM of different GABA subtypes (there are 24 of them) and then separating the positive from the negative.... so just general GABAgenic won't cut it.
I REALLY wish someone would produce a paper that details how methaqualone works. I know it's a partial agonist at some sites, a full agonist at some others AND most importantly - a SUPERAGONIST at some (i.e. it causes more modulation than GABA itself).
www.ncbi.nlm.nih.gov
pubmed.ncbi.nlm.nih.gov
www.guidetopharmacology.org
But none of them give the EC50 at each site. Evidently for pyeyzolam, you need quite a lot to reach the ED50.
I REALLY wish someone would produce a paper that details how methaqualone works. I know it's a partial agonist at some sites, a full agonist at some others AND most importantly - a SUPERAGONIST at some (i.e. it causes more modulation than GABA itself).
A Multifaceted GABAA Receptor Modulator: Functional Properties and Mechanism of Action of the Sedative-Hypnotic and Recreational Drug Methaqualone (Quaalude)
In the present study, we have elucidated the functional characteristics and mechanism of action of methaqualone (2-methyl-3-o-tolyl-4(3H)-quinazolinone, Quaalude), an infamous sedative-hypnotic and recreational drug from the 1960s–1970s. Methaqualone ...
www.ncbi.nlm.nih.gov
A Multifaceted GABAA Receptor Modulator: Functional Properties and Mechanism of Action of the Sedative-Hypnotic and Recreational Drug Methaqualone (Quaalude) - PubMed
In the present study, we have elucidated the functional characteristics and mechanism of action of methaqualone (2-methyl-3-o-tolyl-4(3H)-quinazolinone, Quaalude), an infamous sedative-hypnotic and recreational drug from the 1960s-1970s. Methaqualone was demonstrated to be a positive allosteric...
pubmed.ncbi.nlm.nih.gov
GABA<sub>A</sub> receptors | Ion channels | IUPHAR/BPS Guide to PHARMACOLOGY
GABA<sub>A</sub> receptors in the IUPHAR/BPS Guide to PHARMACOLOGY.
But none of them give the EC50 at each site. Evidently for pyeyzolam, you need quite a lot to reach the ED50.