2-FA, 3-FA, 4-FA toxicity

[TORTILLA]

As I sit here on 200mg of 4fa I run across this exciting piece of news. Is this guy just talking out his ass and is this just all speculation. I didn't enjoy the part where he says

"4-CA is used as a neurotoxin by neurobiologists to selectively kill serotonergic neurons for research purposes" and that 4fa was only a slight tweak of 4-ca

Hello everyone,

Look I'm posting here as an pharmacologist and bioinformatics researcher to WARN you guys that you are putting yourselves at risk by consuming halogenated amphetamines, which are increasingly sold as Research Chemicals (RCs). The main substances in question I refer to are known as 2-FA, 3-FA, and 4-FA -- in particular, I am warning about 4-FA.

Some of you know there is a risk of neurotoxicity with compounds such as 4-FA, and choose do consume these substances anyway with informed consent. That's fine. As long as you know there is a risk of brain damage (with the risk level unknown), and you accept that risk , then go ahead.

I am writing to those young people, without the wisdom of age or a background in pharmacology or chemistry, are are just starting in research chemicals (RCs) who do not understand or are unaware that the risk profile of halogenated amphetamines (2-FA, 3-FA, 4-FA, etc) is MUCH DIFFERENT than older research chemicals with a relatively safe track record (2C-I , etc).

MDMA and 2C-I etc are relatively safe when used in moderation, and CANNOT be compared to compounds such as 4-FA. Yes, MDMA has a risk of neurotoxicity, but when used in moderation (a few times a year) that risk is relatively low. 4-FA has a MUCH MUCH higher risk.

Here is why you are at risk if you consume halogenated amphetamines.[indent]1) Amphetamine is ALREADY neurotoxic due to the formation of reactive oxygen species (ROS) in the brain [1]. The neurotoxicity is dose-dependent and duration dependent. If you are on a low-dose Adderall prescription for a couple of years, this is certainly safer than someone who is consuming 1g of methamphetamine a day for a couple of years, but in both cases there is a risk.

[1] Prostaglandin H synthase-catalyzed bioactivation of amphetamines to free radical intermediates that cause CNS regional DNA oxidation and nerve terminal degeneration
http://www.fasebj.org/content/20/6/638.short


Racemic Amphetamine (low-to-moderate neurotoxicity)


Racemic Methamphetamine (moderate-to-high neurotoxicity)

So listen: Read the link above [1]. Just by consuming amphetamines (especially methamphetamine), you are putting your brain at risk due to the formation of ROS via Prostaglandin H. The impact of amphetamine neurotoxicity be reduced by pre-treating yourself with approximately 500mg of aspirin for every 5mg-10mg of amphetamine, up to a maximum of approx. 4g of aspirin per day. Read the study I linked for more info.

The risk with regular amphetamine is there, it exists in rats, but there are additional significant risks with compounds like 2-FA, 3-FA , and 4-FA...

On to the really toxic stuff, the HALOGENATED AMPHETAMINES. ...

2) Halogenated amphetamines (the Research Chemicals) such as 2-FA, 3-FA, and 4-FA inherit risk profile of dextroamphetamine and methamphetamine above(with low to high neurotoxicity risk) well as inherit toxicity profile of a really dangerous and neurotoxic related compound known as para-chloroamphetamine.

Para-chloroamphetamine is used to selectively KILL (yes, kill) serotonin neurons in the brain in labs around the world. It is MUCH more toxic than MDMA or Amphetamine. Let's take a look at what this awful amphetamine analog looks like (4-CA).


Para-chloroamphetamine (4-CA): Highly toxic to serotonin neurons.

Hmmm... that 4-CA alot like a substance sold by unscrupulous research chemical vendors, out to make a buck on your suffering -- even if they cause you brain damage. Compare the above structure of Para-chloroamphetamine (4-CA) to your beloved 4-FA.


4-FA: Almost the exact same thing as the highly serotonin-toxic para-chloroamphetamine pictured above. Oh shi0.

Oh, you don't believe me that para-chloroamphetamine is toxic?

Let me quote:

Quote:
Originally Posted by Wikipedia
[Para-chloroamphetamine, aka. 4-CA] is used as a neurotoxin by neurobiologists to selectively kill serotonergic neurons for research purposes, in the same way that 6-hydroxydopamine is used to kill dopaminergic neurons.[2][3][4][5]
The ONLY different between the research chemical 4-FA and the highly- neurotoxic Para-chloroamphetamine (4-CA) is the substitution of a single atom -- a fluorine atom for a chlorine atom.

