Stimulants of the Future

[Reminisant B]

These look an interesting set of compounds!

Neurochemical and behavioural profile of Lu 17-133, (±)-trans-4-[3-(3,4-dichlorophenyl)-indan-1-yl]-1-piperazineethanol, an inhibitor or the uptake of dopamine and noradrenaline

http://cat.inist.fr/?aModele=afficheN&cpsidt=7292386

 

[Reminisant B]

Dude, the references are from '85 and are for setraline's twin brother indatraline.

The 3-phenyl-2-indanamide may or maynot be a good idea. Such novelties require literature based verification to prove their validity.

Right just realised its indatraline (I am still learning sorry )

Still what do you think about the piperazine analogue above, seen it before?

 

[Smyth]

Never seen it before. It looks OK I guess but technically WAY beyond the reach of the wishful garage chemist.

 

[Refluxer]

It was over a period of 3 days.
And it was crystal (or thereabouts).
And I don't know what the purity was.

Over 3 days sounds a bit more reasonable.

 

[haribo1]

I still say that this stuff is deserves more attention (the right one). Active at sub-milligram levels, shorter T1/2 that desoxypipradrol. Wonder what esterification would do or making the reversed ester? Esterification would bring down the BP at least and might produce a 'prodrug effect'...

 

[vecktor]

Right just realised its indatraline (I am still learning sorry )

Still what do you think about the piperazine analogue above, seen it before?

this looks a lot like the gbr12909/ vanoxerine pharmacophore minus the fluorophenylmethoxy ether with the indanyl moety locking the alkyl chain rigidly in a certain configuration.

GBR type reuptake inhibitors are a waste of time from a stimulant point of view, as they almost always inhibit dopamine release. they also appear to bind at a different location on the DAT to cocaine.

indatraline is very potent substitutes for cocaine and is extremely >20hr long lasting, but given its slow onset is unlikely to be euphoric. there is a related cyclopropane which is also very potent but I cannot remember its name.

I assume everyone interested in this, has read the Singh review chemistry design and structure activity of cocaine antagonists, deals with most of the major DAT SERT inhibitor families chem rev 2000, 100, 925-1024 is online somewhere
v

 

[Smyth]

I have my suspicions that Sch-5472 may be an active metabolite of desoxy-pipradol anyway.

 

[fastandbulbous]

I assume everyone interested in this, has read the Singh review chemistry design and structure activity of cocaine antagonists, deals with most of the major DAT SERT inhibitor families chem rev 2000, 100, 925-1024 is online somewhere

Yeah it has info regarding the pharmicophore with respect to the placing of the aromatic and amine groups and how good a fit different configurations match that with the rigid norborane like structures. The psuedotropane like configuration of amine & aromatic group seem the more potent in inhibiting reuptake as opposed to just sitting in the active site with little overall effect. The GBRs - can't remember, do they have the tropine type configuration of phenyl & amine groups?.

The piperidine analogues of cocaine don't have that ethylene bridge, so aren't rigidly in held a set distance apart due to the modified chair/boat like conformational changes that can occur. I wonder if 4-phenylqunuclidine would be a good reuptake inhibitor? I've read that 2-methyl-3-phenylquinuclidine is reasonably efficient inhibitor of DAT

 

[fastandbulbous]

Over 3 days sounds a bit more reasonable.

Why wasn't it stated in the first place? Unless some indication of repeated dosing is given then a dose like that is taken to be a single dosage unit. A bit off from the harm reduction point of view (even 'an average of 330mg/day' would have helped)

2-BzP is less toxic than METH (no deamination catabolic reactions; ammonia and methylamine are toxic in vivo)

They are, but deamination in vivo leads to urea/substituted ureas and you don't get methylamine from meth (it is first demethylated to amphetamine before deamination). 2-Benzylpiperidine is most likely excreted unmetabolized for the most part. By the time it takes to ring open the piperidine or stick a benzylic OH group on, chances are it would be mostly in the bladder

 

[Dr.Heckyll]

I still say that this stuff is deserves more attention (the right one). Active at sub-milligram levels, shorter T1/2 that desoxypipradrol. Wonder what esterification would do or making the reversed ester? Esterification would bring down the BP at least and might produce a 'prodrug effect'...

Somewhere in the article on SH-7452 they mention that the effects are unreliable:
Compound
14 had minimal cardiac arid respiratory effects at
stimulant doses and was tried ~linically.~I t was a
potent stimulant, but the dose-response effect mas too
marked. At a given dose, due to the variation in the
individual patient response, the level of stimulation
attained frequently was above or below that desired.
Journal of Medicinal Chemistry (1968), 11 792-6

The patent on it is US 3218330.

 

[haribo1]

Somewhere in the article on SH-7452 they mention that the effects are unreliable:
Compound
14 had minimal cardiac arid respiratory effects at
stimulant doses and was tried ~linically.~I t was a
potent stimulant, but the dose-response effect mas too
marked. At a given dose, due to the variation in the
individual patient response, the level of stimulation
attained frequently was above or below that desired.
Journal of Medicinal Chemistry (1968), 11 792-6

The patent on it is US 3218330.

