Thiorphan

[Paregoric Kid]

has anyone heard of thiorphan? it has been used to treat diarrhea I believe. its pretty interesting, it is a beta-enkephalinase inhibitor which means it inhibits the breakdown/reuptake of enkephalin an endogenous opioid. it works kind of in the way an SSRI works but instead of working on serotonin it works on enkephalin. anyone have any info on this?

[Hoss]

I have not personally heard of Thiorphan before, nor am I well vexed in chemistry, however, a leap over to Wikipedia turned up this chemical structure that perhaps one of our resident molecule minds could decipher.

http://upload.wikimedia.org/wikipedia/commons/thumb/f/fa/Thiorphan.png/200px-Thiorphan.png

[Indy]

Apparently (not sure if this is true, got it off the net) it can actually ease naloxone induced precipitated withdrawal, and potentiates morphine. The fact that it can help precip. withdrawals is very intriguing, since normally no amount of dope helps that (only time)

[jacky]

finally....
a reuptake inhibitor that I could actually see myself giving a fuck about.

some dopamine reuptake inhibitors are ok....recently I bioassayed one that people were claiming works better than cocaine.
I tried a decent dose of this amfonelic acid...or similiar spelling. it was somewhat potent...but far less interesting than even the mundane cocaine molecule.

mesembrane/mesembrine are interesting reuptake inhibitors.

this stuff sound interesting.
thanks pgkid!

[Paregoric Kid]

its also been shown in studies to potentiate the pain killing effects of THC.
damn why is the whole world oblivious to the possibility that depression could be opioidergic in nature? its like they don't want to investigate the possibility or are afraid of what they might find. who knows, guess it means we'll have to take things into our own hands and do the research ourselves.

[The Paregoric Man]

damn why is the whole world oblivious to the possibility that depression could be opioidergic in nature?

Its two things really, number one is the uncomfortable truth thing, number two is pharm companies have a lot of profit invested in the SSRI model they are not prepared to let go of.

[DCBA]

where can one find this ? not schedule anywhere in the world isnt it?
This could work as a lift for opiates as well..

[Paregoric Kid]

if you google around you can find thiorphan from some suppliers who sell peptides and amino acids. not trying to give out sources, even though this is completely legal, but I am curious what the lowest price can be found. if anyone goes price shopping report back to us on what prices you find.

Thiorphan (DL) http://www.biomol.com/Biomol2/images/wht.gif http://www.biomol.com/Biomol2/images/wht.gif DL-3-Mercapto-2-benzylpropanoylglycine
97%, MW=253.3 [76721-89-6] Storage: -20°C
Inhibits the metalloprotease neprilysin (neutral endopeptidase 24.11) and neprilysin 21. Inhibits opioid-degrading enzymes, potentiating THC-induced antinociception2. Potentiates the effects of natriuretic peptides3. Blocks enzymatic degradation of luteinizing hormone releasing hormone (LHRH)4.

[Shadowsblaze]

I'm not sure but I think I would like to know what all this means. In case I'm missing out on something good. Thiorphan, sound like a super hero. Later, up up and away.

[jacky]

its something to approach with much MUCH caution.

and I wouldnt encourage anyone to take the plunge. but it is an interesting subject.

[ryan]

Cool stuff, will have to check out some of my suppliers.
I am always up for a little research =]

[OxiContinKing]

5mgs for 90 bucks.

[DCBA]

5mgs for 90 bucks.

In my country its sold as a medication, it costs about 6 euros for 600mgs.

Has anyone tried this already? I'm on MMT and i think wouldn't feel a thing and also would agravate my constipation.. But i may try it when i get off methadone or in the latest stages of tapering the methadone.


its something to approach with much MUCH caution.

and I wouldnt encourage anyone to take the plunge. but it is an interesting subject.
Yeah....
But.. Also.. Its sold for children in this country.

[Paregoric Kid]

recently I've read that thiorphan doesn't cross the BBB very well so it gives primarily peripheral effects, thats why its used like immodium. however, acetylated thiorphan, called acetorphan, crosses the BBB when injected (and probably when taken intranasal, sublingual, and plugged too) and produces analgesia and other effects in the CNS. acetorphan is sold in some places OTC like thiorphan.