The Research Chemical 4-FA has a fluorine in a para position on the phenyl group which is VERY CLOSELY RELATED to the highly neurotoxic 4-CA (para-chloroamphetamine), which has a chlorine in a para position on the phenyl group.

These compounds are SO SUBSTANTIALLY SIMILAR that they are considered 'obvious' functional analogs according to U.S. patent law. If you were to patent para-chloroamphetamine for its neurotoxic properties, it is highly likely the U.S. patent office would consider your beloved 4-FA to also have neurotoxic properties (it is 'obvious' to an expert in the field), and would be considered non-patentable.

Given that the ONLY difference between 4-FA and 4-CA (para-chloroamphetamine) is the type of halogen atom, it is highly likely that 4-FA retains some of the neurotoxic properties of 4-CA. The nature and scope of the neurotoxicity is up for debate, but the risk is certainly there. And in my opinion the risk is very high. The physical properties of the halogens are just TOO similar (electronegativity, radius, orbital configuration, etc).

In the same way that anyone who has taken 2C-B will say it is VERY SIMILAR to 2C-I (2c-B / 2c-I causes the same body feelings, the same psychedelic effects, etc and the only difference is ONE HALOGEN ATOM and they only really differ in the biological half-life), anyone taking 4-FA is running the risk of the same neurotoxicity present in 4-CA (difference also = ONE HALOGEN ATOM).

Let's take a look at the properties of the HALOGEN SUBSTITUENTS ... they are VERY SIMILAR. If you are taking 4-FA, you might as well be taking para-chloroamphetamine (4-CA).



Electronegativity of fluorine and chlorine are VERY SIMILAR.



Fluorine and Chlorine have the SAME VALENCE ELECTRON CONFIGURATION (as they are in the same column in the periodic table.)



Fluorine and Chlorine have VERY SIMILAR ATOMIC RADII
(look at F- at 136 and Cl- at 181).

Look at the above properties. 4-FA and 4-CA (para-chloroamphetamine) are so closely related that they might as well be the same chemical. This is like the difference between the OTC antihistamine Chlorpheniramine vs the OTC antihistimine Brompheniramine. They only differ in biological half-life.

There is a small chance (less than 10%) that 4-FA is safe. But the weight of the evidence points to erring on the side of caution -- we need to assume that halogenated amphetamines are neurotoxic (90% probability) -- and that they are much more neurotoxic than regular amphetamines. The evidence is overwhelming.

Given that 4-FA is ALMOST IDENTICAL to the highly neurotoxic 4-CA (para-chloroamphetamine), differing by ONLY ONE ATOM,

Do you really want to take that risk with your brain?

Read more: http://www.drugs-forum.com/forum/sho...#ixzz1ptzQhWbr

http://www.drugs-forum.com/forum/sho...d.php?t=175262
granted its drugforum

[JustinBieberz]

I read this as well. This guy doesn't mention that fluorine is the most electronegative halogen, and therefore has some different properties when it comes to bonding that may cause different effects. Although 4-FA and 4-CA are almost identical, the substitution of the fluorine with the chlorine does make a difference. The neurotoxic effects that this guy mentions happen at higher dosages for all amphetamines, not specifically substituted ones. In your case, 200mg is on the high end of dosages. I'd be careful with extended use.

[iMagiNation]

LOL this guy is ridiculous. what a horrible understanding of chemistry. z0mg its only ONE ATOM DIFFERENCE.

[Plainchems]

I saw this thread long ago and was briefly bothered. However the comparison being made is a slightly ignorant one as not all halogens are created equal and assuming so is making a vastly ignorant generalization about the intricacies of brain/metabolic function and chemistry in general.

Read further on in the thread and you will see plenty of evidence to the contrary of the OP's sensationalist conjecture:

p-chloroamphetamine produced a reversible short-term and an irreversible long-term depletion of rat brain serotonin (5-hydroxytryptamine, 5-HT) and 5-hydroxy- indoleacetic acid (5-HIAA) (Fuller et al., 1975b,c; Harvey et al., 1975). Fuller et al. (1975a) presented comparative studies of three different haloamphetamines having chlorine, bromine, or fluorine in the para-position
of the aromatic ring. They reported however, that p-fluoroamphetamine showed an interesting difference from the other two. It lowered 5-HT levels initially to a lesser degree than did p-bromo-or p-chloroamphetamine
but the effect was transient, contrasting with the long term deficit caused by the other two halogenated amphetamine derivatives.

