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Research provides new understanding of how heroin affects brain (HEROIN =/= MORPHINE)

23536

23536

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New research from the Norwegian Institute of Public Health suggests that our understanding of how heroin affects the brain should be changed. A new report shows that heroin is metabolised to 6-MAM which then crosses the blood-brain barrier to cause the intoxicating effects that arise shortly after heroin administration.

When heroin is injected, it is metabolised to morphine in the brain. Until now, the prevailing perception has been that morphine causes the rush and heroin addiction is thus a form of morphine addiction. Morphine stimulates the µ-opioid receptors in the brain. When these receptors are affected in certain areas of the brain it leads to a sense of euphoria - the "rush" - and further to the development of addiction.

Euphoria caused by 6-MAM

Research at the Department of Drug Abuse Research at the Norwegian Institute of Public Health, has previously questioned the notion that heroin addiction is caused by morphine. A new report by Fernando Boix and colleagues confirms that it is not primarily morphine, but the metabolite 6-monoacetylmorphine (6-MAM), that provides the euphoria and intoxication after heroin intake. It opens up new avenues in the treatment of addiction.

- What happens when heroin is injected?

"Heroin is converted rapidly to 6-MAM in the blood. The concentration becomes high and it quickly crosses the blood-brain barrier. In the brain, 6-MAM binds to µ-opioid receptors and provides the rush. In addition, some 6-MAM is metabolised to morphine. Morphine also binds to µ-opioid receptors, but this only gives a supplementary effect. Essentially it is 6-MAM that produces the effects," said Fernando Boix.

. . .

These new results mean that the international scientific community should review their understanding on how heroin affects the brain. To date, researchers have assumed that heroin is converted to morphine.

full: http://www.news-medical.net/news/20...nderstanding-of-how-heroin-affects-brain.aspx
 
Not only that, but 6-MAM has a much higher potency than 3,6-DAM (heroin) proper, and requires much less drastic acetylation conditions, so it's possible that poor acetylation conditions might give rise to more potent product, such as in the case of black tar..?
Also, isn't this old news? Well, the information anyway, not this particular study.
 
^ I think the study is more of a minor clarification than a new breakthrough in understaning. many authoritative sources use the claim that heroin is simply a morphine prodrug.
 
stirfry said:
^ I think the study is more of a minor clarification than a new breakthrough in understaning. many authoritative sources use the claim that heroin is simply a morphine prodrug.
Click to expand...
What's new in this study, as far as I know, is that the majority of the heroin gets turned into 6mam, not just a little bit like it was previously believed.
 
^Yeah, and it has been understood for awhile that 6-MAM was responsible for at least a decent percentage of the effects... The metabolization of heroin to metabolites has always been what is responsible for effects... Obviously it wasn't just heroin -> morphine, they act very different. Look at just the histamine release difference.
 
this is the abstract:

NSFW:
Addict Biol. 2011 Apr 11. doi: 10.1111/j.1369-1600.2010.00298.x. [Epub ahead of
print]

Pharmacokinetic modeling of subcutaneous heroin and its metabolites in blood and
brain of mice.

Boix F, Andersen JM, Mørland J.

Norwegian Institute of Public Health, Division of Forensic Toxicology and Drug
Abuse and University of Oslo, The Medical Faculty, Norway.

High blood-brain permeability and effective delivery of morphine to the brain
have been considered as explanations for the high potency of heroin. Results from
Andersen et al. indicate that 6-monoacetylmorphine (6-MAM), and not morphine, is
the active metabolite responsible for the acute effects observed for heroin.
Here, we use pharmacokinetic modeling on data from the aforementioned study to
calculate parameters of the distribution of heroin, 6-MAM and morphine in blood
and brain tissue after subcutaneous heroin administration in mice. The estimated
pharmacokinetic parameters imply that the very low heroin and the high 6-MAM
levels observed both in blood and brain in the original experiment are likely to
be caused by a very high metabolic rate of heroin in blood. The estimated
metabolic rate of heroin in brain was much lower and cannot account for the low
heroin and high 6-MAM levels in the brain, which would primarily reflect the
concentrations of these compounds in blood. The very different metabolic rates
for heroin in blood and brain calculated by the model were confirmed by in vitro
experiments. These results show that heroin's fast metabolism in blood renders
high concentrations of 6-MAM which, due to its relatively good blood-brain
permeability, results in high levels of this metabolite in the brain. Thus, it is
the high blood metabolism rate of heroin and the blood-brain permeability to
6-MAM, and not to heroin, which could account for the highly efficient delivery
of active metabolites to the brain after heroin administration.


PMID: 21481103 [PubMed - as supplied by publisher]


Is the "Boix" in Fernando Boix pronounced like the English word "boy"? It would be stunningly appropriate for a heroin researcher's surname to be BOY.
 
phrozen said:
What's new in this study, as far as I know, is that the majority of the heroin gets turned into 6mam, not just a little bit like it was previously believed.
Click to expand...

no, it's that the velocity of conversion of heroin to 6-MAM is very high--high enough that the majority of opiate reaching the brain is in the form of 6-MAM, not heroin.
 
so i remember reading somewhere that if I prep a shot of US east coast h and leave it for over an hour that it would turn into 6-MAM and therefore would not be as "strong". so does this mean that prepping a shot is ok and may even be better than a freshy?

