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Stimulants of the Future

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Actually the '1st day if spring' quip was just that it was very nice to find a CNS stimulant that doesn't leave me feeling like I've got a bit too much adrenaline in my bloodstream. Just looking at vecktors post, it mentions the (adopt Edinburgh schoolmistress voice) creme de la creme stimulant IMO, fencamfamine. That was so smooth it was the James Bond of stimulannts!


Oh, one other thing I like about it (desoxypipradrol), it has bog all anorectic effect, which means I can have my cake and eat it! (as opposed to looking at it, feeling a bit sick and saying I might try a bit later... =D )
 
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fencamfamine is very very pleasant, it seems to have the right amount of releasing versus reuptake action on the right neurotransmitters...salivating now

other fencamfamine analogs include the N-methyl analogue, the N-propyl analogue, the 2' hydroxyphenyl analogue etc etc. whilst at first sight the nornbornane appears complex to synthesise and there is the obvious problem of multiple isomers, diels adler is a great reaction and a good use of those pesky itchy nitrostyrenes.

the original merck patent deals with the nn dimethylamino the n-methyl etc
patent GB 913866

a word of warnng, I have made the mistake of misordering fencamine which whilst a stimulant is totally unrelated.
 
If fencamfamine (fencamfamin according to DEA) is so good, why isn't it more popular? Why isn't it more abused? Why is it only C-IV? :o

Are we talking about the stuff, that is sold/has been sold under the name Reactivan?
 
Survival0200 said:
If fencamfamine (fencamfamin according to DEA) is so good, why isn't it more popular? Why isn't it more abused? Why is it only C-IV? :o

Are we talking about the stuff, that is sold/has been sold under the name Reactivan?
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because cocaine is more readily available?
because the average muppet meth or MDMA chemist would struggle with the synthesis? who knows.

In the UK at least it is very rarely prescribed and is a controlled drug

Reactivan is a merck trade name for low dose fencamfamine 10mg per tablet plus vitamins.

there are several drugs out there which are inexplicably unpopular, despite being rather tasty.

now I shall ask ze questions..

what does flushed tomato smiley mean? :o
 
While we are on the subject of fencamfamine derivatives, does anyone know anything about the 2-(Aminomethyl)-3-phenylbicyclo[2.2.2]- and -[2.2.1]alkane dopamine uptake inhibitors, most recently cited in this article:

J. Med. Chem., 42 (5), 882 -895, 1999.
 
a word of warnng, I have made the mistake of misordering fencamine which whilst a stimulant is totally unrelated.
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Well I actually ordered fencamfamine (in the days when Aldrich still dealt eith me) & just before it was readded to thre Misuse of Drugs Act, had a couple of policemen come round to remind me of it's changing status & the need to dispose of it as I didn't have a Home Office licence. Guess how it was disposed of? - That was a rather good Xmas as I recall!

I have no idea why it never caught the imagination of the drug using community as the people who got to try some thought it was infinitely better than amphetamine's rough & ready feel
 
If I remember correctly, Fencamfamine is Sch. 1 in Canada, along with Cocaine and all Opiates. The same schedule contains PCP, a couple of obsecure benzos (definitely brow-raising) and a few barbiturates.

Canadian schedules are very weird. It seems like they are organized roughly according to drug category (rather than claimed medical usefulness as with the US). Sch.2 is entirely devoted to cannabinoids. Sch. 3 seems to comprise most tryptamines and phenethylamines/amphetamines, and I think Ketamine. Sch. 4 is mostly benzos and the rest of the barbs and depressants. The lower schedules deal with precursors and steroids.

EDIT: nevermind, I actually mixed up Fencamfamine's and Ketamine's scheuling. It is actually the former is Sch. 4 and the latter is Sch. 1 as a sub-article of PCP. How nauseating.

EDIT2: Hahaha. I just came across this article randomly while skittering through the CDSA trying to figure out the rationalle.

[pertaining to benzodiazepines in pariticular] (3) A targeted substance [viz. benzos] that constitutes the remainder of an open ampule, the partial contents of which have been administered to a patient, may be destroyed by a hospital employee who is a licensed health professional without a witness.
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I love the fact that it "may" be "destroyed" without a witness. So I guess if you're a doctor, you can always give half-assed shots of benzos to patients and "destroy" the rest with your liver ;). Sorry to go off topic but I find this ammusing.
 
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What about a stimulant that works as an antagonist at melatonin receptors? I don't think that there are any that has such a particular mode of action.
 
vecktor said:
there is a thesis related to the J med chem article here:

http://etd.gatech.edu/theses/available/etd-06242004-225750/unrestricted/moore_susanna_200406_phd.pdf
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Had a read through tyhat last night & it was very interesting, a lot of the compounds didn't have the usual Aryl-C-C-N structure as their basis. Also had a bit about the postulated pharmacophore for the DAT binding site. Lots of food for thought. It does seem that if you want to design a really good dopamine reuptake inhibitor, it's a def advantage to have a conformationally restricted structure to stick your other bits on to (that's real SAR-design talk for you!); generally formed by joining together two ring structures eg tropane or norborane.

