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N&PD Moderators: Skorpio | thegreenhand
4-methyl-5-thiazoleethanol
- Thread starter wungchow
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kidamnesiac
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something tells me it would just metabolize into ethanol, which does have barbituate like activity...
hussness
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The drug is related to chlormethiazole, which is the same compound but with a Chlorine replacing the alcohol. Keith Moon actually died of a chlormethiazole overdose. Wikipedia said chlormethiazole inhibits alcohol dehydrogenase. Beyond that I don't know too much about it.
fastandbulbous
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They're both based on one (can't remember which) of the B vitamins if you compare structures. \Chlormethiazole is a fairly effective CNS dep[ressant in my experience (got some given), but on the alcohol dehydrogenase inhibitor bit are you sure you're not confusing it with disulfram (antabuse); both are used for alcoholics only chlormethiazole is ised to replace alcohol & prevent DTs whereas disulfram is used to prevent dried out alcoholics from drinking. The antibiotic metranidazole is an alcohol dehydrogenasse inhibitor and I once saw someone who was taking them druink a half glass of shandy. He thought the avoid alcohol warning was the same as other 'avoid alcohol' medications' I witnessed him projectile vomiting 15 mins later and looking like death warmed up!
fastandbulbous said:
Are you sure you don't mean acetaldehyde dehydrogenase inhibitor? Since it is acetaldehyde that causes the negative effects of drinking, where as an alcohol dehydrogenase inhibitor would increase the positive effects of drinking because the ethanol sticks around longer.
hussness
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fastandbulbous said:
I just got that from: http://en.wikipedia.org/wiki/Chlormethiazole. I don't know how valid it is. I would trust your opinion or any random guy who writes a pharmacology stub on wiki though. The molecule is based off Vitamin B1 (thiamine). http://en.wikipedia.org/wiki/Thiamine says that Thiamine decomposes if heat. Does it decompose to 4-methyl-5-thiazoleethanol plus that other fragment, or what?
haribo1
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I've used clomethiazole quite a lot. It's legal everywhere except Australia and you can buy in online for $19 for 20. The effects are very alcohol-like. Even a heavy drinker doesn't feel like a drink after 3-4 of those little grey capsules. The only downsides are retrograde amnesia and histamine release. It's a LOT more fun that barbiturates or benzodiazipines. You can make it from B1 in 2 steps. If you can acquire the intermediate alcohol, then thionyl chloride in DCM gets the job done. The problem is forming a salt. Its ever so fussy. The capsules are the freebase (taste/smell like rotten apples, fun to breathe on people after crunching them). So you can make it, but it doesn't keep unless you put it under nitrogen and keep it cool.
The effects are similar, but not quite the same, as methaqualone. Oh, and it doesn't make you throw up if you do drink, but it's very dangerous to mix the two...
The effects are similar, but not quite the same, as methaqualone. Oh, and it doesn't make you throw up if you do drink, but it's very dangerous to mix the two...
Limpet_Chicken
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Bump to avoid pruning related bullshit.
And to add, that the other fragment left after the typical bisulfite cleavage of the B vitamin (its thiamine, B1) is highly toxic. It has a name, toxopyrimidine, and its a convulsant poison, inhibiting GABA biosynthesis because toxopyrimidine and it throws a spanner in the works of biological processes which use vitamin B6 as a cofactor. Nasty stuff, so if making chlormethiazole or bromethiazole, etc., which isn't difficult, and without going into too much detail, its just two steps, cleavage and halogenation of the intermediate alcohol. The alcohol is much, much less potent than the chlorinated or brominated derivatives. But careful workup is needed to make sure that the intermediate alcohol is pure, and free of toxopyrimidine. At least unless not having enough GABA to go around, convulsant poisons and possible excitotoxicity is your cup of tea.
Thankfully the aqueous solubility of the unwanted, noxious component differs greatly from that of the intermediate alcohol so washing the toxic component out is practical with ice cold water, and especially given the thermolability of chlormethiazole. Also, there is one downside to chlormethiazole I've noticed, namely that if dosed high and for at least a couple of days, there appears to be a metabolic pathway that leads to some sort of horrendous, virulently stygian sulfurous stinker being formed in-vivo and excreted slowly, leaving you a pariah for anything and anyone in possession of a functioning nose and a pair of legs to turn the other way and run like hell once they get within a couple of hundred meters of you if you inflict your leaving the house on anyone.
It comes out in sweat, urine, shit, saliva, ocular fluid even, stinks like hell took a shit in an ruptured afghan sewer, then threw in a molotov cocktail.
Even, and worst of all, it comes out in nasal fluid. Think letting off a weapons-grade stink bomb not in a public toilet, or tram, or air conditioning system, but right up the nose of the victim (you, in other words), as if one snapped the ampoule of a stinkbomb using both nostrils to break the glass, only less appeal.
