MDPV - So how dangerous is it?

[Clean_Cut]

Ive combined with alcohol. Had about 8 standard drinks over 2-3 hours and had no troubles.
Ive had a mate drink more than he ever has and felt pretty sober due to the PV.
Id still try to limit it. PV is a better high anyway

 

[nuke]

Are you talking about affinity? Correct me if I'm wrong, but actually cocaine has roughly the same DAT affinity as methylphenidate. I must be missing the distinction you're making.

rotterdam-era: Uh I'm not trying to be an ass but... never underestimate the power of paragraph breaks

I'm not completely sure; I'm at a loss to find a really good assay of human NET for methylphenidate (that is, with the hot ligand as tritium labeled NE). Studies usually show cocaine having a higher affinity for DA over NE as compared to methylphenidate, but the one value for methylphenidate in human cells for DAT is very low.

Cocaine Ki (nM)
DAT 555 (Human cloned cells, Hot ligand: 3H-DA UPTAKE)
NET 217 (Human cloned cells, Hot ligand: 3H-NE UPTAKE)

Methylphenidate
DAT 42 (Human cloned cells, Hot ligand: 3H-DA UPTAKE)
NET ?

Remember, less is more.

 

[rnd.id.]

I had this research in mind (but obviously you know more than I do about the measurement methods):



http://dx.doi.org/10.1016/S0024-3205(99)00225-8

Methylphenidate and cocaine have a similar in vivo potency to block dopamine transporters in the human brain

Nora D. Volkow1, 2, Corresponding Author Contact Information, E-mail The Corresponding Author, Gene. -Jack Wang1, Joanna S. Fowler1, Marian Fischman3, Richard Foltin3, Naji N. Abumrad4, Samuel J. Gatley1, Jean Logan1, Cristopher Wong1, Andrew Gifford1, Yu-Shin Ding1, Robert Hitzemann2 and Naomi Pappas1

The similar in vivo potencies at the DAT for methylphenidate than for cocaine are in agreement with their reported relative in vitro affinities (Ki 390 nM and 640 nM respectively), which is likely to reflect the similar degree of uptake (8–10% of the injected dose) and regional distribution of these two drugs in the human brain.

 

[nuke]

The affinities in that study are from quite an old reference, and I'm not sure what the source of the receptor was (eg human, rat). There's also the difficulty of measuring the displacement of an active ligand (radiolabeled cocaine) from the receptor rather than the native substrate (DA or NE). All of the more recently reported values of methylphenidate for DAT are about 50nM in cells with human DAT -- this is much higher than cocaine. I'm starting to not really like to compare Ki values that are cross-species or using different assay hot ligands: there seems to be a lot of variability.

 

[any major dude]

I doubt it's that much more toxic than methylphenidate. Seems like a pretty run of the mill NDRI, with more emphasis on the N aspect.

are there any studies with comparative data for NE/DA activity of mdpv? I'd be really interested to know how much NE activity it has. I had been under the impression it was pretty much just a DARI

 

[ebola?]

If it is (also iff it lacks direct adrenergic agonism and particularly if it exhibits a high ratio of CNSNS fx), it would be mysterious indeed why the fucker is so jittery.

We'd need to check the metabolites too...

 

[rnd.id.]

Do we know for a fact that dopamine RI doesn't cause jitters? (Either peripherally or centrally - dopamine plays a role in movement after all)

 

[any major dude]

I don't see why it couldn't

 

[Choronzon333]

Do we know for a fact that dopamine RI doesn't cause jitters? (Either peripherally or centrally - dopamine plays a role in movement after all)

Yeh depending on who you are it definately can be jittery. Most people I see get very jittery on amphetamines and definately on meth/). I don't believe meth cuases significant Noradrenaline reuptake inhibition and I know amphetamines don't. ALthough having been prescribed amphetamines for adhd amphetamines since young childhood I must say that they haven't been much of a shaky thing for me unless I undereat, overexcercise or take way too much.

As far as mdpv, it makes you feel jittery in a much different way which is weird. I can't really describe it. Definately felt more like cocaine jitters than any amphetamines.

 

[ebola?]

Well, comparing the fx of differing DA releasers and DARIs, a pattern emerges where those agents exerting a higher ratio of dopaminergic to (nor)adrenergic fx feel 'smoother'. Think of meth vs. d-amp vs. racemic amp*, or d-methylphenidate vs. the racemate. There's an additional trend where a high ratio of CNSNS fx feels 'smoother', eg propylhexedrine vs. meth...or desoxypipradrol vs. other DARIs.

There's a problem to such speculation though: in many if not most of our comparison cases, it's difficult to dissociate these two qualities in empirically existent substances.

And then, IIRC, desoxypipradrol isn't too selective for DA.

*maybe people find meth "jittery" by dosing a 'wee bit' too high on it.

