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Pharmacology How drugs affect the workings of the human body.

 
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  #1  
Old 28-09-2012, 19:12
Graye Graye is offline
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5f-AKB48, metabolic activity regarding the 5f

A friend of mine is gearing up to make a new smoking blend containing 2g 5f-AFK48 over 1 lb of various herbs. In discussing the chemistry of the process he raised a question regarding how the body reacts to the 5f chain attached to the terminal carbon. I've seen this particular method of modification before in the UR-144 series and my question is this: How does the addition of the 5f chain to the terminal carbon affect the potential neuro-toxicity of the drug, if at all?
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Old 30-09-2012, 05:57
nigh nigh is offline
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Re: 5f-AKB48, metabolic activity regarding the 5f

Even though there's not much data on this subject with regards to 5f-AKB48 in particular, it stands to reason that 5f-AKB48 would be dealkylated to fluoropentane in a mechanism similar to other fluorinated cannabinoids. Donno with certainty which enzyme in particular dealkylates it, though.

Anyhow, it's not likely that 5f-AKB48 metabolizes into anything neurotoxic, as fluoroalkanes, unlike the other haloalkanes, generally don't function as alkylating agents. As a matter of fact, even if fluoropentane did function as an alkylating agent, it'd likely be much more harmful to cells in places such as bone marrow and the GI tract, not cells in the brain. Since the former cells divide very frequently, they'd likely incur more effects from DNA damage through guanine alkylation than neurons would. That's not to say that fluoropentane wouldn't hypothetically damage neurons as all; just that it'd damage cells elsewhere more significantly.

As to the question of how the body reacts to fluorine substitution in general, I can't say much because it's hard to generalize the effects that a substituent produces across many different drug categories and molecular structures. Substituting halogens can certainly change a drug's pharmacological profile significantly, but it's hard to say how it does so in a random substance.

Last edited by nigh; 30-09-2012 at 07:21.
  #3  
Old 30-09-2012, 06:07
Phenoxide Phenoxide is offline
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Re: 5f-AKB48, metabolic activity regarding the 5f

Quote:
Originally Posted by nigh View Post
Even though there's not much data on this subject with regards to 5f-AKB48 in particular, it stands to reason that 5f-AKB48 would be dealkylated to fluoropentane in a mechanism similar to other fluorinated cannabinoids.
Which N-fluoroalkylated cannabinoids are documented to be metabolized in this way? From what I've seen the major metabolites of these cannabinoids tend to be mono-hydroxylations of the N-alkyl chain. AM-2201 for example is documented to clear predominantly as N-(4-hydroxylated) metabolite in humans. Oxidation of the indole ring is also documented. I'm unaware of any indication that the fluoropentyl chain is cleaved in any of the compounds from this family that have been studied to date.

Quote:
Donno with certainty which enzyme in particular dealkylates it, but if I had to make an educated guess, I'd say cytochrome P450 is probably responsible.
Cytochrome P450 is not a specific enzyme. It's a superfamily of enzymes.

Quote:
Anyhow, it's not likely that 5f-AKB48 metabolizes into anything neurotoxic
Again what are you basing that assertion on? This is a very new chemical with a practically non-existent track record of human use. In fact it's so new that as far as I know it's not even been confirmed to exist by an independent analysis, let alone having a detailed characterization of its metabolic profile. In the absence of evidence we should be careful about assigning arbitrary likelihoods of harm. If it were that straightforward that we could define toxicity just by looking at the structure then pharmaceutical companies wouldn't spend tens of millions of dollars on ADME studies.

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Excellent use of chemical knowledge and human caution
Good critiques, especially the last point. Harm interpretation on a novel compound is purely speculative.
  #4  
Old 30-09-2012, 07:03
nigh nigh is offline
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Re: 5f-AKB48, metabolic activity regarding the 5f

Quote:
Originally Posted by Phenoxide View Post
Which N-fluoroalkylated cannabinoids are documented to be metabolized in this way? From what I've seen the major metabolites of these cannabinoids tend to be mono-hydroxylations of the N-alkyl chain. AM-2201 for example is documented to clear predominantly as N-(4-hydroxylated) metabolite in humans. Oxidation of the indole ring is also documented. I'm unaware of any indication that the fluoropentyl chain is cleaved.
I wasn't responding concerning all of 5f-AKB48's metabolites; rather, I was directing my responses at his questions concerning the fluoropentyl chain. After some preliminary Googling, I saw a lot of information stating that the fluorinated AM-x series members (including AM-2201, at least from what I found) are N-dealkylated during their metabolism, and I was just extrapolating that data to 5f-AKB48 due to the fluorinated AM-x compounds having identical fluoropentyl chains.

