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Unusual DRIs

polymath

polymath

Bluelight Crew
Joined
Nov 4, 2010
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According to the article found here, the simple compound 4-(diphenylmethyl)pyridine is as potent as cocaine in inhibiting dopamine reuptake. It also has some affinity to the 5HT and NE transporters. It's not even structurally related to any illegal drug.

Is it likely that unusual DRIs like this would be recreational? One sometimes hears of compounds like bupropion that inhibit dopamine reuptake but still have no 'abuse potential'. What factors in addition to DAT affinity contribute to the euphoria caused by cocaine-like compounds?
 
I'd say it comes close to desoxypipradrol, or 2-(diphenylmethyl)-piperidine, which is something I was quite interested in to try (I still have it lying around) but was urgently warned to steer clear from it.

Supposedly 2-DPMP is like a (too) long lasting MPH type deal - initially it may seem perfect but the high potential for insomnia, redosing, mania and stim-related mental instability I guess after what I read I would not touch it with a 10 ft pole.

Curious anyway how the compound you suggest is different. :)

(maybe you were very aware of the analogy considering 2-DPMP is not immediately illegal, although it is at the very least a scheduled pharmaceutical I think)
 
Bupropion only hits the da transporter for 20% in humans wich prob wont even cause therapeutic da mediated effects.
 
A big portion is the pharmacokinetics of a drug, stimulants seem to need to have rapid absorption and distribution to be interesting. Just looking at those compounds I can tell that they'll be lipid soluble as can be an will probably have extremely long half lives.
 
2dpmp kept me up for 4 days once(had no benzos) and I still think it's a useful drug. Little negatives compared to MPH and lasts a lot longer. And at least for me there was a dose that lasted basically all day at a level of effects that was still acceptably high.
 
Here in Finland there's been several cases where overdose of desoxypipradrol has caused rhabdomyolysis and kidney failure. I'm not sure if amphetamine OD can cause the same.
 
Rhabdomyolysis/kidney failure sounds like the result of overheating or physical tissue damage from overexertion. I was under the impression that that's the same syndrome that MDMA overdose produces.
 
polymath said:
According to the article found here, the simple compound 4-(diphenylmethyl)pyridine is as potent as cocaine in inhibiting dopamine reuptake.
Click to expand...

We should remember, though, that cocaine isn't particularly potent (hence the high dosages that are required). If anything, it's surprising that binding isn't more effective, given the structural similarity to desoxypipradrol.

solipsis said:
Supposedly 2-DPMP is like a (too) long lasting MPH type deal - initially it may seem perfect but the high potential for insomnia, redosing, mania and stim-related mental instability I guess after what I read I would not touch it with a 10 ft pole.
Click to expand...

Can you measure your dose with a scale and and avoid redosing NO MATTER WHAT (including having your judgment skewed by a stimulant high)? If so, you're okay. If not, you may accidentally be up for a few days. :p

ebola
 
w1YEJ.png


Yikes! Looks almost like like MPTP to me. 3 aromatic rings in one, no thanks...

I wonder if diphenylmethyl-piperazine is active? aka alpha-phenyl-bzp?
 
Lots of stims have a tri-ring layout, like desoxypiperidol, diphenylprolinol, pipradrol, etc. It looks like this compound is just 2-DPMP with an aromatic ring (pyridine) instead of 2-DPMP's piperidine ring. Can't really see the concern of an MPTP scenario.
 
ebola? said:
Can you measure your dose with a scale and and avoid redosing NO MATTER WHAT (including having your judgment skewed by a stimulant high)?
Click to expand...

That's probably a 'hells to the no' on the second account. 8)

OT: actually I find mesocarb to be a funny looking DRI, and lo' it is even supposedly nootropic.

These days I am restricted to things like racetams and intranasal modafinil though.
 
sekio said:
Rhabdomyolysis/kidney failure sounds like the result of overheating or physical tissue damage from overexertion. I was under the impression that that's the same syndrome that MDMA overdose produces.
Click to expand...

Yeah, rhabdomyolysis happens when the body totally runs out of energy and starts breaking down muscle all over the place -- the muscle tissue is full of potassium, which gets into the blood and destroys the kidneys and can cause heart failure in the worst cases. It can happen on anything, or even on no drugs at all -- "rhabdo" is a well-known risk among Crossfitters, for example.

ebola? said:
avoid redosing NO MATTER WHAT (including having your judgment skewed by a stimulant high)?
Click to expand...

My understanding is that this is impossible.

polymath said:
Is it likely that unusual DRIs like this would be recreational?
Click to expand...

Some of them. vecktor has stated in the past that the benzhydryl-piperidines [GBR-type compounds] are generally not recreational:

http://www.bluelight.ru/vb/threads/171971-Stimulants-of-the-Future?p=4831360&viewfull=1#post4831360

On the other hand, amfonelic acid is definitely recreational, though it isn't the Holy Grail of stimulants that some used to think it was. Ethylphenidate did a lot to demonstrate that "pure DRI" does not mean "awesome".
 
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Apparently a dopamine reuptake inhibitor doesn't even necessarily have to contain a nitrogen atom... I was a bit surprised by this.

The full text of the article found here describes a compound that's like 3,4-dichloro-methylphenidate, but has an ether oxygen in place of the amine nitrogen. Apparently that compound has DAT affinity similar to methylphenidate itself. Similar non-amine derivatives have also been made from cocaine and are identified as 'cocaine-like' by animals in drug discrimination tests.

But then again, there's also non-amine opioids, so maybe this isn't so remarkable after all.
 
On the topic of unusual DRIs, Amfonelic acid is a quinolone initially synthesized as an antibiotic but was found to be an extremely potent DRI (cited as 50x greater affinity than MPH) with a duration of 12 hours.
220px-Amfonelic_acid.png

Structure is not typical of a DRI
 
^ Too bad there doesn't seem to be any research on the SAR of amfonelic acid derivatives (what structural features in that molecule are necessary for DAT binding?).

Off topic, I wonder if there will ever be a psychedelic 5-HT2A agonist that doesn't belong to the typical phenethylamine/tryptamine/ergoline classes...
 
I'd be intrigued to see weather anything comes of those quinazoline-2,4-dione based ketanserin modifications. Tweaking the sidechain of ketanserin resulted in some partial agonists for the 5HT2aR, such as RH-34, which incorporates the 2-methoxybenzoyl group, cited in wikipedia as a moderate affinity partial agonist.

Although weather it is psychedelic or not I do not know. I haven't tried it personally. Very interesting development IMO-a completely new backbone structure, outside of the ergolines, tryptamines and phenethylamines (inc. their 3-carbon homologs and the N-benzoyl derivatives.)

http://en.wikipedia.org/wiki/RH-34
 
Nomifensine is a dual NE-DA reuptake inhibitor that binds to NET twice more effectively that to DAT. It seems to have low abuse potential. Is this because it crosses the blood brain barrier slowly or is it because of the larger effect to NE than DA?

I found an article about nomifensine derivatives that lack the amino group at aromatic ring (should make the molecule more lipid soluble): http://www.sciencedirect.com/science/article/pii/S0960894X12011961 . Some of them have higher DAT selectivity than nomifensine... Is it possible that some of these compounds could be more 'interesting' in the sense of recreational use than nomifensine itself?
 
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