same or different material?

[MurphyClox]

A SAR about 4-MMC??? That one I'd really like to see!

The stuff is hardly researched at all; No SciFinder entries (!), neither using the structure as search entry, nor the terms "4-methylmethcathinone" or "mephedrone". No publications that mention this stuff (I'm not speaking about the british rainbow press) at PubMed or PubChem. Just nothing. No entry in the Merck Index, no CAS-number. Not mentioned in the Rhodium-mirror (@Erowid).

If there is a SAR out there, I can't wait to see it... Interestingly, Erowid lists melting and boiling point. Where did they get it from?

Apart from this, the lack of official info tells me that all statements about the toxicology of this substance are pure speculation.

So? We got a SAR? Where?

Peace! Murphy

 

[IlostaMadge]

I posted one, but deleted as it seems no-one else has come to the glaringly obvious conclusions I have, pm me and I will happily discuss in private.

They are far safer than their non BK counterparts.

That report is false, a main newspaper article posted a report and mislabelled 4-MTA as 4-MMC, it was even discussed on bluelight.

 

[Iodjini_dk]

Well, would you like the original article in Danish then? I live in Denmark myself and followed the case on the news. They never mentioned 4-MTA, however they did indeed relate 4-MMC to the incident.

 

[IlostaMadge]

I'll dig it up on bluelight, it mentioned something along the lines of: -

the young man consumed 4-MTA then overheated and died. 4-MTA commonly known as Mephedrone is a dangerous chemical known for its ability to raise body temperature dangerously high and has been implicated in past fatalities.

From then on all the articles called it mephedrone, as it is a far easier word for the general public than 4-MTA, a major vendor in your country stopped selling at this point.

 

[Furious George]

I posted one, but deleted as it seems no-one else has come to the glaringly obvious conclusions I have, pm me and I will happily discuss in private.

They are far safer than their non BK counterparts.

That report is false, a main newspaper article posted a report and mislabelled 4-MTA as 4-MMC, it was even discussed on bluelight.

Share the knowledge here then you'll only have to do it once. Why did you delete it? Was it somehow sensitive information? Why PM's? Inquiring minds want to know.

 

[Hammilton]

You can't produce a SAR based upon how you feel when you take the drug. It'd be more useless than generalizations based upon poorly reported overdoses.

 

[kaskelot]

Anyhow, withholding your analysis whilst claiming you have one is not a reasonable way to act in a discussion.

If you actually can show why mephedrone is a pretty safe substance, you should do so. There are quite many people, at least in Sweden, who have overused this substance and thus are quite worried about symtoms related to use of this substance, such as depression, bipolarity, so called brain zaps, tremor, paresthesia, akathisia/restlessness.

 

[djsim]

Can you post the original Danish report? I can read/speak Norwegian so it shouldn't be too hard for me to translate the Danish article

 

[fastandbulbous]

The cathinone is not take up into the presynaptic neuron (despite the methyl being a hydroxyl mimicker)

Er, the methyl group inhibits para hydroxylation, but considering one is lipophilic and one is hydrophilic, methyl ain't going to me much of a 'hydroxyl mimicker' otherwise 3,4-dimethylPEA would be very similar to dopamine

Furthermore, the 4 fluorinated and 4 methylated versions of both methcathinone and cathinone will have barely any 5HT2b agonism, as SE, being a mood regulator amongst other things, will have evolved to not accept electronegative groups there

How come fenfluramine (an N-ethylated amphetamine with a ring CF3 substituent) is such a potent 5HT2b agonist that it was withdrawn from clinical use because it caused pulmonary hypertension - I mean CF3 is a pretty damn electronegative ring substituent (it's more of a halogen than any of the 'real' halogens)

 

[Furious George]

Ok. What I received wasn't what I understand to be a SAR. I thought a SAR involved using modeling software (like Sybyl and GOLD), then things like cellular assays, radioligand compettion binding assays and such like.

I'd love for 4MMCat to have a great safety profile, I've got tonnes of it sat in a draw.

Mr F&B, would you have any comments to make as to the likely similarities/dissimilarities of Methcathinone and 4MMCat? Or without a real paper to consult is this all just a fruitless guessing game?

