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Research Chemicals Piperazines, Phenethylamines, Tryptamines & other designer drugs.

 
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  #26  
Old 10-05-2007, 09:50
fastandbulbous fastandbulbous is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

The (R) isomer is an impressive 3 times more powerfully drawn to the DAT than cocaine is.

Quote:
Unfortunately for them, they were trying to make a chemical that also has a high uptake value. A high uptake value would mean that when the chemical attaches itself to the DAT, it's very weak at interfering with it.

Fortunately for everyone else, they got the exact opposite, this drug has a very low Ki value for uptake, meaning it is very powerful at fucking up DAT activity.

In fact it's even better than cocaine at interfering with the DAT functioning. So in theory this drug should be very very good at raising dopamine transmission.

Maybe oral consumption is a bad way of consuming it? SWIM is going to order a gram to experiment with anyway, it's very cheap and has a great deal of potential.
It's the ratio of binding to reuptake Ki's that are most important in giving a gauge of what it'll be like:

Cocaine has a Ki binding value of 0.12uM and a Ki reuptake value of 0.20uM. Now just because something binds to the protein receptor doesn't mean it's going to do anything, so the ratio of binding to reuptake is important. If most of what binds also inhibits reuptake, you end up with a drug like cocaine with a sizable abuse potential (ratio of binding:reuptake of 1.67). Although the Ki binding value of the compound in question is 0.04uM, it takes 0.17uM to inhibit reuptake. The higher ratio of 4.25 means that it's much less effective at inhibiting reuptake as a percentage of the DAT that it binds to leading to a less abuse prone stimulant. If you got one with a ratio of say 1.2, you'd have a problem drug on your hands, even if the Ki reuptake was say 2uM (would just require a higher dose, but once achieved would be frightenly efficient ).

Subsequently, it wouldn't be a bad choice as a drug to treat coke addicts as it still provides some stimulation, but can't be made like coke by increasing the dose; it'd also partially block any coke consumed on top of it. All in all an improvement for the coke user as the compounds of this type (pipradrol derivatives - diphenylmethanol/diphenylmethyl substituted onto a nitrogen heterocycle such as piperidine, pyrrolidine or morpholine) are of very low toxicity, esp regarding the cardiovascular system; in which respect cocaine is a rather cardiotoxic drug

Post Quality Evaluations:
Informative as always. Making the abstracts and so on understandable for non-academics
  #27  
Old 10-05-2007, 16:04
lulz Gold member lulz is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

Quote:
Originally Posted by fastandbulbous View Post
If most of what binds also inhibits reuptake, you end up with a drug like cocaine with a sizable abuse potential (ratio of binding:reuptake of 1.67). Although the Ki binding value of the compound in question is 0.04uM, it takes 0.17uM to inhibit reuptake. The higher ratio of 4.25 means that it's much less effective at inhibiting reuptake as a percentage of the DAT that it binds to leading to a less abuse prone stimulant. If you got one with a ratio of say 1.2, you'd have a problem drug on your hands, even if the Ki reuptake was say 2uM (would just require a higher dose, but once achieved would be frightenly efficient ).

I don't quite understand the logic to this. From the article:

Quote:
The lower the Ki, the higher the potency.
Quote:
Kiuptake is how well the compound is at inhibiting the functioning of the DAT
Therefore a lower Ki for uptake should mean the better that the drug in question inhibits DAT activity.

So if Diphenyl-2-pyrrolidinemethanol has a higher affinity to the same site on the DAT receptor that cocaine binds to, and it interferes with the DAT better than cocaine does when it gets there, by simple logic Diphenyl-2-pyrrolidinemethanol must increase dopamine levels better than cocaine does.

The ratio on it's own can't mean anything without reference to one of the variables in each substance.

Also I've heard accounts from more than one person that if rectally adminstered, Diphenyl-2-pyrrolidinemethanol is in the same league of addictiveness as cocaine.
  #28  
Old 10-05-2007, 22:31
snapper Gold member snapper is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

As it binds, it uses up open receptor sites, so if more binds, more receptor sites are used. In spite of more binding, less dopamine reuptake is occuring which means that 4x more receptor sites need to be occupied to equal the reuptake inhibition of cocaine, but binding there blocks those sites from endogenous dopamine, cocaine or other dopamine receptor ligands. In this sense, D2PM functions in part as an antagonist, or maybe a better term is a mixed agonist. It would theoretically also block the effects MDPV, etc.
The reason rectal dosage works better is that it bypasses the liver, and consequently gets more of the D2PM into the bloodstream faster. This causes a rush as the receptors are occupied quickly, unlike oral dosing which from the onset of effects means receptors are being bound more slowly and diluting the effects. Does that help ?
  #29  
Old 10-05-2007, 23:37
lulz Gold member lulz is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

Aha, I didn't understand the significance of the ratio before, thanks for explaining it.

