Novel stimulant compounds (perhaps with less spam than the 'stims of the future')

[Riemann Zeta]

I have a few questions concerning several new possible stimulant compounds, but the "Stimulants of the Future" thread has virtually collapsed under its own weight--there is some gold in there, but the signal to noise ratio has gotten pretty low. So, on to the chemicals:

First, does anyone have any information on the compound known as VSF-173? Supposedly, it is a novel 'wake-promoting' chemical (i.e. probably a non-amphetamine mild stimulant like modafinil) that is currently in P-II trials. The patent is owned by a company called Vanda Pharm. I can't even find the structure of this one, let alone the patent information or any hint as to the mechanism of action.

Second, has anyone out there tried (R)-modafinil yet? It is (obviously) the single enantiomer of modafinil. While modafinil did not really need to be enantiomerically separated (it is not particularly stereospecific like (d)-amphetamine or (d)-methylphenidate), I hear that the (R)-enantiomer lasts longer, comes in higher doses (50, 150 and 250mg) and has a better pill formulation. Normally the pill formulation wouldn't matter, but modafinil is a quirky drug--different excipients and production methods seem to effect bioavailablity.

Also, I would like to open up the floor to anyone would has tried one of the particular rare gems of the stimulant world. For example, prolintane ([N-pyrrolidyl]-alpha-ethyl-phenethylamine), pyrovalerone or N-propyl-amphetamine. Most of all, I would like to hear some opinions of the ultra-rare gem desoxypipradrol. I have always wanted to try this one; it seems like a clean, long-lasting, less-annoying version of methylphenidate with better oral bioavailability. Considering, however, that it has been barely mentioned since the 1950s--save for some nice info posted here--it will likely remain an esoteric footnote in the history of tweakage.

 

[Xorkoth]

I experimented with desoxy a while back, and it's one of my favorite stimulants. I made a number of posts with it in the Desoxypipradrol thread started by F&B in Trip Reports.

At first I wasn't a big fan. But once I got used to it and made it to 10mg plus a poissible 5-6mg at the 8-hour mark, I started to really like it and I ended up "experimenting" for almost 2 weeks in a row. As time went on I liked it more and more. It became very euphoric for me. The euphoria peaked around 8 hours or so in, and I'd just want to talk non-stop. Sex was enhanced a lot but there was no fiending for it. I could sleep a bit each night, but overall I ended up with a bit of sleep deprivation by the end. My final dose was strange and somewhat psychedelic, with visuals and an extreme experience of depersonalization while laying down listening to music.

After that period of constant use, I went into a rut for a little while, partly also due to work and stress. So that wasn't cool. But it only happened after sustained constant use. Also, it made my sweat smell really bad and it made me sweat a lot. That was most uncool, as it was really bad. I disgusted myself at times even though I used deodorant several times a day and always showered in the mornings. And I don't normally sweat abnormally much.

My posts in the experience thread go into more detail if you're curious, and there is a lot more discussion about desoxy (11 pages I think, actually).

 

[MDPVagrant]

I experimented with desoxy a while back, and it's one of my favorite stimulants. I made a number of posts with it in the Desoxypipradrol thread started by F&B in Trip Reports.

At first I wasn't a big fan. But once I got used to it and made it to 10mg plus a poissible 5-6mg at the 8-hour mark, I started to really like it and I ended up "experimenting" for almost 2 weeks in a row. As time went on I liked it more and more. It became very euphoric for me. The euphoria peaked around 8 hours or so in, and I'd just want to talk non-stop. Sex was enhanced a lot but there was no fiending for it. I could sleep a bit each night, but overall I ended up with a bit of sleep deprivation by the end. My final dose was strange and somewhat psychedelic, with visuals and an extreme experience of depersonalization while laying down listening to music.

Probably dopamine psychosis... frankly, I view the stuff as a menace at this point. But I was really a serious idiot dosage-wise last time I tested my labrats, so you might want to take what I say with a grain of salt. Anyway, I would not recommend desoxypipradrol to my worst enemy. Nobody should have to find out what getting almost no (REM) sleep for two weeks straight is like.

 

[hussness]

We you only on desoxypipradrol during that time? I wasn't aware of people staying up for 2 weeks straight on anything less than meth.

 

[Paregoric Kid]

Diphenyl prolinol, desoxypipradrol, bemegride (not sure but I've read it is equivalent to phendimetrazine and pemoline), lometopane, there are many more

 

[Jamshyd]

We you only on desoxypipradrol during that time? I wasn't aware of people staying up for 2 weeks straight on anything less than meth.

Although I haven't tried desoxypiperadol, the mania I found it induces in people who post here was scary enough.

I don't know what all the interest in new stims is. You can't go much worse than meth, and meth is already bad enough. It seems that good stims are good thanks to their dopaminergic action, and that means that sooner or later they will turn people into maniacs.

It would be interesting to find a euphoric stim that does not eventually lead to dopaminergic psychotoxicity.

 

[fastandbulbous]

I found desoxypipradrol to be very nice, subtle, incredibly long lasting and almost devoid of physical symptoms. It's a good background stimulant at the 2-5mg dose range (keeps you up and at 'em for hours), it's just that in the full on dose range (8mg+) you can say goodbye to sleep for a good 36 hours

 

[Riemann Zeta]

F&B: Wow, 36 hours of insomnia from a <10mg dose. While I have never had any trouble falling asleep after a stimulant, this one sounds particularly likely to cause insomnia. Anything that eliminates sleep to that extent will probably make people edgy, paranoid and (eventually) downright loony. In addition to the paranoia of cocaine/amphetamine psychosis experienced after days of high-dose administration, I can see where people would run into trouble.

