Stimulants of the Future

[kong]

Some of the guys my dad used to work with chewed betal nuts. I tried some and was also not impressed, although the nuts were somewhat stimulating similar to caffiene, but it felt to jittery for me to enjoy it. I can see how people might become addicted however.

 

[fastandbulbous]

Of this series which stereochemical configuration about the alpha-alkyl corresponds to the more active enantiomer? Do they happen to follow the configurational rules for amphetamine (even though they probably don't share a similar mechanism)?

Not a clue as he only produced the racaemic versions, but I have more than a sneaking feeling that the most active isomer has the same absolute configureation as the amphetamines (well ir's true for cathinone/methcathinone so I'd imagine it's that way for the larger alpha alkyl chains)

Arecoline mostly just makes you sweat, you get a little bit wired but its more like nicotine than anything else. Tried both fresh betel nuts and concentrated extract, the extract is stronger but they both taste nasty and don't do that much.

Betel nut is possibly one of the vilest tasting plant materials I've ever decided to chew on and I can't imagine how it became so popular as I can't imagine ever getting to like the taste. Khat is an acquired taste, but once you're used to it the taste almost becomes part of what you look forward to (almost!)

 

[Dr.Heckyll]

How about 4-benzylpiperidine? According to US patent 3632767 it's an antidepressant at low doses and a stimulant at higher doses. Conveniently, it's commercialy available from a number of chemicals supply houses.

 

[fastandbulbous]

^ So is 4-(alpha,alpha-diphenylmethyl)piperidine (or is it pyridine) - it's a reuptake inhibitor. Low doses are probably similar to what amineptine would be like as it's (amineptine) apparently a specific dopamine reuptake inhibitor.

Only thing that preys on my mind is if it's such a versitile drug, why hasn't some firm marketed it as a clinical antidepressant? I know it's most probably because of an abuse potential, but it would be nice to see that confirmed in writing just in case it's something nasty like what happened with alphaethyltryptamine (fatal agranulocytosis)

 

[Dr.Heckyll]

Aletamine derivatives according to J. Med. Chem.; 1972; 15(6); 590-592 could also be considered interesting:

However, all of the compounds, unlike aletamine, showed
CNS stimulation as indicated by hyperreflexia, irritability,
and increase in spontaneous motor activity. In particular,
19 and 21, which were further examined in chloral hydrate
antagonism (Table V), approximated the stimulating effect
of d-amphetamine.

 

[hugo24]

Care to share what the structures of 19 and 21 are?The simple aletamine seems mainly a analgetic.

Clinical Evaluation of Aletamine as an Analgesic
Leo J. Cass M.D.1 and Willem S. Frederik M.D., Ph.D.2
1 University Health Services, Harvard University, Cambridge, Mass., and Visiting Physician, Long Island Hospital, Boston, Mass.
2 University Health Services, Harvard University, Cambridge, Mass.



The analgesic potency of aletamine hydrochloride was investigated in a doubleblind cross-over study with 35 patients. Aletamine hydrochloride was utilized at two dosage levels (250 and 125 mg. three times a day) and was compared with propoxyphene hydrochloride (65 mg. three times a day) and a placebo. Patients were evaluated three times a day, one hour after administration for relief of pain and once each day for changes in mood. Side effects observed or spontaneously expressed by the patients were also recorded.

The results of this study indicate that, given three times daily, aletamine hydrochloride, 250 mg., has a greater analgesic potency than propoxyphene hydrochloride, 65 mg., or aletamine hydrochloride, 125 mg. Aletamine hydrochloride, 125 mg., produces an analgesic effect almost equivalent to that of propoxyphene hydrochloride, 65 mg. Only minor changes in mood were evident for any of the treatments. The incidence of side effects was relatively low for each of the four drug regimens


http://jcp.sagepub.com/cgi/content/abstract/6/2/96

 

[Dr.Heckyll]

Here they are:

 

[Dr.Heckyll]

I'll throw in another one, just to keep the discussion alive: how about dimethocaine? Only slightly less potent than cocaine according to one source: http://www.ncbi.nlm.nih.gov/entrez/...t_uids=7635175&query_hl=1&itool=pubmed_docsum

 

[fastandbulbous]

To bypass the stress of attempting to find it's structure using Google (all dead ends unless you want to cough up god knows how much for the full paper), I eventually found a site that didn't treat it's molecular structure like it was how to turn lead into gold, I've stuck a pic below.