This finding indicated that p-fluoroamphetamine might share with p-chloroamphetamine the action that is responsible for short-term 5-HT depletion but lack the property of p-chloroamphetamine required for long-term effects. A later study confirmed that p-fluoroamphetamine was
less potent than p-chloroamphetamine in depleting brain 5-HT (Harvey et al., 1977; Fuller, 1978).

Fuller et al. (1975a) also compared the monoamine oxidase (MAO) inhibition by the p-haloamphetamines; p-fluoroamphetamine was distinctly less potent than
p-bromo- or p-chloroamphetamine as an inhibitor of monoamine oxidase. Those workers proposed that the ability of the amphetamines to inhibit monoamine oxidase was related to the lipophilic character of the para-substituent. More recently we have also studied p-chloro- and p-iodoamphetamine, which proved to be relatively selective 5-HT-releasing agents, but the iodo compound had much weaker serotonergic neurotoxic
properties than did p-chloroamphetamine (Johnson et al., 1991a; Nichols et al., 1991).

p-Fluoroamphetamine is also less potent than pchloroamphetamine in stimulating corticosterone release (McElroy et al., 1984). However, the inability of p-chlorophenylalanine (PCPA), 5,7-dihydroxytryptamine
(5,7-DHT), methysergide or fluoxetine to antagonize p-fluoroamphetamine-induced secretion of corticosterone strongly suggested that p-fluoroamphetamine affected hormone release through a nonserotonergic
mechanism (McElroy et al., 1984). The plausibility that p-chloroamphetamine and p-fluoroamphetamine may elevate corticosterone via different
mechanisms is further supported by the demonstration that p-chlorophenethylamine produces the 5-HT behavioral syndrome through a presynaptic action, whereas the p-fluoro derivative produces the same
action by a direct postsynaptic effect (Sloviter et al., 1980). In addition, p-chloroamphetamine and p-fluoroamphetamine appeared to have different modes of action in stimulating pituitary-adrenocortical activity
(McElroy et al., 1984).

Obviously 4-FA is not good for you and in general all amphetamines can be expected to be neurotoxic and have risk of psychosis and other side effects. Making a connection to 4-CA, however, is an ignorant and unecessary technique that muddles up real information about the drug with fearmongering pseudoscience.

[iMagiNation]

^^word.

[H a r o l d]

Expect similar neurotoxicity to dextroamphetamine for 2/3/4-FA. Perhaps a little more for 3-FA due to extensive DA release, and perhaps even a little less due to how hard it is to take the fluorine atom off, not going to metabolize into toxic products. That thread sounds like misinformation that wouldn't fly here on bluelight.

From:

http://www.bluelight.ru/vb/threads/6...-neurotoxicity

^^ Thread in response to the alarmist drugsforum posting.

[Gun Lover]

Yeah, he's talking out of his ass. I once briefly thought it would be neurotoxic like p-CA until I looked into it more.

Don't go crazy with it but this guy's a moron: fluorine =/= chlorine. Fluorine is around the size of a hydrogen atom while chlorine is much larger and fucks with enzymes much more readily.

[Gollum]

Lol, my luck.

I was researching the toxicity of 4-FA, came across this thread (not understanding much of it) but saw the guy got his argument ripped apart. Back out to google and get this thread discussing that very same thread.

So what do you guys suspect are the dangers in using 4-FA then? Is there much to worry about?

[iMagiNation]

Originally Posted by Gollum

Lol, my luck.

I was researching the toxicity of 4-FA, came across this thread (not understanding much of it) but saw the guy got his argument ripped apart. Back out to google and get this thread discussing that very same thread.

fucking google bubbles

[dawg]

All I know is it feels pretty easy on my brain lol. Even the next up all night on the stuff, I don't feel any memory loss or inefficiency at all. I might be a little bit tired, but as far as toxicity goes it's on par with mephedrone imho.

[Gollum]

I was looking for more of a pharmalogical view put in lay mans term.

I do agree that it feels fine on the brain tho. The high itself is very clear headed.

[PsychoDelic]

Easier on the brain than traditional stims??

Doubt it.

[Gollum]

Well have you tried it or can you give me a pharmalogical argument as to why it couldn't be?

It's really clear headed. No motivation, no misconceptions, it's different. I haven't had it in a long time tho but this seems to be the general consensus and I agree with it.