Bemegride? Now this one is a truly weird fellow. It seems to be an anti-barbiturate, much like flumazenil is an anti-benzodiazepine. How can this be compared to a dopaminergic stimulant like pemoline or phenmetrazine? It seems like it might be more of an analeptic convulsant, rather than a proper psychostimulant.

 

[LuxEtVeritas]

Diphenyl prolinol, desoxypipradrol, bemegride (not sure but I've read it is equivalent to phendimetrazine and pemoline), lometopane, there are many more

interesting to bring up bemegride as it is so unrelated to most other classic stims and as well we had been discussing thujone/absinthe and GABA-A antagonism and that is I believe the mode in which this works and produces a stim effect of comparable potency to pemoline or phendimetrazine, though i do not believe the finer qualitative effects may be considered at all parallel

also if used/"abused" recreationally the dose requires fairly rapid escalation, which perhaps is inhernet to the pathway of GABA-A modulation

as such also i believe it certainly can have an anxiogenic potential and likely is something that has a more individual effect variance

 

[almost-]

That desoxypipradrol really sounds like a compound I want to try.

I have tried prolintane orally a couple of time, it's really smooth, quite motivating and mildly euphoric.

 

[Refluxer]

For me and several others I know of, +36h on 8 mg is an exagerration - to say the least. Individual sensitivity seems somewhat pronounced in desoxypipradrol. Have slept by midnight with 10-15 mg in the morning.

 

[hussness]

I wonder if the lipophilicity of desoxypipradol might be partially responsible for the duration of effects and what seems to be a wide variance in dose-response.

 

[Paregoric Kid]

yeah I knew bemegride didn't work through the same pathways that most abused stimulants do but there are some interesting things I've read about it.

In "Drugs of Abuse in the Future," Shulgin (1975) directed attention to another stimulant which also does not contain the phenylethylamine substructure and, in fact, is reminiscent of the depressant glutethimide. The compound is known commercially as bemegride, 4-ethyl-4-methylpiperidine-2,6-dione, and was first synthesized by Thole and Thorpe in 1911 (Thole and Thorpe 1911). The principal medical use is as an analeptic in barbiturate poisoning. As a stimulant, bemegride is approximately equal to phendimetrazine and pemoline in potency. Although glutethimide and bemegride are structurally similar, their pharmacokinetics are diametrically opposed. Hence, bemegride cannot be described as a CsA. Bemegride, by virtue of being a stimulant, has an obvious potential for abuse, although under the conditions of abuse, rather large quantities of the drug will be required. Increasing the possibility of bemegride abuse are the facts that the synthesis of the compound is not difficult and, of course, does not use either a controlled or watched substance as a precursor (Benica and Wilson 1950).

the stimulants that really interest me the most are lefetamine and fencamfamine because of their opioid activity.

 

[LuxEtVeritas]

^^^^^

FCF is never noted as having any opioid type 'feel' present in its effect and simply is relatable as a near optimum stimulant effect


LFA is a relative weak compound with potential neurotoxicity, but is truly more a mix of both true stimulant and opioid effect

 

[Paregoric Kid]

lefetamine is said to be about equivalent to morphine and ritalin, I wouldn't necessarily call that weak. as for it being neurotoxic, well hey so is amphetamine. I wasn't suggesting fencamfamine was equivalent to lefetamines opioid effects but it does effect the opioid receptors and some of its effects can be reversed with naloxone. look up the paper Reinforcing properties of fencamfamine: involvement of dopamine and opioid receptors.

 

[MDPVagrant]

We you only on desoxypipradrol during that time? I wasn't aware of people staying up for 2 weeks straight on anything less than meth.

No, but I don't want to get into the whole story here. I was up "only" 4-5 days. The rest was probably my own brain, although the amount fed to the rats in those 5-ish days... never mind.

Although I haven't tried desoxypiperadol, the mania I found it induces in people who post here was scary enough.

Hard to know how much of that is sleep deprivation, but you hit the nail on the head. Doing too much in too short a period of time appears to induce a psychotic mania. Yes, it is terrifying. Enough to turn a person off to stimulants forever, provided they survive (e.g. suicide).

I wonder if the lipophilicity of desoxypipradol might be partially responsible for the duration of effects and what seems to be a wide variance in dose-response.

Hard to say for sure, but makes sense. IMO it is potentially dangerous, and high dose use constitutes poisoning. Sorry to go off topic (desoxypipradrol is hardly novel), but just following the harm reduction theme of the forum. I won't post again on the topic here.

 

[LuxEtVeritas]

anything is only as good as knowing how to use it effectively on an individual response basis

 

[Refluxer]

I wonder if the lipophilicity of desoxypipradol might be partially responsible for the duration of effects and what seems to be a wide variance in dose-response.

The lipophilicity is most certainly one of the reasons behind the high potency and reduced PNS-activity compared to methylphenidate. Compare with morphine/heroin, where the activity of heroin is mostly due to the fact that it is better at penetrating the BBB (although morphine is the major active once in the brain). I'm unsure about the high variation in response, many factors contribute.

 

[MattPsy]

Well, does plain/vanilla pipradrol have a wide variance in effects like it's deoxy derivative ?
If not, then yeah, could be a valid explanation.

Hmm, i'd be interested to know what happens if you can tack on a group to enable greater lipophilicity to pipradrol. Something simple like an acetyl ester (in keeping with the morphine theme, kinda)

 

[MDPVagrant]

2c-b-bzp

My lab monkey was recently fed a small dose of this (<50mg) in combination with gabapentin, and the euphoria noted came as something of a surprise. Dunno if it's different than regular 'ol BZP or not though. Future experiments MAY be of interest, but stimulants have become a very iffy proposition in terms of my schedule. If they're ever fed any more it will be in smaller, one-off doses only, as I'm no longer formally researching stimulants.