So cocaine's ratio means that 60% of the time when it binds to the DAT, it switches it off, which is much better than D2PM's "success rate" of about 24%.

But since D2PM has a higher affinity for DAT, wouldn't the lower "success rate" be compensated for at least partially if large enough doses were taken? I'm assuming that all DAT proteins aren't typically saturated by either cocaine or D2PM.

Also I am slightly confused about how D2PM blocks postsynaptic receptors on the neuron, I thought it binds directly to the DAT protein.
  #30  
Old 11-05-2007, 00:14
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

If you like long lasting stimulant DATI's you should turn your interest to desoxypipradrol. It leaves 2-benzhydrolpyrrolidine weeping in the dust, I believe.
  #31  
Old 11-05-2007, 01:33
Nicaine Nicaine is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

Quote:
Originally Posted by lulz View Post
But since D2PM has a higher affinity for DAT, wouldn't the lower success rate be compensated for at least partially if large enough doses were taken?
In practice, this is in fact the case. (P.S. SWIM is new here and hasn't introduced himself. He can't offer his credentials at this point, although this may become possible in the mid to long term. He's been researching chemicals for a long time, that's all he can say. If his views end up being unwanted, he will stop posting in this forum. Thanks for reading).
  #32  
Old 11-05-2007, 10:05
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

Several cases of high dose indulgence with this drug are known. I believe a majority of these cases ended up in hospital.

Please don't push the doses in the quest for euphoria with this chemical.
  #33  
Old 11-05-2007, 10:08
snapper Gold member snapper is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

What doses caused someone to be hospitalized and what happened ?
  #34  
Old 11-05-2007, 10:14
NeonCortex NeonCortex is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

They were totally stupid, humongous doses. Can't remember them all, but they were in the hundred of milligrams up to gram scale. They had to have continous IV tranquilizers for a few days, basically.
  #35  
Old 11-05-2007, 10:29
bob_arctor bob_arctor is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

Even up to several grams in one case if remembered correctly. Very tragic expression of the lack of critical thinking in the youth of today. Standard but depressing.
  #36  
Old 11-05-2007, 21:23
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

More experiences with this compound?
What are the side effects of this compound?

I've been promised a write up of experience reports in the range of 60-200 mg Diphenyl-2-Pyrrolidinyl-Methanol.
  #37  
Old 11-05-2007, 23:04
Nicaine Nicaine is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

Quote:
Originally Posted by NeonCortex View Post
Several cases of high dose indulgence with this drug are known. I believe a majority of these cases ended up in hospital. Please don't push the doses in the quest for euphoria with this chemical.
Interesting... can SWIY provide references? If true, this comes as no surprise... what would be surprising is if there were only several known cases. SWIM tells me this sort of thing should be very common in cases of recreational use of this substance. Unfortunately, asking "please don't" doesn't carry the same weight as dopamine receptors demanding "do it now."
Quote:
Originally Posted by bob_arctor View Post
Even up to several grams in one case if remembered correctly. Very tragic expression of the lack of critical thinking in the youth of today.
It would be nice if it were really that simple. ISO the tendency to overdose and/or binge eternally is in the nature of this particular substance, at least if recreational effects are the goal being sought. It's amazingly deceptive, as noted by numerous "this stuff does almost nothing" reports.

Last edited by Nicaine; 11-05-2007 at 23:16.
  #38  
Old 11-05-2007, 23:26
Nagognog2 Nagognog2 is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

Probably for the reasons noted above: Desiring to keep taking more and increasing the dose higher and highr. Then there is a little matter of duration of effects...
  #39  
Old 12-05-2007, 00:04
Nicaine Nicaine is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

Dopamine isn't SWIM's area of expertise; are there other dopamine agonist/antagonists, particularly anything actually in use? It could be the whole concept is fatally flawed. It seems likely antagonism would result in a sense of desperate frustration, while the agonism continued the pursuit. It's hard to imagine a worse combination, unless timing was the critical factor. In other words, which came first, and when.
  #40  
Old 12-05-2007, 01:06
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

There are lots of dopamine agonists and antagonists in use. More relevant to this case, there are also several dopamine reuptake inhibitors in use. Drugs for parkinsons, depression, adhd, narcolepsy, psychosis, etc.

What do you mean by "verifiable data"? The data on overdoses I and Arctor presented are very real. It happened just after a vendor started selling this compound cheaply. The "data" is not in some kind of journal, hence no reference.

