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HDMP-28 or methylnaphthidate

fastandbulbous said:
Don't know what the obsession with replacing a phenyl group with a naphthyl - it's geting as bad as wanting to stick a methylenediox ring on every stimulant...
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Napthyls have consistently added 5HT action to NE/DA specific drugs - look at naphyrone vs pyrovalerone, this vs methylphenidate, napthylisopropylamine vs amphetamine, etc. Now, it's pretty much the last sort of ring I'd like to see on a drug, but serotonin is probably the reason.

'Course, after seeing 6-APB, I have to wonder if a benzofuran wouldn't work just as well as a napthyl, but I don't know if that's better news metabolically.
 
Benzofurans are not considered to be first choice due to hepatotoxicity. Why not a (iso)quinoline?

- Murphy
 
seems to have high abuse potential

if im understand this right. i think its saying that its reinforcing effects were equal to cocaine and methylphenidate, and greater than the other analogs

http://jpet.aspetjournals.org/content/307/1/356.abstract

All drugs had reinforcing effects except HDMP-29. The rank ordering of the peak breaking points (BPs) was cocaine = MP = HDMP-28 ≥ HD-60 ≥ PTT ≥ HD-23 > HDMP-29. The time to peak DAT occupancy for the cocaine analogs was greater than 30 min. The potency to maintain peak BP was significantly correlated with DAT affinity. There was not a linear relationship between monoamine transporter affinity and reinforcing efficacy, but it appeared that in nonhuman primates there is a range of DAT affinity under which maximal responding is maintained. Interestingly, the 5-HTT-selective cocaine analog HD-60 functioned robustly as a reinforcer at several doses in all monkeys tested. These data question the dogma regarding the role of pharmacokinetic factors and the relative influence of DAT and 5-HTT in stimulant reinforcement.
 
Its interesting that of 6 tested MPH analogs and cocaine HDMP-28 had the lowest potential for self administration of them all, does not bode especially well. ahem ahem ahem 3,4-DCl-MPH...
 
dread said:
Why just one? We can stick five of them on it!!!

pahmda.png



OMG THIS IS THE COOLEST STRUCTURE EVER!!!!!!!1111

I'm going to call it either mephzo-furydrone or NRG-3.14. Haven't decided yet.
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muhahaha we need more threads of that. it should be called penta-mdma that will make it a better seller.
 
Genius! :D Oh my what a mutant. It's so mutagenic it's a tumorous molecule, it's own victim.

And 'vegetative'... lol :')

But seriously keep those pyrrolidines and naphthalenes away from me :\

On-topic with my limited understanding I would personally go for p-fluoro-methylphenidate, or
perhaps I should say methyl-4-fluorophenidate.
 
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frankblank said:
if im understand this right. i think its saying that its reinforcing effects were equal to cocaine and methylphenidate, and greater than the other analogs

http://jpet.aspetjournals.org/content/307/1/356.abstract

All drugs had reinforcing effects except HDMP-29. The rank ordering of the peak breaking points (BPs) was cocaine = MP = HDMP-28 ≥ HD-60 ≥ PTT ≥ HD-23 > HDMP-29. The time to peak DAT occupancy for the cocaine analogs was greater than 30 min. The potency to maintain peak BP was significantly correlated with DAT affinity. There was not a linear relationship between monoamine transporter affinity and reinforcing efficacy, but it appeared that in nonhuman primates there is a range of DAT affinity under which maximal responding is maintained. Interestingly, the 5-HTT-selective cocaine analog HD-60 functioned robustly as a reinforcer at several doses in all monkeys tested. These data question the dogma regarding the role of pharmacokinetic factors and the relative influence of DAT and 5-HTT in stimulant reinforcement.
Click to expand...

Reference is appreciated
 
negrogesic said:
Reference is appreciated
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That study is awesome. It's just a shame they didn't check the analogues for their s1r and s2r affinity which seems to play a relatively important role in cocaine's reinforcing properties. In particular I'm wondering if HD-60 has affinity for s2r. Couldn't find any info on that. This seems like a huge flaw, especially when looking at their regression analysis... Then again, if you're only interested in a worthy coke analogue, data seems sufficient to suggest HDMP-28 wouldn't be all that bad a candidate. :D
Personally I think the reinforcing properties also depend a lot on how sharp the drop in a substance's action is. It's my understanding that cocaine dissociates very quickly after hydrolysis of it's ester bonds to DAT has occured, which aren't formed by most other molecules when they dock to DAT. I'm not familiar with the specifics of this process, but from personal experience most of us will agree that the craving kicks in very rapidly after the main pleasurable effects have begun to drop off. This is rarely paid attention to and the pharmacokinetic focus of the study is instead on how rapidly the drug takes effect or for how long it does so.
 
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I bet Penta-MDMA would burn pretty well.

maybe you could pave you driveway with it?
 
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