Does make the synthetic chemistry involved a bit of a pain in the arse unless you've got something useful like diels-alder additions to play around with. I'm Surprised that they haven't also had a bit play around with the adamantane structure in the hunt for something to act as a methadone equivalent for cocaine addiction (or maybe they have - it's quite a while since I've been in a university library), as it's rigid enough and I believe 1-adamantanamine has dopaminergic activity.
 
fastandbulbous said:
Had a read through tyhat last night & it was very interesting, a lot of the compounds didn't have the usual Aryl-C-C-N structure as their basis. Also had a bit about the postulated pharmacophore for the DAT binding site. Lots of food for thought. It does seem that if you want to design a really good dopamine reuptake inhibitor, it's a def advantage to have a conformationally restricted structure to stick your other bits on to (that's real SAR-design talk for you!); generally formed by joining together two ring structures eg tropane or norborane.

Does make the synthetic chemistry involved a bit of a pain in the arse unless you've got something useful like diels-alder additions to play around with. I'm Surprised that they haven't also had a bit play around with the adamantane structure in the hunt for something to act as a methadone equivalent for cocaine addiction (or maybe they have - it's quite a while since I've been in a university library), as it's rigid enough and I believe 1-adamantanamine has dopaminergic activity.
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If I can find it I will post a link to an indian thesis which is most concerned with some seriously cool chemistry but as an aside mentions forward and back bridged cocaine or rather WIN analogues imagine a bridge fron the tropane N to the carboxylic ester position or to the other ring the forward bridged compounds are potent DAT inhibitors, if it is not online anymore I will have to find somewhere to post it and link to there. there is certainly potential for a forward bridged fencamfamine analog.

I am very interested in fencamfamine, 1 because it is nice and 2 because it is a substrate type releaser as well as a reuptake inhibitor and there is potential to modify the Dopamine, Serotonin, norepinephrine ratio.
 
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shvender hoot said:
What about a stimulant that works as an antagonist at melatonin receptors? I don't think that there are any that has such a particular mode of action.
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for a minute I thought you said melanocortin which is interesting rather than melatonin which doesn't seem to be.
I suspect that partial agonists or antagonist of melatonin will mildly mess with the circadian rhythem and not a lot else,
the abstrat is ere
http://www.ncbi.nlm.nih.gov/entrez/...ve&db=PubMed&list_uids=10350542&dopt=Abstract
 
^ Yeah, I was thinking that - melatonin has very little to do with motivation or reward pathways, which is what makes the previously discussed drugs so interesting. As vecktor said, they'd just chance to fuck up the circadian rhythm, meaning that you'd get disturbed levels of things like cortisol etc that are mostly released at certain times of day.

It might be of some value as an adjunct to antidepressants in things like SAD (seasonal affective disorder), but I think the risk of disrupting a lot of endocrine function is a bit dodgy
 
Actually as a little afternote on my ramblings about desoxypipradrol (2-(alpha,alpha-diphenylmethyl)piperidine ), I'm not sure if it has an exceedingly long half life, but otherwise it does seem to have an antidepressant effect that continues on long after the main central stimulation has ceased. I will be giving a couple more trials at differing doses, but I don't think it's something that would appeal to your hardcore speedfreaks as it doesn't appear to produce a rush at the onset of action (that might change with higher doses or route of administration though), but more of a gradual clearing of the head. The people who would find it interesting though are those wanting something to lift their mood and allow them to concentrate for prolonged periods; also as it seems to lack the sexual arousal properties of MDPV and is almost absent of physical signs of use which makes it much more suited to essay writing, driving etc than MDPV & especially any of the amphetamines. The mood lift is quite pronounced and has a euphoric component to it, but not distractingly so as can occur with amphetamines.

The closely related compound pipradrol used to be prescribed to people on opiate dependance in the 70s & 80s to increase motivation etc and this seems to be like a pipradrol with nitrous injection. Sadly pipradrol was added to the Misuse of Drugs Act in 1977 in the UK and after that it's use/prescription slowly diminished to nothing - this compound seems like a worthy, souped up version of it
 
fastandbulbous said:
Well I suppose it can, just that with me, the acronym SAD instantly translates as seasonal affective disorder because I suffer from the bloody condition.
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Me too, for my entire undergrad, then I moved to sunny California %)
and now for something completely relevant...
 
^ Just to end the OT bit, where were you living before going to California? I live in the N of England where even in the summer you get plenty of days where it's overcast and all that gets through is a dull grey light :(

I'd probably go hyperactive & explode if I moved to somewhere that had proper summers!
 
The Pacific Northwest of USA. It is ALWAYS grey in the winter. It rains probably 5/7 days and is of a similar latitude to N England, so it's always twilight in the winter anyway. (and to you Seattle folk, Olympia gets twice as much rain as you!)
The summers were awesome though, 75+ days of gorgeous sunshine, which put me into long term manic-depressive. I damned near did explode when that big bright thing would break the grey shield.
Slightly on topic, is it any wonder stimulant ABUSE is high in these areas? ;)
 
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