I'm one of those young people thankfully I stopped but for the price it is now its probably the cheapest most reliable opiates available in Australia which could be a big problem especially now ice is so fround upon.
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AADD Moderators: Tronica
Heroin Is heroin dying out?? Losing popularity?
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NoiseNinja
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I know a lot of young people are adicted to synthetic opioids here in Denmark.
Not herorin as such, but non the less closely related.
It has become a problem, because it is so easy to get hands on.
Like kiosks will sell them illegally, to underaged people too.
And if you know anyone on Metadone treatment it is easy and realtively cheap to get Metadone too.
Not herorin as such, but non the less closely related.
It has become a problem, because it is so easy to get hands on.
Like kiosks will sell them illegally, to underaged people too.
And if you know anyone on Metadone treatment it is easy and realtively cheap to get Metadone too.
4DQSAR
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I am aware that things such as furanylfentanyl, butyrfentanyl and various other modifications to the key amide moiety have all been sold AS fentanyl from time to time. Many were a lot less potent than the parent but I suspect that the synthesis has been telescoped so much that it's still more attractive to produce some sort of fentanyl derivative than to start from scratch with a new scaffold.
I suggest it may not be the sheer potency but the fact that the N-phenylethyl moiety in the fentanyl scaffold that binds to an extra molecular target plays a part in it being something of a 'one way street' i.e. methadone or even heroin won't bind to that extra target.
I won't bore you with the technical details but there was a medication used in some nations that DOES bind to that extra target. It stopped being used for what I suspect were political reasons. The official reason was that a child died after consuming one dose unit BUT if that WAS the real reason, how come it took 21 years for it's use to be abandoned?
There is also the 1c derivative of R-4066 that binds to that extra target, is orally active and some x108 morphine in potency all while acting for twice as long as methadone.
It isn't like we don't have options - we just choose not to use them.
I'm not privy to the recovery rates among people who use fentanyl but if it's as cheap as people say, it could be that somewhere it was decided that fentanyl IS a one way street so either people cold turkey or die.
I know the above statement seems callous but I can clearly remember the Diconal disaster in the UK. Even Drink and Drug News featured a cover that simply said 'The Limits of Intervention' i.e. with Diconal, it was recognized that people knew it would very likely kill them (so most users avoided it) and as my wife puts it 'some people are born with their self-destruct button taped fimly down' i.e. the very appeal WAS that it would kill you.
I suggest it may not be the sheer potency but the fact that the N-phenylethyl moiety in the fentanyl scaffold that binds to an extra molecular target plays a part in it being something of a 'one way street' i.e. methadone or even heroin won't bind to that extra target.
I won't bore you with the technical details but there was a medication used in some nations that DOES bind to that extra target. It stopped being used for what I suspect were political reasons. The official reason was that a child died after consuming one dose unit BUT if that WAS the real reason, how come it took 21 years for it's use to be abandoned?
There is also the 1c derivative of R-4066 that binds to that extra target, is orally active and some x108 morphine in potency all while acting for twice as long as methadone.
It isn't like we don't have options - we just choose not to use them.
I'm not privy to the recovery rates among people who use fentanyl but if it's as cheap as people say, it could be that somewhere it was decided that fentanyl IS a one way street so either people cold turkey or die.
I know the above statement seems callous but I can clearly remember the Diconal disaster in the UK. Even Drink and Drug News featured a cover that simply said 'The Limits of Intervention' i.e. with Diconal, it was recognized that people knew it would very likely kill them (so most users avoided it) and as my wife puts it 'some people are born with their self-destruct button taped fimly down' i.e. the very appeal WAS that it would kill you.
Hey 4DQSAR, you know a lot about the chemistry and I was wondering if you could help me identify something. I know I can Google it but I would like to have the word of someone on here who I believe to be knowledgeable and honest.
About 13 years ago I tried a bunch of fent analogues and one in particular was some kind of butyrfentanyl which was just sold as "4FBF". It was pretty good, in my opinion. Actual fent and any derivative that I have tried have been ultra strong but not really enjoyable compared to H, Oxy, or just good ol' opium. However, the 4FBF stood out as being enjoyable (in my entirely subjective experience, obviously). It was cut/diluted with lactose and I sniffed it.
I'm just curious if you know about this and have any comments or experience with it. Thanks!
4DQSAR
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@Halif2 - 4-Fluorobutyrfentanyl?
I may be wrong but fentanyl homologues in which the key amide is shorter or longer than the most active (propanamide) have a longer duration of action. I don't know where that fluorine is as it's possible to place it in the para position of either of the benzene rings and it produce an active. I suppose Cayman only offer reference samples of things that HAVE turned up on the street so the one that reached the street had a para fluorine on the A-aromatic, but equally, misdirection is hardly novel and if the law controls the wrong one, that's all to the good for producers.
Oddly, such a substitution was apparently tested by Janssen who one can only conclude saw no clinical advantage. I don't think it confirs significantly different activity.
But I have said elsewhere that I have a hypothesis that opiate 'euphoria' is mediated by the binding-unbinding cycle so if less potent analogues have shorter receptor occupancy times, they may be subjectively better.
But as far as I know, fentanyl only produces a sort of 'plastic euphoria' at quite large doses i.e. although it's analgesic TI is larger than morphine, it's 'euphoric' TI is probably a lot lower than morphine.