ISO's opinion is that this substance's only use as a psychoactive is for alertness - in proper dosages, not as an euphoriant. It is a dead end when it comes to euphoric stimulation.

Last edited by NeonCortex; 12-05-2007 at 01:12.
  #41  
Old 12-05-2007, 01:18
snapper Gold member snapper is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

That's what SWIM meant - the data is a testimonial. Not much is known about the safety and dosing of this drug, so any specific information, even involving overdoses, is useful to the community at large.
SWIM agrees that this product is significantly euphoric. However, what is the ideal stimulant dose, what might occur in combination with other products and with different routes of administration has yet to be established. Any information is potentially useful...
  #42  
Old 12-05-2007, 01:37
Nicaine Nicaine is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

Quote:
Originally Posted by NeonCortex View Post
There are lots of dopamine agonists and antagonists in use. More relevant to this case, there are also several dopamine reuptake inhibitors in use. Drugs for parkinsons, depression, adhd, narcolepsy, psychosis, etc.
I meant combination agonist/antagonists. Substances that have both properties simultaneously, as in opiate receptor examples like buprenorphine.
Quote:
What do you mean by "verifiable"? The data on overdoses I and Arctor presented are very real. It happened just after a vendor started selling this compound cheaply. The "data" is not in some kind of journal, hence no reference.
Sorry, I didn't mean to suggest your data wasn't real, merely that I hadn't seen it. It does in fact come across as likely outcome for this substance, as I previously stated.
Quote:
ISO's opinion is that this substance's only use as a psychoactive is for alertness - in proper dosages, not as an euphoriant. It is a dead end when it comes to euphoric stimulation.
If there isn't any 'push' or tendency toward gradual dosage increases and eventual addiction, SWIM agrees... otherwise it could be considered a dead end there too, unless discipline on the part of the user is presupposed (pardon the negativism, but SWIM hasn't found this quality to be common in his fellow human beings). As far as being a dead end in terms of euphoric stimulation, unless the user were willing to accept a high degree of risk, SWIM concurs.
Quote:
Originally Posted by Alfa View Post
Note that he took close to a gram of Dipenyl-2-Prrolidinyl-methanol in 5 days and quantities of the desoxypipradol analog had also been taken around that period.
Given various uncertainties (body weight, method of admin, etc) ~1g in 5 days strikes SWIM as pushing the borderline of safety issues but not necessarily going over. If it involved no sleep or food in 5 days, never mind... that complicates the matter beyond any rational analysis.

Last edited by Nicaine; 12-05-2007 at 02:06.
  #43  
Old 12-05-2007, 01:48
snapper Gold member snapper is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

Most receptor binding involves some degree of antagonism. It depends on how long the molecule is bound in the receptor site and how much it activates the receptor when bound to it. Reuptake mechanisms can be similarly considered.
  #44  
Old 13-05-2007, 04:50
Nicaine Nicaine is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

Out of curiosity, has anyone considered some simple experiments actually involving a rat or other small rodent: e.g. two water supplies, one with the compound added in the proper mg/kg ratio, one without. Then observing if the animal tends to choose the water source containing D-2-P-M, and if so how often and in what amounts? This would be an experiment any layman could perform, given access to a pet-store. Even under uncontrolled conditions, it would be interesting to hear the results of such an experiment. Dopamine reuptake inhibition typically involves compulsivity, and the animal's behavior might provide a rough estimate how compulsive this substance is and whether a tendency to overdose really is in the nature of the substance or just related to human beings seeking something it doesn't provide.

Last edited by Nicaine; 13-05-2007 at 04:59.
  #45  
Old 20-05-2007, 04:44
Nicaine Nicaine is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

Quote:
Originally Posted by nanobrain View Post
smoking is not viable, neither is insufflation and for what its worth, the ratties found oral dosing virtually worthless.
SWIM's friend (who gave the brief experience posted earlier) wanted to see why it isn't smokable. According to him, the stuff is like gunpowder... it catches fire and burns rapidly when heated, emitting a nasty black smoke. Luckily for him (that's SWIM's judgment) he didn't attempt to inhale any of it. As vivid as the description SWIM heard, it sounds like the stuff could be explosive if packed tightly and subjected to flame or high heat.