Quote:
Originally Posted by Phenoxide View Post
Cytochrome P450 is not a specific enzyme. It's a superfamily of enzymes.
I was going to simply end the sentence with "dealkylates it, though" but changed my mind and absent-mindedly tacked the rest of it on there. So yes, that's incorrectly worded - thanks for pointing it out to me. I was aware of cytochrome P450 not being a single enzyme when the post was made, so the mistake was just an error in communication.

Quote:
Originally Posted by Phenoxide View Post
Again what are you basing that assertion on? This is a very new chemical with a practically non-existent track record of human use. In fact it's so new that as far as I know it's not even been confirmed to exist by an independent analysis, let alone having a detailed characterization of its metabolic profile. In the absence of evidence we should be careful about assigning arbitrary likelihoods of harm. If it were that straightforward that we could define toxicity just by looking at the structure then pharmaceutical companies wouldn't spend tens of millions of dollars on ADME studies.
I definitely have no idea if the substance is actually safe for humans to use, but I doubt that fluoropentane itself is neurotoxic. That's what I was getting at with that portion of my comment and this post as a whole. However, it does seem that fluoropentane possesses a degree of hepatotoxicity, so I'd definitely advise against 5f-AKB48's use if it is actually metabolized into fluoropentane at some point.
  #5  
Old 02-11-2012, 01:41
hookedonhelping hookedonhelping is offline
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Re: 5f-AKB48, metabolic activity regarding the 5f

Quote:
Originally Posted by Graye View Post
A friend of mine is gearing up to make a new smoking blend containing 2g 5f-AFK48 over 1 lb of various herbs.
Im curious what your friend thought of the this AFK48 analog.. 2g over 1lb seems like a cautious consistency, but I have found little info about the potency of this variant.

Im reading most people preferred AFK48 to UR-144.. I wonder if this is analog is the best one available atm..
  #6  
Old 02-11-2012, 01:59
Yet Another Junkie Yet Another Junkie is offline
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Re: 5f-AKB48, metabolic activity regarding the 5f

Quote:
Originally Posted by hookedonhelping View Post
Im curious what your friend thought of the this AFK48 analog.. 2g over 1lb seems like a cautious consistency, but I have found little info about the potency of this variant.

Im reading most people preferred AFK48 to UR-144.. I wonder if this is analog is the best one available atm..
Could you please elaborate on why people prefer afk48 to ur-144? I have seen a few animals become distressed from ur-144.
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Old 02-11-2012, 02:18
hookedonhelping hookedonhelping is offline
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Re: 5f-AKB48, metabolic activity regarding the 5f

Quote:
Originally Posted by Yet Another Junkie View Post
Could you please elaborate on why people prefer afk48 to ur-144
What I have read seems to lack real specific data, but rather generalizations that this is more cannabis like with less anxiety and is more manageable when OD occurs. The standard of what people seem to judge these cannabinoids by.

These readings were all off board, so it would be nice to hear from people who are established members and not furthering a particular agenda to increase the analogs popularity for monetary reasons.
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Old 02-01-2013, 22:57
fourtysevenpercent fourtysevenpercent is offline
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Re: 5f-AKB48, metabolic activity regarding the 5f

Quote:
Originally Posted by hookedonhelping View Post
What I have read seems to lack real specific data, but rather generalizations that this is more cannabis like with less anxiety and is more manageable when OD occurs. The standard of what people seem to judge these cannabinoids by.

These readings were all off board, so it would be nice to hear from people who are established members and not furthering a particular agenda to increase the analogs popularity for monetary reasons.
No dude, that is spot on!

5F on UR-144 made it feel methed/cracked out
5F on AKB48 made it feel... again methed/cracked out, but so much better than 5F-UR-144
I think I like 5F-AKB48 and I judge my cannabinoids on what you said.

So 5F appears to "meth out" its derivative?
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Old 25-06-2013, 13:50
putterball putterball is offline
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Re: 5f-AKB48, metabolic activity regarding the 5f

Thank you. I had a feeling that 5F-AKB48 was too good to be true. I worked in the industrial packaging field for over 30 years, and generally anything that sounded like "fluoro" or "pentane" was generally considered hazardous...
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Old 16-07-2013, 16:32
Jabbawaya Jabbawaya is offline
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Re: 5f-AKB48, metabolic activity regarding the 5f

Again, just because a compound contains a fluorine moiety does not mean that it is harmful (e.g. paroxetine, one of the most widely prescribed antidepressants). However, some compounds containing fluorine are harmful (e.g. perfluoroalkylated compounds). The point is, in this case, we just don't know and have no real way of finding out. Unless, of course, you have a lab and a lot of mice.

This is why we caution people about "research chemicals" with minimal history of human use; it's like starting clinical trials at Phase V without having gone through the previous steps to establish an in vitro and in vivo safety profile. Use at own risk/enjoyment.
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Old 03-07-2015, 06:30
GK212659 GK212659 is offline
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5f-akb48

5F-AKB48 shows little metabolic toxicity when taken without pyrolysis.

