Chemical Forums
Chemistry Forums for Students => Organic Chemistry Forum => Topic started by: shontay on December 10, 2007, 02:15:39 PM
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can someone help me with a way to easily combine GABA with an ester to allow it to pass the bbb efficiently. would the combination of ethyl oleate, GABA, and olive oil heated have any chance to cros the BBB. How exactly can you tell if a compound will pass the BBB?
thanks,
shontay
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acylate it? With an acetic anhydride?
edit: sorry I just read that you need to combine it with an ester. Don't really know much about this I just know that acylating compounds makes them more likely to cross the BBB. And for that matter I couldn't tell you why GABA doesn't cross it in the first place, it doesn't look like it's too big.
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To cross the BBB your substance must be lyphophilic (means: soluble in fats) and acetylating serves this purpose!!! And in fact GABA itself does cross the BBB...
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everything i've read said that GABA on it's own can't cross the BBB?
so what is the process of getting a lyphophilic solution from acetic anhydride and GABA? once this solution is made, can it be combined with something like heptanoic acid to slow the GABA delivery into the blood stream?
sorry for the lack of knowledge, and thanks for the help.
shontay
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I can't understand you shotnay what'll you do by slowing the GABA delivery into the bloodstream??? Acetylating is mostly done by not using any solvent just combining the desired substance w/ acetic anhydride! Or if you really want to you can dissolve the substance in acetic acid!
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hello lutesium,
let me give you some background. i have social phobia. curently i'm perscribed 4mg/day of the benzo clonazapam (GABA influence), and 20mg adderall. it's has been a great solution for me, and for the first time in my life i'm happy and functioning as a normal person. i'm sure you know much better than me that the long term effects of benzos aren't great, so i thought why not look into GABA. GABA injested doesn't pass the bbb, but as you've mentioned it does as a lyphophilic. it seems like it could be a great substitute for the benzos, and if it doesn't cause the drowsiness of the benzos, i may also be able to get off the adderall (also not a great long term solution drug).
by adding an ester and slowing the delivery into the blood stream, you can inject a larger amount of GABA that will give a long constant dilevery. so instead of injecting small quantities of GABA twice a day (don't know the half life, just an example), one larger injection a week can have the same effect. so to answer your question, i'd prefer 1 injection/week to 2/day.
ok, so if GABA is mixed with acetic anhydride are there byproducts that need by washed away? if so, what is used to do this? do you just mix the two and let evaperate? what would be the actual chemical after acetylating it? will this new chemical be completely solible in oil without the use of a solvent, bb for example?
thanks for the help, sorry for the lack of knowledge. i'm trying to learn from researching what you post, and reading simular articales. i'm really not ignorant, i trying to learn. i just don't have the knowledge or background to do this alone.
thanks,
shontay
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hello lutesium,
let me give you some background. i have social phobia. curently i'm perscribed 4mg/day of the benzo clonazapam (GABA influence), and 20mg adderall. it's has been a great solution for me, and for the first time in my life i'm happy and functioning as a normal person. i'm sure you know much better than me that the long term effects of benzos aren't great, so i thought why not look into GABA. GABA injested doesn't pass the bbb, but as you've mentioned it does as a lyphophilic. it seems like it could be a great substitute for the benzos, and if it doesn't cause the drowsiness of the benzos, i may also be able to get off the adderall (also not a great long term solution drug).
by adding an ester and slowing the delivery into the blood stream, you can inject a larger amount of GABA that will give a long constant dilevery. so instead of injecting small quantities of GABA twice a day (don't know the half life, just an example), one larger injection a week can have the same effect. so to answer your question, i'd prefer 1 injection/week to 2/day.
ok, so if GABA is mixed with acetic anhydride are there byproducts that need by washed away? if so, what is used to do this? do you just mix the two and let evaperate? what would be the actual chemical after acetylating it? will this new chemical be completely solible in oil without the use of a solvent, bb for example?
thanks for the help, sorry for the lack of knowledge. i'm trying to learn from researching what you post, and reading simular articales. i'm really not ignorant, i trying to learn. i just don't have the knowledge or background to do this alone.
thanks,
shontay
No offense but this sounds like a terrible idea
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please explain minimal.
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I do also think the same way as minimal 'cuz injecting something that YOU've produced is not only illegal but also REALLY VERY HAZARDOUS FOR YOUR HEALTH!!! IV injection should be made in fully sterile environment!!!