Well thanks for that. I'm wondering if the kinetics are any better when we increase the dose from theraputic to recreational? Could you say what dose range they were testing? I tried desoxypipradrol at 30mg and I'm pretty certain thats well above any theraputic range but it was very good.
Also, like I mentioned, esterification might be an interesting move, as would the reversed ester (like ritalin and co) from a kinetics POV). Desoxy was a real winner barring it's T1/2 so fixing that would be a worthwhile project.

 

[Smyth]

Also, like I mentioned, esterification might be an interesting move, as would the reversed ester (like ritalin and co) from a kinetics POV). Desoxy was a real winner barring it's T1/2 so fixing that would be a worthwhile project.

War, that's creamy! ​

 

[haribo1]

War, that's creamy! ​

Tilt:D

 

[Refluxer]

Why wasn't it stated in the first place? Unless some indication of repeated dosing is given then a dose like that is taken to be a single dosage unit. A bit off from the harm reduction point of view (even 'an average of 330mg/day' would have helped)

Of course it's fishy, and outrageous from a harm reduction POV. BTW On a swedish forum, a guy took one gram of what was sold as R-2-benzhydrolpyrrolidine, but obviously mixed with something else. Then some MDPV to top it. And he didn't make a sound for several days - people grew a bit worried. Anyway, he recently posted again and said he was still slightly on, and IV benzos had not helped very much. Clearly, that forum is not too much of a harm reduction forum. I wonder what the crap was mixed with (and how much) - obviously it had a "taste" of menthol in the nose if you snorted it. Would you get very wired on 50-100 mgs of the supposed compound?

EDIT: The benzos helped, but because of the long duration, as soon as their effect subsided the stimulant effect shot right up again, and many redoses had to be administered. Apparantly, the experience included a 5-day visit to the hospital.

 

[bydefinition]

I don't usually do a gram of crystal at once.

As far as Harm Reduction, this board is imo primarily a source of Harm Reduction Information. How you choose to use that information is 100% up to you and is also imo your prerogative.

Just as some ppl may attend church or uni and apply nothing of it to their lives, other blers may od (eg PhreeX) and or die (quicksilver). How other ppl do their drugs is of less concern to you than it is to them; in fact, it is none of your business in most cases.

Amphetamines and methamphetamines are from an LD50 standpoint, quite a bit safer than opiates and many other classes of drugs. If someone wants to kill himself or herself (ie Kurt Cobain), you cannot stop them.

Others do not even care.

But and to answer your question, I would if I had any 2-BzP (I accept donations btw) take between 100 and 250mg right now but YMWV usually.

 

[Refluxer]

Ymwv?

 

[slopoke]

Think he means- Your Mileage May Vary!

^ as to the muppet from another forum, i'm sure he bought from 'the leather' one and as such he deserves what he gets!!!

 

[fastandbulbous]

As far as Harm Reduction, this board is imo primarily a source of Harm Reduction Information. How you choose to use that information is 100% up to you and is also imo your prerogative.

Just as some ppl may attend church or uni and apply nothing of it to their lives, other blers may od (eg PhreeX) and or die (quicksilver). How other ppl do their drugs is of less concern to you than it is to them; in fact, it is none of your business in most cases.

Well it is if you want to follow the harm reduction ethos. If they're using a dangerous route of administration, you hasve to know about it in order to advise them of how dangerous that route is (eg people smoking MDPV with a 2 % pyrrolidine impurity)

I don't usually do a gram of crystal at once.

This isn't crystal, it's 2-benzylpiperidine which will have differences in dose, pharmacology, toxicology etc. Might be that it requires 250mg to get the best from it; then again 2.5mg might do the trick. Your post gave the impression that the gram was all consumed at the same time - anybody using that as a dosage guide could be in danger.

 

[Morninggloryseed]

Also, I would prefer it if you guys would refer to me as "chemically gifted" or "chemically psychic" or just plain "knowledgeable" rather than "schizophrenic" which I am most certainly not. Thanks.

PLUR.

Pretending that you have synthed and tried something, and wording it just so, makes you a dishonest charade of a 'person', if not an outright liar. It certainly DOES NOT make you gifted or knowledgable, but perhaps creative.

 

[fastandbulbous]

Pretending that you have synthed and tried something

If this is the case, it goes so completely against the harm reductionethos of BL that I'll be seeing the admin staff. At least Helios says that it's a 'psychic assay', thus indicating that it's not hard fact, but his opinion

3-ethylmethamphetamine.
3-propylmethamphetamine.
3-isopropylmethamphetamine.
3-(n)-pentylmethamphetamine.
4-propylmethamphetamine.
4-(n)-pentylmethamphetamine.

Do Your Homework!!!

I have spent an hour searching for any of these compounds without success. Comments like the 'do your homework' indicate that you have a reference for them, if so please cite it as in light of MGS's statement, I want to see a ref for the above as making guesses and touting them as actual hard fact will not be tolerated.

Doing such things is dangerous should anybody treat them as fact and if it's made up/guesses without saying so it's also somewhat sad as well