Lefetamine: Opioid, Amphetamine, NMDA Antagonist

[Paregoric Kid]

anyone have anything more to share on this really good looking drug?

Lefetamine, 1-dimethylamino-1,2-diphenylethane, SPA, Santenol
C16H19N

Lefetamine is a psychoactive drug which has effects similar to both morphine and methylphenidate. Due to its chemical structure, it binds to opioid receptors while simultaneously inhibiting reuptake of dopamine and norepinephrine. Lefetamine has the necessary tertiary amine functional group required for opioid receptor recognition, as well as a phenethylamine skeleton (which is responsible for its amphetamine-like effects). It has been marketed under the name Santenol.
http://upload.wikimedia.org/wikipedia/en/f/f3/Lefetamine1.gif

also I'm pretty sure I read somewhere it had some sort of antagonist effect at the NMDA site, though that may sound like it would turn it into a horrible drug like dxm or pcp realize that methadone and levorphanol antagonize the NMDA receptor. it's likely it only has weak action at the NMDA receptor like methadone and levorphanol, but I haven't seen any info on it's binding affinity.

it is only Schedule IV in the US CSA

[robojunkie]

I wonder which effect would "win out": More nod or more tweak?

It does break the morphine rule though, no quarternary center where it should be, but then again neither does fent. Do you know what it is actually marketed for? I know, I could look it up, but...no I think I will.

[Paregoric Kid]

well it is supposed to be about as potent as morphine in it's binding abilities I think and it's DA and NE reuptake is probably similar to ritalin maybe a bit more, I'll have to check the binding affinities. sounds to me like a pseudospeedball, just like taking morphine and ritalin or adderall at the same time.
amphetamines have analgesic value, in fact I've heard some mention it to provide almost mg:mg (d-amp:morphine) analgesia. though I doubt that statement. but it is true that stimulants can provide analgesia and that may make sense, opioids cause dopamine release. it has also been shown that amphetamines can enhance the analgesic effects of opioids.

so it should provide more pain relief than just an opiate or just a stimulant. also it would likely prevent unwanted drowsiness in patients. they give a lot of chronic pain patients a script for ritalin if they're becoming too drowsy from their opioid medication. then there is the NMDA antagonism which likely potentiates the opioid properties, may prevent or slow development of tolerance, and also helps with neuropathic pain. this could be a huge benefit for some people, 3 effects in one pill, likely a lot cheaper buying one pill than spending money on 2 or 3 medications.

*Amphetamine and Analgesia http://www.doctordeluca.com/Library/Pain/Pain-Amphetamines.htm
The Independent Drug Monitoring Unit (I.D.M.U. LTD) is an independent research consultancy conducting original research, including large-scale surveys of drug users, and providing expert evidence to the courts in criminal cases involving controlled drugs.
British National Formulary 35 (March 1998) p186

[robojunkie]

Yeah that makes sense about the drowsiness side effect in some pain patients. I tried looking it up just to see what the company (some Italian pharm that I couldn't find, even with the name) or the FDA or equiv. approved it for (Schedule IV?) but I couldn't find anything but a few abuse studies from Italy and Japan and a whole crapload of drug scheduling/legal crap. I wonder if its approved for anything in the US. I'll have to look it up tomorrow on the uni/research search engines. It would definitely be interesting to compare it to the parallel combination of opiate/stimulant. That would seem like really good luck (or design) if the effects were essentially equivalent in intensity to an actual psuedo-speedball in the right ratios. I think the IC50's would have to perfectly line up for both receptor type activation for the effects to be "even" and not more opiate or more stimulant. Love to find out though.

[jacky]

yeah, that sounds like a great compound there....probably not much in the recreational sense alone, but most likely a great combo option.

anyone know about synth. routes on this compound? anyone that knows about chemistry?

very interesting.
it is schedule 4 in canada. doesnt seem to be OTC there though.

probably some old timers out there that hate the stuff, but love to talk about it maybe?

put that on my list of things to do.