Lutesium...
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Lutesium,
injections will be IM with an oil transporter for the ester (extended release). the oil solution will contain 2% BA, be boiled, and then filtered with a .22 micron filter. there is a very minute chance for infection, and the first trials for toxicity will be on a non-human animal. i'm sure you are very busy, but could you please read the article in this link (http://www.freepatentsonline.com/5051448.html?highlight=5051448,patent&stemming=on) it explains exactly what i'm attempting to do. my problem is it's a bit over my head because there needs to be chemical changes to the examples they provide to get what i want (a lyphophilic solution combined with heptanoic acid, or other slow releasing esters used in an oil transporter). can you help me?
thanks,
shontay
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shotnay I've looked over your document but I don't want to infect you and I don't think that it would be a solution for your problems cuz you use a really heavy medication scheme. Clonazepame and Aderall are so much heavy to be resolved by acetyl ester of GABA.
Lutesium...
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GABA doesn't cross membranes per se, although it can be actively transported by a variety of carriers, or leak through epithelial junctions or through certain osmoregulatory anion channels so why don't you just take it ORALLY??? But not as a replacement for your medicines. Just as an additional supplement!!!
But ask your doctor first. Maybe it can interact with your medicines or do a research on the net. If it didn't have any CNS effeects why would they sell it??? For the PNS??? I don't think so!
Lutesium...
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hello lutesium,
yes benzos and amphetimines are heavy meds (a good reason to get off of them). Gaba has the ability to illiminate the need of both these. GABA is the the effected neurotransmitter in benzo use. the side effects of using benzos is fatigue, lack of focus, short term memory loss, etc. so basically i'm taking an amphetimine to combate the side effects of the benzo.
now to directly influence the GABAa-c receptors (selectively), could have the ability to use a simple amino acid to cure what i'm now taking scheduled narcotics for. The IM injection are great because i'm allready taking them, and with the enanthate or cypionate esters, only 1 shot a week is necessary.
are you familuar with HRT. Many men my age are perscribed testosterone enanthate to elevate their testosterone level to normal. this HRT theripy is a once a week IM injection in a solution of oil.
i'm not going way out on a branch here. you've read the artical, i'm sure you can see the benifits. i'm just asking for help in the chemical bonding that would seem very easy to someone in your field of study.
thanks,
shontay
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No shotnay I don't think so! 'Cuz a replacement (substitute) for a medicine is another one which has the not excatly but pretty same effects + side effects! Take a molecule (for ex. Phenobarbitone -Phenyl-Ethyl Barbituric Acid) this molecule is used for severe seizures is there a replacement for this molecule - yes the Clonazepame that you're using but if the patient is in a really severe seizure Phenobarbitone must be used! SIDE EFFECT AND ADDICTION PROFILE: Phenobarbitone >>>much more greater>>> Clonazepame. But it has got its uses at somewheres! While Secobarbital is rarely used as a sedative due to its very high addiction potential. And I see this addiction potential in you that's why I dont want to help you. Or I'm a very knowledgeable person in GABA and its derivatives (like GABA neurontine...)!!!
Think about Morphine Codeine or Carfentanyl While Carfentanyl is used to sedate big size mammals Morphine is used to relieve severe pain while Codeine is used for mild - moderate pain! And the toxicity and side effects increase as the drug gets stronger!!!
But there might be some points that you might be right (a medicine can be subsituted by another) like very old Urethanes (Urea derivatives) which were used as analgesics and/or sedatives!!! Now take an Urethane and Clonazepame which is newer??? Of course Clonazepame! But if you want to replace Clonazepame or Aderall (was he d-Amphetamine???) you have to find a newer molecule that has the same receptor function but with fewer side effects!
Things Are Said...
Lutesium...
