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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.
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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..
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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.
  #7  
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.
  #8  
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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