What got me is that it's an ester of para-aminobenzoic acid, and not even a very complicated one at that. If it's all that's being hinted at I'm very surprised that it's not flooding the streets as we speak (or even earlier)

 

[phase_dancer]

Shit, I could have posted it. It's on the CD version of 13th ed Merck index. Wouldn't be hard to synthesize (we did very similar things in second year org chem) so I tend to agree that it's rather surprising it's not heard about on the streets.

 

[hugo24]

And who says this is a good stimulant in humans?

 

[MattPsy]

From PubMed: "Cocaine and dimethocaine produced similar 12-fold increases in dialysate dopamine at concentrations of 0.1 mM and 1 mM respectively."

 

[mad_scientist]

To bypass the stress of attempting to find it's structure using Google.....

Pubchem has structures for pretty much any compound that has a CAS number and a good few that don't.

This site is pretty good for finding structures of obscure compounds, and if you click on the structure it goes to the pubchem page for that molecule:

http://www.chemindustry.com/apps/chemicals

 

[haribo1]

To bypass the stress of attempting to find it's structure using Google (all dead ends unless you want to cough up god knows how much for the full paper), I eventually found a site that didn't treat it's molecular structure like it was how to turn lead into gold, I've stuck a pic below.

What got me is that it's an ester of para-aminobenzoic acid, and not even a very complicated one at that. If it's all that's being hinted at I'm very surprised that it's not flooding the streets as we speak (or even earlier)

That structure is very close to some of the local anathetics. I've heard that shooting those local anasthetics gives a rush but no high. Maybe these modifications give the the rush AND the high. I mean, can you freebase tetracaine?

 

[hussness]

what kind of therapeutic range does dimethocaine have? Given that it substitutes for cocaine at 10x the dose, what kind of "recreational ratio" would it have?

 

[haribo1]

Yeah, I know someone who produced a whole series of alkanone derivatives and his favourite was 1-phenyl-2-methylamino-1-butanone. I think it's that it has a small amount of noradrenergic activity coupled with a lot of dopaminergic activity, which seems to be the right combination for maximum euphoric effects

I wonder about para fluoro aminorex. It's supposed to be the most euphoric of the lot, isn't it (as well as the strongest of the series). Precursors no problem. Should do the 1-pot shot and freebase is smokable...

 

[Vanadium]

here's an idea of MDPV analaog : 1,4-dimethoxy instead of methylenedioxy group

 

[Morninggloryseed]

I am pretty sure tetracaine is a stimulant. I remember a couple of newsprograms about it in the late 80s...some doctors in NYC were giving it as a gel, up the nose on a q-tip, as some form of therapy. The newsreporter (undercover) was shown with q-tips up his nose claiming to feel well-being and other stimulant effects.

 

[haribo1]

I think tetracaine might give a high by itself and this interesting analog posted by F&B makes me think this even more.

This could be the new crack... An easy to make crack alternative that doesn't show up in tests & since it's lower cost, would make importation costs reduce. Price goes through floor, SA dealers screwed. The new 'mom n' pop meth-labs' out of fashion. Start hoarding precursors...

 

[Jamshyd]

here's an idea of MDPV analaog : 1,4-dimethoxy instead of methylenedioxy group

I doubt this will do what you may be expecting it to do, just like the methylenedioxy counterpart didn't do what many people here hoped it would do.

It looks like the bulkines added to the chain renders it useless for amphetamine-like suggestions.

EDIT: RE tetracaine... interesting, I thought I saw it OTC the other day. And indeed, look:

In Canada-

* After Burn Double Strength Gel 5
* After Burn Double Strength Spray 5
* After Burn Gel 5
* After Burn Spray 5
* Alphacaine 5
* Dermoplast 2
* Endocaine 1
* Norwood Sunburn Spray 5
* Nupercainal Ointment 4
* Pramegel 7
* Shield Burnasept Spray 1
* Tronothane 6
* Xylocaine 5