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i understand what you're saying. my hope isn't to substatute anything with GABA. why use GABA if you're using other narcotics that are GABA agonist to transport it. I know reading the artical they mention such bonds to make GABA pass the BBB. don't they also mention ways to get GABA to pass the BBB without the use of narcotics or what combined with GABA would be a narcotic? chemicals that would have little or no effect on the brain other than the GABA amino acid itself. better yet, what about the posibility to bond GABA with chemicals that selectively effect the GABA receptors (GABA antagonist).
from your post, it would seem you think i'm asking you to develope some sort of narcotic. this isn't the case. my understanding is GABA can be bonded with many chemicals to make it pass the BBB.
you've posted that as long as GABA is lyphophilic, it will pass the bbb. wouldn't mixing GABA with guaiacol in an oil and heating it make GABA lyphophilic? how about just mixing GABA with a organic solvent like ethyl oleate in oil and heating, wouldn't that make it lyphophilic?
lutesium, all i'm looking for is a way to get the otc amino acid GABA to safely pass the bbb. i like the idea of using oil and an long acting ester so that the chemical can be administered weekly, and has a nice steady delivery to the brain (no yoyo efect).
i'm not sure about the addition potential you see in me. i'm trying to use an over the counter amino acid to get off two narcotics. wouldn't an addict want more, or stronger drugs than they allready are on, and not the othere way arround. maybe it's just that i don't understand what i'm asking in getting GABA to cross the bbb?
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GABA has some derivatives which are stronger and more habit forming than the medicines you use (if you use them as medicines - not inject or do some sort of other tricks with them-) Anyways these derivatives are so powerful that even if you inject your medicines I think these derivatives are more powerful!!!
Lutesium...
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what would GABA, pyridine, and Heptanoyl chloride produce?
thanks,
shontay
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come on you young smart people, through me a bone here.
thanks,
shontay
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wohoo, my post is unlocked. So can someone please help me with the result of GABA, pyridine, and heptanoyl chloride, or guide me in the direction of adding the enanthate ester to GABA.
thanks,
shontay
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I don't think that Heptanoyl Chloride will make it able to cross the BBB because its a so big ester that won't be able to cross the BBB... Why don't you search over internet? Because drug synthesis posts aren't allowed in here! Show some respect plase!!!
Lutesium...
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hey lutesium,
you're probably right, but the enanthate ester will seperate from the GABA once in the blood stream. this ester is just to prolong the half life of the GABA. an enanthate ester in an oil solution won't start freeing the GABA into the blood stream for 3-4 weeks, and at a nice steady pace once it starts. it's like an extended release formula. getting the GABA past the BBB is still another issue.
why do you say i have no respect? there are many other chemical synthesis post on this forum. i did read the rules, and i don't see where i've broken the rules. mitch unlocked the post, so if rules were being broken, i don't think he would have unlocked it.
i have done research on this topic, i just don't have the chemistry knowledge to understand. isn't that the purpose of this site?
shontay
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I really don't think so... You're contradicting with yourself!!! If the GABA will seperate from its ester once its in the bloodstream how will it cross the BBB???
Lutesium...
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lutesium glad i didn't upset you.
i have two seperate issues with GABA. #1 is it won't pass the BBB on it's own. #2 it has a half life of a few hours. by adding the enanthate ester i solve the half life issue, and the need to administer every few hours (with enanthate ester it would only need be administered once a week).
the BBB is another issue and more complex. with my limited knowledge of chemistry, i thought by asking the outcome of the GABA, pyridine, and heptanoyl chloride combination would be a relatively easy question to answer for a chemist, or someone studying organic chemistry.
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maybe there is an easier way for me. do they make a software program that does organic synthesis, and could also be used as a teaching aid?
i'm old but still capable of learning.
shontay
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Pyrdine will absorb the HCl formed thus drives the reaction to the right! That's all I can do for you because if I do more that will pass the limits!!!
Lutesium...
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I wouldn't do this, I really wouldn't, I can see it producing GABA downregulation, and coming off it won't be fun at all.
Practically speaking, if this was dissolved and given as a depot injection, I can see it being immediately attacked by one or other of the bodys esterases, and being turned straight back into GABA, rather than whatever fatty acid ester you produced.
A med you could look into is tiagabine, it acts as a selective GABA reuptake inhibitor, so, short term it could work for coming off clonazepam.
Benzos tend to produce adrenergic symptoms in WD, so a beta blocker or alpha-2 adrenoreceptor agonist like clonidine might help make it less painful.
I think a better site than here to help you out, would be www.bluelight.ru its not a chemistry orientated site, but I think its more what your looking for in this case :)
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Having injected GABA I can tell you that it is NOT a pleasant experience, the full body rush/burn is an inhibitory experience & there are virtually zero CNS effects - you may wish to reconsider.
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This is a remnant from the old times, I am locking the thread.