When smoked or even vaporized in a glass pipe - where the powder turns dark brown on melting - 5F-AKB48 is transformed into a variety of toxic chemicals.

Similar to a burning Teflon frying pan, 5F-AKB48's Fluorines can recombine with other atoms in a large variety of ways. One of the ways is Perfluorooctanoic Acid. Another one is HF - Hydrofluoric acid.

HF is a certainty with any pyrolized fluorinated molecule. HF is a strong mineral acid that is highly corrosive to tissue.

There's worse than HF. After a couple years of once-a-day, I notice these things.

One of those things is the foul smell produced after smoking. In the pipe and eventually on everything.

Another is that same or very similar smell on sweat for a day or more after.

A toxic odor so pervasive that it soaks my clothes and eventually even the washing machine reeks.

Another is the swollen feet gradually losing nerve sensation.

This drug seems to inhibit Oxygen absorption / respiration.

Then there is the chronic lung infections and cough.

What is worst is that these toxic effects seem to be cumulative like nuclear radiation, or like Fluoroquinolone antibiotic exposure. A series of exposures can produce few or no symptoms but when the body's toxicity threshold is surpassed the symptoms can suddenly and dramatically appear.

Just a single dose, or just a dozen once-each-day many months or even a year after quitting can bring back toxicity symptoms to nearly their maximum during a previous peak regime.

That is a sign that something or a lot of things that are not easily fixable get damaged a bit after each dose of 5F-AKB48. Then when those things reach a critical level of damage or functional loss, the cumulative symptoms start to show.

Here are some theories. Cannabinoids lower mitochondrial energy conversion. Synthetic full agonists are stronger than natural partials. So they ought to lower it more.

What mangled molecules manage to get into the body and the brain when a halogenated drug is pyrolyzed?

Perhaps, twisted molecules that can never be broken from their ligand receptors. Covalent bonds.

Fluorine is this Universe's most electronegative element. It forms carbon bonds that are tighter than anything else. That's why Teflon is so useful. I know how useful Teflon is. I managed to inhale two or maybe three lungfuls of Teflon smoke thanks to a roommate's carelessness. He caused a Teflon fire and I had to deal with it. That fire filled the entire room with pure Teflon smoke - the pot was empty. In ten minutes I had fume fever and since that day three years ago I have not been able to breath properly.

Life never succeeded in making much use of halogens bound organically inside molecules - Iodine excepted. Fluorine and Chlorine are just too strong. They tend to irreversibly bind things. They are too strongly electronegative. Same with heavy metals. Some rare exceptions are Cobalt(III), Chromium and Vanadium.

That's not to say that halogenated drugs are evil. But mangling them, mutilating them before they get inside can turn into lots of problems.

There are safe 'wooden' cannabinoids - the CHMINACAs apart from FUB. They produce high CB2 activation and low CB1 activation; good for sleep and medical purposes. Even used once a day though, they don't produce the psychedelic high CB1 activation. Of course they are not 'receptor-safe' as most potent drugs are not. But they won't damage other body systems due to pyrotox products.

It seems there has been a failure of chemistry to produce high-CB1 activators that lack the 'required' Fluoropentyl chain or paraFluorobenzene. Yet this fluorination is a cumulative, insidious sickening killer.

There is ADAMANTYL-THPINACA which is my hope and is predicted to produce decently high CB1 activation.

We are out of luck if 5F-AKB48's Adamantane group is implicated in any toxicity.

If pyrolysis or inherent metabolic toxicity can't be avoided, it seems the best option is to use hyperpotent Fluoronoids. 5F-AMB. Microdoses can be used to limit damage, or it can be used orally.

For long duration or sleep there are the CHMINACAs and a few other non-halogenated options.

If anyone can post a list of non-halogenated cannabinoids and their respective CB1 / CB2 dominance I would be very pleased. A safe list. Not safe for receptors of course, but the safety of everything else in a body from pyrolysis and metabolic toxicants.

That distinction - between 'toxicity' symptoms that are caused by receptor over- or under-activation - and that caused by disruption of all those other body systems by the drug, its metabolites, and any pyrolytic products consumed due to smoking/vaporizing. Even vaporizing. 5F-AKB48 reacts with itself and/or air at its evaporation temperature. It cannot be cleanly vaporized in air.

So I am also very interested to hear from others about these toxic symptoms - not the receptor effects. Some of the receptor effects are (agonist & withdrawal): sweating, low appetite, vomiting, depression, low Testosterone, low energy, poor memory.

The other toxic effects are very distinct: the 'toxic feeling' body-wide isn't associated with CB receptors.
Neither is the poor Oxygen utilization, nor the swollen painful feet. I'm pretty sure not.
The lung toxicity has nothing to do with CB receptors and everything to do with Fluorine. Hydrofluoric acid and every Fluorinated organic/inorganic molecule a good chemist could imagine.

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