But as with all street drugs - users are always playing the 'mystery powder game' i.e. a seller can claim almost ANYTHING because the end-user is in no position to CHECK.
I may be wrong but fentanyl homologues in which the key amide is shorter or longer than the most active (propanamide) have a longer duration of action. I don't know where that fluorine is as it's possible to place it in the para position of either of the benzene rings and it produce an active. I suppose Cayman only offer reference samples of things that HAVE turned up on the street so the one that reached the street had a para fluorine on the A-aromatic, but equally, misdirection is hardly novel and if the law controls the wrong one, that's all to the good for producers.
Oddly, such a substitution was apparently tested by Janssen who one can only conclude saw no clinical advantage. I don't think it confirs significantly different activity.
But I have said elsewhere that I have a hypothesis that opiate 'euphoria' is mediated by the binding-unbinding cycle so if less potent analogues have shorter receptor occupancy times, they may be subjectively better.
But as far as I know, fentanyl only produces a sort of 'plastic euphoria' at quite large doses i.e. although it's analgesic TI is larger than morphine, it's 'euphoric' TI is probably a lot lower than morphine.
But as with all street drugs - users are always playing the 'mystery powder game' i.e. a seller can claim almost ANYTHING because the end-user is in no position to CHECK.
Thank you so much!
I am not going to pretend I understand much of anything when it comes to the chemistry side of things - I just take drugs - but it's so interesting to read about. 4-Fluorobutyrfentanyl was the only subjectively enjoyable version of fent I've come across.
And I think "plastic euphoria" is a great term. Around that time 13 years ago I tried 'regular' fent and thought it kinda sucked. Very stupidly I thought it might get better if I took more. It didn't get better but it did get scary for a bit. I still recall the feeling like someone had placed a sandbag across my chest - the difficulty in breathing was a frightening sensation, and I was afraid of nodding off and not waking up. Not good, not safe, not fun.
4DQSAR
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@Halif2 - well, I'm sure Janssen would only have carried out tests for analgesic activity in animal models and they can be utterly useless when considering activity in man.
More recent studies suggest that the -F confirs different selectivity:
Fentanyl being μ > κ > δ
p-F fentanyl being μ > δ ≥ κ
Important to know that KOR agonists produces dysphoria so maybe it is subjectively different BUT if you play the 'mystery powder game' then who knows? Musrepresentation is hardy rare.
More recent studies suggest that the -F confirs different selectivity:
Fentanyl being μ > κ > δ
p-F fentanyl being μ > δ ≥ κ
Important to know that KOR agonists produces dysphoria so maybe it is subjectively different BUT if you play the 'mystery powder game' then who knows? Musrepresentation is hardy rare.
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puke
Bluelighter
From what I hear all my old dope spots are pretty much all fetty etc, really sad because the dope used to be phenom. The whole area is different like unsafer with the way the kids running the blocks are ruthless psychos now with no general respect for the user dealer relationship. With my old spots I never got treated as if I was just some junkie.
4DQSAR
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I don't have any way of judging the veracity of the story but I clearly recall reading of one town in the USA where fentanyl was being sold in $2 units. Now no context was given so it's unclear if this was someone simply applying Grisham's law so ALL opioid users swiched before the price was racked up and/or it's actually still profitable at that price.
The potency values are almost always in terms of analgesic activity but at scale but I note that as an API fentanyl citrate can cost as little as $300/g and one assumes that there is a profit margin even at that price.
I DO recall reading that some of the fake Oxycontin's contained 15mg which seems to me a totally insane amount (it certainly killed a few unwary people who went to a Mexican pharmacy).
Even now I note that seizures have shown anything from 0.1% purity to 64% purity in the same geographical location. That really is very scary.
Just checking, was the kappa receptor the off target one you mentioned earlier in this thread? I'm very curious about that upon having just learned there are actually 5 cannabinoid receptors whereas I always thought there were 2.
4DQSAR
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Yes. It's a matter of degree which is why only suggested that para F MAY alter subjective action.
In the 1990s an Austrian researcher tested a number of dualists that have both MOR and DOR acivity but nothing came of it. Selective DOR agonists are proconvulstant so possibly that was the issue.
But in fact it's cychlorphine that is the worst offender in recent history. There is DECADES of research showing that every time an simpe NH or N-CH3 was replaced with an N-CH2-CH2-CN, the result was a compound with far more analgesic activity in animal models... but in every case researchers went on to say 'but it doesn't substitute for morphine'. It does repeatedly amaze me that people think analgesic activity in a rodent is a reasonable guide to activity in man. It's because that N-2-cyanoethyl produces a lot of KOR affinity - making the result DYSPHORIC.
In the 1990s an Austrian researcher tested a number of dualists that have both MOR and DOR acivity but nothing came of it. Selective DOR agonists are proconvulstant so possibly that was the issue.
But in fact it's cychlorphine that is the worst offender in recent history. There is DECADES of research showing that every time an simpe NH or N-CH3 was replaced with an N-CH2-CH2-CN, the result was a compound with far more analgesic activity in animal models... but in every case researchers went on to say 'but it doesn't substitute for morphine'. It does repeatedly amaze me that people think analgesic activity in a rodent is a reasonable guide to activity in man. It's because that N-2-cyanoethyl produces a lot of KOR affinity - making the result DYSPHORIC.