It is absolutely vile. And bloody potent too. And will follow you around like the hounds of hell for about a week. Happened to me once, after I went on a chlormethiazole bender for several days
Whatever the metabolite is, it got produced, and I had a needed medical appointment to attend that week, and had to hide in the bog rather than use the waiting roooms, so as not to inflict the devilish reek on any more people than necessary at any more intensity than what seeped into the waiting room from behind the closed bog doors and waiting room doors. Ghastly, ghastly stuff, not chlor/bromethiazole, chlormethiazole is without a doubt, my favourite GABAergic sedative-hypnotic. I get no physical dependency from using it at 192mg 3x/daily, have been taking it at that level for years, and its a very rapid acting and for me, very effective seizure prophylaxis med, and rescue drug for the onset of a seizure, it will bring me out of it near enough as fast as the capsules break open, I've had to have someone stick them in my mouth before, after an atonic seizure left me almost totally immobilized, I was just about able to draw attention by knocking something over with what little muscle tone I had at my disposal, and very weakly managed to sign to someone in ASL and they knew what to do. Couldn't move to get to the chlormethiazole or pick up, open a bottle myself, so they had to stick a couple of caps in my mouth, as I could still swallow, swallowing and breathing are about all I CAN do if I get hit by an atonic seizure. Real fucking pain in the arse at best.
So given the alcohol counterpart is at least 10x weaker, IMO, I'd say its weaker than that having tried both. And if the deschloro intermediate is also liable to formation of a noxious sulfurous perdition-fart metabolite, then it stands to reason that 10x (or more) larger dose would be needed and correspondingly a larger quantity of the stinking sulfurous abortion of a metabolite would be formed.
Anyone know anything about activity of either a di- or trifluoroethyl group or a nitroalkyl substitutent analog? since an EWG on the end of the ethyl sidechain appears to be needed for activity in a respectable degree.
And to add, that the other fragment left after the typical bisulfite cleavage of the B vitamin (its thiamine, B1) is highly toxic. It has a name, toxopyrimidine, and its a convulsant poison, inhibiting GABA biosynthesis because toxopyrimidine and it throws a spanner in the works of biological processes which use vitamin B6 as a cofactor. Nasty stuff, so if making chlormethiazole or bromethiazole, etc., which isn't difficult, and without going into too much detail, its just two steps, cleavage and halogenation of the intermediate alcohol. The alcohol is much, much less potent than the chlorinated or brominated derivatives. But careful workup is needed to make sure that the intermediate alcohol is pure, and free of toxopyrimidine. At least unless not having enough GABA to go around, convulsant poisons and possible excitotoxicity is your cup of tea.
Thankfully the aqueous solubility of the unwanted, noxious component differs greatly from that of the intermediate alcohol so washing the toxic component out is practical with ice cold water, and especially given the thermolability of chlormethiazole. Also, there is one downside to chlormethiazole I've noticed, namely that if dosed high and for at least a couple of days, there appears to be a metabolic pathway that leads to some sort of horrendous, virulently stygian sulfurous stinker being formed in-vivo and excreted slowly, leaving you a pariah for anything and anyone in possession of a functioning nose and a pair of legs to turn the other way and run like hell once they get within a couple of hundred meters of you if you inflict your leaving the house on anyone.
It comes out in sweat, urine, shit, saliva, ocular fluid even, stinks like hell took a shit in an ruptured afghan sewer, then threw in a molotov cocktail.
Even, and worst of all, it comes out in nasal fluid. Think letting off a weapons-grade stink bomb not in a public toilet, or tram, or air conditioning system, but right up the nose of the victim (you, in other words), as if one snapped the ampoule of a stinkbomb using both nostrils to break the glass, only less appeal.
It is absolutely vile. And bloody potent too. And will follow you around like the hounds of hell for about a week. Happened to me once, after I went on a chlormethiazole bender for several days
Whatever the metabolite is, it got produced, and I had a needed medical appointment to attend that week, and had to hide in the bog rather than use the waiting roooms, so as not to inflict the devilish reek on any more people than necessary at any more intensity than what seeped into the waiting room from behind the closed bog doors and waiting room doors. Ghastly, ghastly stuff, not chlor/bromethiazole, chlormethiazole is without a doubt, my favourite GABAergic sedative-hypnotic. I get no physical dependency from using it at 192mg 3x/daily, have been taking it at that level for years, and its a very rapid acting and for me, very effective seizure prophylaxis med, and rescue drug for the onset of a seizure, it will bring me out of it near enough as fast as the capsules break open, I've had to have someone stick them in my mouth before, after an atonic seizure left me almost totally immobilized, I was just about able to draw attention by knocking something over with what little muscle tone I had at my disposal, and very weakly managed to sign to someone in ASL and they knew what to do. Couldn't move to get to the chlormethiazole or pick up, open a bottle myself, so they had to stick a couple of caps in my mouth, as I could still swallow, swallowing and breathing are about all I CAN do if I get hit by an atonic seizure. Real fucking pain in the arse at best.
So given the alcohol counterpart is at least 10x weaker, IMO, I'd say its weaker than that having tried both. And if the deschloro intermediate is also liable to formation of a noxious sulfurous perdition-fart metabolite, then it stands to reason that 10x (or more) larger dose would be needed and correspondingly a larger quantity of the stinking sulfurous abortion of a metabolite would be formed.
Anyone know anything about activity of either a di- or trifluoroethyl group or a nitroalkyl substitutent analog? since an EWG on the end of the ethyl sidechain appears to be needed for activity in a respectable degree.