(pardon me if i am totally wrong about everything i wrote here bc i dont know much about science and have no research to back up anything i am saying and may be spewing complete garbage.)
 
itsok said:
so i remember reading somewhere that if I prep a shot of US east coast h and leave it for over an hour that it would turn into 6-MAM and therefore would not be as "strong". so does this mean that prepping a shot is ok and may even be better than a freshy?
Click to expand...

I've never been patient enough to let a shot sit.

Depending on the pH and temperature of the solution, hydrolysis of either or both ester groups is theoretically possible. This opens the way to 6-MAM, 3-MAM and morphine. I see no reason why there wouldn't be equal amounts of 6-MAM and 3-MAM (if hydrolysis indeed takes place). Since 3-MAM is far less active, the shot would probably be weakened.

^conjecture
 
235360287471352662 said:
no, it's that the velocity of conversion of heroin to 6-MAM is very high--high enough that the majority of opiate reaching the brain is in the form of 6-MAM, not heroin.
Click to expand...
I reread it again. You're right.

But I'm still under the impression that the consensus before this study was that most of its effects were caused by morphine and not 6mam.
 
hmmm and black tars 6-MAM content increases over time as a result of hydrolysis with moisture in the air... Does that mean that you could take tar and 'cure' it like bud by storing it for a long time? eh, guess it wouldn't really matter if your body does all the work for you anyway
 
That study is completely flawed. Everyone knows heroin is a morphine prodrug. Morphine diacetate ("heroin") is converted to morphine and 6MAM (which itself is converted into morphine aswell) is what binds to the opiate receptors and gets you high. 6MAM is a minor metabolite - there is over 70 years of science behind that. This new "research" is flawed and you'll have scientists in the field challenge it left and right.

Heroin is "morphine diacetate". An ester salt of morphine and a morphine prodrug. This has been established and is taught in ALL medical and pharmacy schools across the world in all universities and colleges - from Harvard and Oxford to your local community college and that's not going to change, not now not ever. This "Fernando Boix" is daring to challenge this established FACT - well, he's quickly going to be swatted down like a fly by the leading scientists on issues like this.

Pfft.
 
kokaino, your argument against the study is that it is contrary to common knowledge?
 
235360287471352662 said:
kokaino, your argument against the study is that it is contrary to common knowledge?
Click to expand...

No. Morphine diacetate ("heroin") has been studied for over a century. The book on it being a morphine prodrug is done and closed. It has been studied over and over and over again - all with the same results. This study is flawed somehow because it goes against thousands of studies before it in the most prestigious universities around the world by some of the most renowned scientists in the field of medicine and pharmacology. This one "study" by some random scientist is running smack against a century of research and studies. I don't know about you, but I'm going to go with the century of research over this one study that will be swatted down and ripped apart by other scientists in the field.

Don't take this one study and hold it as solid proof of something that has been already studied to death and always come up with the same result.

Don't tell me you are falling for this "study"?
 
phrozen said:
I reread it again. You're right.

But I'm still under the impression that the consensus before this study was that most of its effects were caused by morphine and not 6mam.
Click to expand...

It is caused by morphine. 6MAM is a very minor metabolite that is also converted to morphine before binding to any opioid receptors.

The two acetyl groups detach from the morphine molecule as soon as it crosses the BBB and morphine binds to the opioid receptors to produce the high. The acetyl groups are responsible for the quicker action and the rush is caused by them detaching from the morphine molecule. 6MAM is produced in the brain and it too is converted into morphine which binds to the opioid receptors.

"Heroin" is an ester salt of morphine and a morphine prodrug - it's name is morphine diacetate.
 
kokaino said:
No. Morphine diacetate ("heroin") has been studied for over a century. The book on it being a morphine prodrug is done and closed. It has been studied over and over and over again - all with the same results. This study is flawed somehow because it goes against thousands of studies before it in the most prestigious universities around the world by some of the most renowned scientists in the field of medicine and pharmacology. This one "study" by some random scientist is running smack against a century of research and studies. I don't know about you, but I'm going to go with the century of research over this one study that will be swatted down and ripped apart by other scientists in the field.
Click to expand...

it is what it is. Rats were given heroin. Then they were anesthetized and their brains were dissected. Plus, the study reproduces the results of an earlier study.

You have a bit of a notion of scientific knowledge being a Rock of Gibraltar type thing. Surely you know that it isn't.
 
Go to this link. Scroll down to the chart titled "Table 1: Classification of prodrugs" and you'll find heroin listed as a prodrug under Intracellular Type IB.

The source is listed as Adapted from Pharmaceuticals (2:77-81, 2009) and Toxicology (236:1-6, 2007).

Yes, so what if my argument against the study is that it is contrary to common knowledge. It's not just "common knowledge". It's a century of research and studies by renowned scientists in the most prestigious universities around the world in the U.S., UK, Germany, France, Canada, Japan, and elsewhere.

One little study is not going to change that. It's flawed and it will be challenged and rebutted by scientists. It's just not right, that's all there is to it.

What we know is still going to be taught in medical schools and pharmacy schools and this little study will not even be looked at or recognized.
 
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