 

[nuke]

Structure activity relationships detail any modulation of quantitative value in respect to a compound's structure, be it dose to anxiolytic activity in rats or its ability to bind to SER233 in a protein, etc

 

[MurphyClox]

...yeah, and as i said before: There is no such (official!) information available for 4-MMC. The stuff isn't published, neither in a SAR-study nor in anything else. It doesn't even possess a CAS-number.

I have to emphasis that all claims of lower/higher/different potency and in particular toxicity (!) for this compounds stems only from subjective experiences from the underground. So please take this into consideration if you tell anyone that 4-MMC beats any of its derivatives in any respect. That was just not proven yet.

Here one can find some useful info about SARs: http://en.wikipedia.org/wiki/Quantitative_structure-activity_relationship

Peace! Murphy

 

[Hammilton]

Question: has 4-MeO-MCat and 4-MeO-Cat been made? I'm wondering if they share the PMA/PMMA issues.

 

[fastandbulbous]

I thought a SAR involved using modeling software (like Sybyl and GOLD), then things like cellular assays, radioligand compettion binding assays and such like.

At it's simplest it's comparing molecular structure & relating it to its effectiveness (eg appetite supression). That's what generally indicates which ones to investigate via radioligand displacement etc for determining the pharmacophore model. It's Structure Activity Relationship and activity isn't always the same as receptor binding (eg 2-bromo LSD; binds to the 5HT2a receptor but isn't a psychedelic)

 

[IlostaMadge]

I will post a full DARI binding SAR on the darker shade, after I post 5HT2a complete amino acid structure for the binding points, I will include 10 trypts, 10 phens and LSD with 3D modelled diagrams to prove my observations.

Fenfluramine doesn't have a electronegative on the beta carbon (the thing that stops NE/E binding) so it can sit in a receptor far far more effectively.

4 MEO Mcat has been made, it can't enter the SE neuron and inhibit MAO due to the beta ketone, and thus carries no risk of SS.

 

[Furious George]

So would you consider the info you received (and posted some corrections to) to constitute a SAR? I'd always thought the activity part had to be quantified somehow, such as with cellular assays, tail-flick tests, and whatnot.

 

[IlostaMadge]

I haven't received anything, they are all my personal observations.

A SAR at it's most perfect relates structure and activity perfectly, it needs no binding assays or firing data, whereas when you have innacuracies you need more and more data to attempt to explain those.

What I sent you was innacurate to some degree, I will be posting on the darker shade from now on.

 

[fastandbulbous]

after I post 5HT2a complete amino acid structure for the binding points

Like this you mean?

Besides weren't we talking about 5HT2b in regard to cardiac problems? Never mentioned 5HT2a receptor

Fenfluramine doesn't have a electronegative on the beta carbon (the thing that stops NE/E binding) so it can sit in a receptor far far more effectively.

Previous quotes:

The cathinone is not take up into the presynaptic neuron (despite the methyl being a hydroxyl mimicker)

Furthermore, the 4 fluorinated and 4 methylated versions of both methcathinone and cathinone will have barely any 5HT2b agonism, as SE, being a mood regulator amongst other things, will have evolved to not accept electronegative groups there

Again you were talking about the methyl group, which is a ring substituent as is the CF3 in fenfluramine and increases it's affinity for the 5HT2b receptor (with subsequent cardiac/pulmonary problems). Also a beta keto group doesn't stop noradrenergic activity; both cathinone & methcathinone are reuptake inhibitors of noradrenaline. It's only when the side chain reaches about 5 carbons that you get almost exclusively dopaminergic activity and 4-methylmethcathinone has a 3 carbon side chain

What I sent you was innacurate to some degree, I will be posting on the darker shade from now on.

Anybody translate?

 

[Hammilton]

A SAR at it's most perfect relates structure and activity perfectly,

This is nonsense. If you don't have any proof of binding affinity, all you have is conjecture based upon nothing.

 

[Furious George]

I haven't received anything, they are all my personal observations.

I was directing that at F&B, I'd guessed that they were personal observations. Interesting ones though.

A SAR at it's most perfect relates structure and activity perfectly, it needs no binding assays or firing data, whereas when you have innacuracies you need more and more data to attempt to explain those.

What about the SAR paradox, can you really draw such conclusions without biological data?

What I sent you was innacurate to some degree, I will be posting on the darker shade from now on.

How does one get to the darker light?