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Just a quickie about lefetamine

You have likely seen this before but...

Thirty-nine methadone maintenance patients were included in a 9-day, double blind, randomized, inpatient detoxification trial. Methadone was tapered to 10 mg/day and then patients were assigned to one of these 3 protocols: clonidine (0.3-0.9 mg/day), lefetamine (60-240 mg/day), buprenorphine (0.15-0.9 mg/day). Buprenorphine treatment was significantly superior to clonidine and to lefetamine (F = 3.96 df = 2, 29 P < 0.05) in controlling objective, subjective and psychological withdrawal symptomatology. Clonidine was more effective than lefetamine in suppressing withdrawal in the first 3 days of treatment (day 3: F = 4.10 df = 2, 30 P < 0.05), and this trend was apparent on the objective and psychological items. In addition to evaluations of the efficacy of the single drugs used, the study showed that tapering methadone to low doses before entering the pharmacologically assisted discontinuation phase was clinically acceptable in detoxification from long-term methadone treatment.
http://www.ncbi.nlm.nih.gov/pubmed/7851281
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You sir, are an absolute star (I'd 'read' that article but must have skipped over that bit, possibly when one of the cats knocked over a pan in the kitchen!).

It's just that I have my grubby paws on some & wanted to verify the 50-100mg dose range for it before poisoning myself ;)
 
Since lefetamine is only one isomer, is it less of an nmda antagonist than the racemate? I say this because in other non-human studies, desglycinyl-remacemide was comparable in potency to ketamine if I remember correctly.
 
(zonk) said:
Since lefetamine is only one isomer, is it less of an nmda antagonist than the racemate? I say this because in other non-human studies, desglycinyl-remacemide was comparable in potency to ketamine if I remember correctly.
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It is the racaemate (I should have just called it N,N-dimethyl-1,2-diphenylethylamine), so here's hoping...

(I think this might be worthy of a trip report even if it's a bit of a disappointment)
 
yes defintaly! and even if it not all that and the bag of chips it's been sort of hyped up to be(in the 50-100mg that you're planning on), I wouldn't discount it, ....If it doesn't do much at doses upto .5g then that will be the final word if I was the guinneapig
 
I'd be very interested in knowing how the racemate compares to the pure isomer in terms of dosing and effects as well.
 
DOOOO EEEET!

The fact that it proved very popular in the short period it existed in Japan and Italy tells me that it won't be a disappointment.

And empty your inbox while you're at it :p
 
well I don't think these compounds will provide any decent amount of nmda antagonism as desglycinyl-remacemide is less active than dxm according to this... http://linkinghub.elsevier.com/retrieve/pii/S0014299996007303 The rank order of potency, MK-801>ARL 16247AA>PCP=dextrorphan>PCA≥ketamine≥ memantine>dextromethorphan>desglycinyl remacemide>ADCI>ARL 15896AR
I don't know what specifically this is reffering to as I do not have access to the artical, however interesting enough replacing the amine with piperidine increases the nmda antagonism. But the is only one way to find out I guess...
 
does anyone have the original synthesis papers from 1960 in the journal pharm. society japan? First author Oigu I think. Is it even in english?
if you could pm me that'd be great.

ps-first impressions: more DRI than opiate.
 
yea, definitely a dissapointment. lots of peripheral stimulation and no focus improving abilities. The tail flick test definitely shows analgesia, but no euphoria. the rats consumed ~1mg/kg of the racemate in two doses spaced 1.5 hrs apart.
There is good reason for thinking that the S isomer is not going to have the opiate effex, as Sasaki et al J. Med Chem 1966 show that the R has an eclipsed geometry that is proposed to be important in stereoselectivity for the opiate receptors.
Interestingly, the Merck has it listed as controlled as a stimulant but having therapeutic value as a analgesic.
the wet dreams can end now :(
 
the wet dreams can end now

we'll still see a thread started on it i am sure not too long from now 8) :\ =D ;)

i always thought this would be a loser...
 
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