 

[Choronzon333]

Well, comparing the fx of differing DA releasers and DARIs, a pattern emerges where those agents exerting a higher ratio of dopaminergic to (nor)adrenergic fx feel 'smoother'. Think of meth vs. d-amp vs. racemic amp*, or d-methylphenidate vs. the racemate. There's an additional trend where a high ratio of CNSNS fx feels 'smoother', eg propylhexedrine vs. meth...or desoxypipradrol vs. other DARIs.

There's a problem to such speculation though: in many if not most of our comparison cases, it's difficult to dissociate these two qualities in empirically existent substances.

And then, IIRC, desoxypipradrol isn't too selective for DA.

*maybe people find meth "jittery" by dosing a 'wee bit' too high on it.

This makes sense then. Yeh amphetamines feel alot cleaner and smoother than mdpv where as it feels kinda bumpy...

 

[ebola?]

I should also add that no DA releaser lacks significant concurrent NE releasing action. In fact, even with meth's 'high selectivity', one could say that it exerts greater fx at NE than DA. I dunno...maybe 4-FA is even more selective for DA (+ minor 5ht biznass).

A theoretical exception might be careful concurrent use of a DA releaser and selective MAOB inhibitor. We should expect potentiation of DA-mediated fx to far eclipse general potentiation.

ebola

 

[boohigh]

I will add from my expierence that only beta-ketones with pyrrolydine group gave me such a jitters, no any amphetamine overdose can do this, but let's say IV 200 mg of alpha-PPP or 20 mg smoked MDPV and my hands are shaking in tremor.

 

[rnd.id.]

Think of meth vs. d-amp vs. racemic amp*

Don't forget meth's serotonin releasing action, though. Btw, I'm not doubting that NA makes the peripheral stuff worse and doesn't add much to the euphoria; the point was just whether pure dopamine RI has peripheral effects as well.

Apropos serotonin -- how sure are we that MDPV is not serotonergic at all?

Anecdote: I've been taking it with sertraline (the sertraline had been steady at 200mg for a long time before) and so far I'm still amongst the living. So have I basically reinvented cocaine, except with less heart damage? (Except that the serotonin doesn't come rushingly)

 

[PsychedelicDoctor]

I'm curious if anyone has had any experience with something that feels pulsitile in nature, spastic perhaps, with tension repeating with use of MDPV.

i have a small sample of light beige/off-white MDPV which i have used a few times to keep me awake enough to read late into the night. lately i have noticed what i would describe as a tension spasm located behind my medial ankle bone. for those without any anatomy experience, there are three muscle tendons of note, an artery, vein, and nerve passing there. they are all bound by a tight fibrous band. this is where the pulsation is felt. i can't see anything going on when it happens, though it feels like a muscle spasm somewhat. I"m trying to figure out if this is related to MDPV use and what's going on.

the drug's impact on my vitals is substantial. quickened HR and heightened BP. perhaps the increased BP would tend to expand the vessel and with the fibrous sheath, leave nowhere else for the pressure to go. there is no edema noted. I have just used approx 5mg and am currently noticing it. it has been happening all week. i have used mdpv three times during this span in these modest amount, and have redosed on two of those occasions. i am discontinuing use at this time to see what happens.

in the mean time, anyone have any similar reports or any educated guesses as to what i'm feeling. i should note, there is no pain involved.

 

[PsychedelicDoctor]

especially considering cocaine's penchant for causing vasospasm and Prinzmetal angina. no angina has been identified.

 

[PsychedelicDoctor]

the problem is resolving. at some pont last night I lost the posterior tibial pulse on my left ankle and at others it was barely present. after a hot bath, some l-arginine, ethanol, and clonazepam, i woke up this morning feeling better but with still with a weakened pulse on the left side. claudication is a bitch.

 

[kken]

Any idea still on what the orange gooey stuff is when you vaporize this? is vaporizing safe at all?

Any guesses what we are breathing in?

inhaled trough bunch of cotton the dark orange "gooey" stuff seems to be the bad tasting stuff and cotton works to filter that out. at least its tastier

 

[daddysgone]

Any idea still on what the orange gooey stuff is when you vaporize this? is vaporizing safe at all?

Any guesses what we are breathing in?

inhaled trough bunch of cotton the dark orange "gooey" stuff seems to be the bad tasting stuff and cotton works to filter that out. at least its tastier

ewwww. why risk it man? Think about the possible risk vs. reward. No one really knows enough about this substance yet to make any definitive statements about its safety. Until more is known, if you are ok with experimenting with a an unknown and potentially toxic substance, at least try to avoid things that add to the risk. What I mean by this, is that if vaping this stuff creates an odd goey substance, you probably should avoid this route of administration.-DG

 

[kken]

valid point. guess i will have to stick with sublingual or plugging


edit: just doesn't feel the same its not bad but once a while a rush would be nice. Maybe should try IV as next option for only rare use