Last edited by Nicaine; 20-05-2007 at 04:52.
  #46  
Old 20-05-2007, 08:22
snapper Gold member snapper is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

Hmm. Maybe that's what SWIM could do with the rest. Sounds more useful than flushing it. SWIM also concurs, but with a different ratio - 1/3 hint of good dopamine effects, 2/3 cracked out like drinking too much coffee and feeling vaguely ill. Too bad, but you never know until you try. SWIM wants MDPV back. Why mess with a good thing ?
  #47  
Old 20-05-2007, 10:19
Nicaine Nicaine is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

Quote:
Originally Posted by snapper View Post
Hmm. Maybe that's what SWIM could do with the rest. Sounds more useful than flushing it.
SWIM has none in possession; he's not using a figure of speech here, he really does have a buddy who has been relaying information on his request. SWIM has been either interested in or involved with research chemicals for over ten years, and chats with lots of folks on a regular basis. A friend recently got interested and acquired some Di2PyMeth, but does not want to bother signing up here.
Quote:
SWIM also concurs, but with a different ratio - 1/3 hint of good dopamine effects, 2/3 cracked out like drinking too much coffee and feeling vaguely ill. Too bad, but you never know until you try. SWIM wants MDPV back. Why mess with a good thing ?
MDPV strikes SWIM as generally safer and more effective than diphenyl prolinol, no doubt about it. Its only serious issue seems to be a level of compulsivity akin to slavery (SWIM is talking regular use here of course), but there's a lot of variation in how people react to and deal with this. Some are less affected than others, and a very few claim to be entirely unaffected, or able to easily overcome it using "will-power." At this point, SWIM is reserving judgment on the claims of this tiny minority due to insufficient data.

Postscript: the "cracked out" feeling can be ameliorated somewhat through the judicious and careful use of CNS depressants, although SWIY was probably already aware of this .
  #48  
Old 22-05-2007, 20:59
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

Something tells me smoking this is not the wisest of ideas.
  #49  
Old 22-05-2007, 22:52
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

SWIM thinks smoking most compounds is not wise. SWIM knows people smoke things like meth and freebase, but these people do do damage to their lungs. It is one thing to vaporize something known to not degrade (DMT, DPT,etc), but with a complete unknown, it really is gambling with one's wellbeing. Sometimes experimenting can have dramatic consequences. SWIM wholeheartedly agrees with Alfa.
Interesting research BioCellular Enigma, but someSWIM needs to analyze this stuff after vaporization and same with MDPV, before SWIM would even consider vaporization.
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Old 24-05-2007, 02:30
Nicaine Nicaine is offline
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Re: Diphenyl-2-Pyrrolidinyl-Methanol

Quote:
Originally Posted by Alfa View Post
Something tells me smoking this is not the wisest of ideas.
SWIM believes that's particularly true until someone posts about what's happening in the chemical reaction he mentioned, and what the resulting end product really is. SWIM is not up enough on chemistry to know if what's happening is a salt being converted to a base (ala cocaine to crack) or something else entirely.


Even if it were D2PM free base, SWIM doesn't know if it would vaporize, break down (which at best would waste product, at worst be inhaling some unknown chemical doing who knows what) or some combination of the two. He does strongly suspect there's at least some D2PM in the smoke.

It would help greatly as well to know if the smoke is toxic to the lungs (more accurately, too toxic to be worth it)... even if it were purely vaporized D2PM, the stuff is too irritating to be snorted, so it could possibly be harmful if inhaled.

If all that were figured out and found to be safe, SWIM thinks it would probably be OK (insofar as smoking stimulants ever would be anyway).
Quote:
Originally Posted by snapper View Post
It is one thing to vaporize something known to not degrade (DMT, DPT,etc), but with a complete unknown, it really is gambling with one's wellbeing.
Fwiw, ingesting D2PM at all may be gambing with one's well-being. This was the one tested for use in treating cocaine addicts, correct? If so, he's wondering if anyone knows for sure why it was rejected and not released as a pharmaceutical drug. If not, it is an unknown quantity itself, never mind the smoke.

Supposing it were originally meant for cocaine withdrawal and withdrawn for reasons other than health, SWIM has seen a few accounts floating around of addictive behavior with this substance, which depending on a lot of factors could be very toxic; e.g. large amounts ingested harming various organs.

Anyway, SWIM is not saying this makes smoking it a good idea, just that taking it at all is likely not a good idea and should be limited to risk-takers willing to sacrifice their health. Smoking it may be worse, and given the fragile nature of the lungs and fairly common fact of toxins showing up in smoke he agrees nobody should do it until some basics are known.

Last edited by Nicaine; 24-05-2007 at 02:52.

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2-dpmp, addicts, amphetamines, cocaine, coffee, coke, d2pm, desoxypipradol, desoxypipradrol, diphenyl-2-pyrrolidinyl-methanol, diphenylprolinol, dopamine, dopamine agonist, drug, drugs forum, euphoric, insufflation, mdpv, methylone, methylphenidate, neuroblast, orgasm, overdose, plugging, receptor binding, research chemicals, sexual, stimulant, vaporize

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