• Neuroscience & Pharmacology Discussion Welcome Guest
    Posting Rules Bluelight Rules
    Recent Journal Articles Chemistry Mega-Thread
    FREE Chemistry Databases! Self-Education Guide

  • N&PD Moderators: Skorpio

Dimethocaine

Aeon Psyche

Aeon Psyche

Bluelighter
Joined
Dec 11, 2007
Messages
2,146
Hi, do you guys think this would be a nice compound? (3-diethylamino-2,2-dimethylpropyl)-4-aminobenzoate ? :)
 
is this now available as an RC? I knew it was going to be soon, but i hadn't seen that it was actually available yet.

Yes, it's not bad- however, be careful with dosing too high because too much local aneasthetic + your heart is a bad combination. If you're going to have problems being careful with it, I'd avoid it.
 
Wow, this is a shockingly bad idea. If individuals are that desperate for a cocaine-like DAT inhibitor, there are many, many better options than a local anaesthetic with some DAT-mediated side effects. A compound like this--if ab/used for psychostimulant purposes--just screams cardiotoxicity.

Personally, I would much rather have an amphetaminergic transporter substrate than a DAT inhibitor, but to each his own. If you want a DAT inhibitor, some of the cathinones that have limited substrate-like activity (e.g. ethylcathinone) would be a decent choice. The best choice for a non-tropane cocaine-like DAT inhibitor would be a desoxypipradrol compound: desoxypipradrol itself for extra long-lasting activity or methylphenidate for extra short action.
 
I've used it, and it's not bad. It really worries me that cocaine afficianados are going to start using this as a replacement. It is not. It's a unique stimulant that really has to be treated with respect if you don't want to overdose from it.

This is probably the closest thing to a cocaine replacement, at least in terms of effect and duration, that I've tried.

What I really hoped to see was an analogue minus the aromatic amine. AFAIK, this is metabolized into PABA or some close relative as well- which doesn't bode well for a large scale introduction. How many people know if they're allergic to PABA? Not many. And how many would know if they're pseudocholinesterase mutants? Probably even fewer.

I hope that serious warnings are issued along with the sale of this. It's kind of nice for occasional use, but that's it.

The only benefit I can see is that, like cocaine and procaine, it should have the local vasoconstricting properties which, is actually good for occasional intranasal use as it prevents a really rapid flood into the entire body, which should help to limit toxicity (the same way it helps reduce cocaine toxicity- though it's very damaging for long term use).
 
While I think that human use of this compound (as a stimulant) is a bad idea, the compound does interest me from a chemical perspective. By all structural logic, this shouldn't be a DAT inhibitor, at least certainly not one with a cocaine-like profile.
 
Has the ratio of monoamine reuptake been discussed here before? Is it even known? I have very little experience with cocaine, so my comment that it was similar should be taken with an Irit-sized grain of salt.

IIRC, though, in 3D this overlays with cocaine really well. I think amines are most distant at something like .7A, but I'd imagine that dimethocaine, being more flexible could fit into the same pocket quite well. Or maybe not.
 
You are dead right about the molecular overlay. I just did a comparative molecular field analysis of the energy-minimized conformations of both cocaine and dimethocaine--I am astounded how well the isosteric volumes of the two respective molecules correlate. If the board still supported attachments, I would post the rendered 3D picture of the overlay.
 
I just hosted it at imageshack.us

my.php


wtf why doesn't a .jpg show???

anyway, here's the link: dimethocaine on cocaine
 
Yep, I made an overlay, too and it looked quite similar to Hammilton's results. The similarity is astonishing.
Now think about the differences in both molecules:
- What serves the para-amino group for in dimethocaine (and some of the other local anaesthetics)?
- What's the effect of cocaine's methylester?

- Murphy
 
I think it's something like 1/4 as potent, half at most. Problem is that aneasthetic potency is equal. On paper as I recall, anyway. From using it, it's hard to say, I have little cocaine experience, and who knows how heavily it was stepped on. Considering that most of the cocaine out there has lidocaine added, this problem substantially more dangerous than street coke.
 
But, even if it is a quarter as potent, I've never had anywhere near pure cocaine, i'm sure. So probably 1/2 or 3/4 of the cocaine that I'm used to.
 
I did some more looking, and this is just as good as many of the cocaine analogues that are being pumped out with even less potency and same aneasthetic potency (or higher potency but equally higher aneasthetic potency).
 
Hammilton said:
I did some more looking, and this is just as good as many of the cocaine analogues that are being pumped out with even less potency and same anesthetic potency (or higher potency but equally higher anesthetic potency).
Click to expand...

I will find out soon how it compares to cocaine. Any ideas on ROA? I assume insuffulation would be safe and preferred due to its similarity to cocaine and it's local anesthetic properties.
 
This looks interesting, indeed...

I found sources (text! not mat :p ) saying it's about the same as potent as cocaine. But that was just found somewhere while quick-searching; no reliable sources of information i guess.

Anyway, i got a decent feeling that some more cocaine-like substances will appear on the "rc"-market in the next months/years. From a vendor's point of view that would be quite economic, as this might have a positive effect on the customer retention - for the vendors of course. ;)
 
i remember a thread awhile back where someone overlaid clofenciclan w/cocaine, with astonishing similarity

200px-Clofenciclan.svg.png


^my guess is that this guy wont have nearly as potent local anaesthetic effects (no ester or amide)
 
wungchow said:
i remember a thread awhile back where someone overlaid clofenciclan w/cocaine, with astonishing similarity

200px-Clofenciclan.svg.png


^my guess is that this guy wont have nearly as potent local anaesthetic effects (no ester or amide)
Click to expand...

Yeah, I did that. Clofenciclan and cocaine and dimethocaine all overlay very well in 3D.
 
You must log in or register to reply here.
Top