BTCP science and toxic effects

[vecktor]

Supposedly this material has appeared on the market, there appears to be a lack of even basic research literature search by those promoting this substance. this thread is for discussion of the science anything off topic will be deleted.

This on the face of it does not look good, especially for a dopaminergic drug which due to its very nature encourages repeat dosing.


Psychopharmacology (1999) 145:370–377

Toxic effects of BTCP
During initial studies, we began training a group of six
rats to discriminate 10 mg/kg BTCP from saline; however,
one animal died after approximately 50 training sessions
(approximately 20 BTCP injections spaced according
to the sequences listed in Methods) and a similar premorbid
state (excessive weight loss and abdominal tenderness)
was observed in the five remaining animals.
Necropsies were performed on all of the animals, and the
findings indicated that death and morbidity were associated
with gastrointestinal effects, such as adhesive peritonitis,
ileitis, and encapsulation of the liver. Histological
findings confirmed the existence of severe chronic peritonitis
associated with mesenteric lymphadenopathy. Although
we then began using a lower training dose in
drug-naive rats, it was observed subsequently that these
animals did not live as long after repeated administration
of the lower training dose as did rats used for other discriminations
in our laboratory.
Survival analysis using the number of sessions conducted
with rats trained to discriminate BTCP (5 mg/kg)
or cocaine (10 mg/kg) indicated that BTCP-trained rats
were used for a significantly smaller number of sessions
(C2=15, P<0.001) than cocaine-trained rats (204±42
days vs 403±65 days; BTCP vs cocaine, respectively).

occasional moderate use is probably harmless, I know several people who have taken it a few times up to 25mg without serious adverse effects, however the risk is with repeat dosing or longer term use.
The compound appears to exert hepatotoxicity, which is most likely attributable to the benzothiophene moety. which probably becomes oxidised to a S oxide, Similar compounds are known hepatotoxins and medicines with this property are used with liver function monitoring. see Zileuton http://en.wikipedia.org/wiki/Zileuton

 

[Jamshyd]

Thanks for posting this, and thanks for shedding light on the toxicity mechanism.

I guess we can assume, until further proof of safety, that this info would extend to substituted-BTCP analogues as well?

 

[fastandbulbous]

\Yep anything with the benzothiophene nucleus is going to be dodgy. I wonder what differences it would make to the pharmacology/toxicology if the aromatic sulphur (which after metabolism seens to be implicated in the hepatotoxicity) was replaced by an oxygen (benzofuran), a nitrogen (indole) or even justanother carbon (indan)

 

[vecktor]

\Yep anything with the benzothiophene nucleus is going to be dodgy. I wonder what differences it would make to the pharmacology/toxicology if the aromatic sulphur (which after metabolism seens to be implicated in the hepatotoxicity) was replaced by an oxygen (benzofuran), a nitrogen (indole) or even justanother carbon (indan)

2-substituted and 3 substituted benzofurans (substitution in the furan part) often show hepatotoxicity. In the case of furans it appears that hepatic metabolism opens the furan ring and creates a reactive metabolite. benzofurans substituted in the benzene ring but not in the furan are not associated with this problem.

 

[hamhurricane]

occasional moderate use is probably harmless, I know several people who have taken it a few times up to 25mg without serious adverse effects, however the risk is with repeat dosing or longer term use.
The compound appears to exert hepatotoxicity, which is most likely attributable to the benzothiophene moety. which probably becomes oxidised to a S oxide, Similar compounds are known hepatotoxins and medicines with this property are used with liver function monitoring

is 25mg a very high dose? it would certainly seem high given the potency of this material. BTCP is a DARI with an IC50 of 7 nM - compare that to MPH with an IC50 of 24 nM (although i find conflicting numbers) so it could be at least three times as potent and MPH has terrible oral bioavailability - as low as 11%. so if BTCP is highly available i could see the potency being in the league of 2DMP. from those that have tasted it are there any comments on the subjective effects, does it present signs of physical toxicity? there are analogs of BTCP which are even more potent, i would be interested in the indole analog.

EDIT: has the pyrrole analog of PCP been made?

 

[any major dude]

good info, thanks. definitely saved me a heap of searching. hopefully this one won't become terribly popular

 

[MurphyClox]

good info, thanks. definitely saved me a heap of searching. hopefully this one won't become terribly popular

Too late, I'm afraid. It's already offered to ridiculous low prices. This stuff WILL become popular and I'm convinced that we WILL see the casualties. Activity is said to emulate cocaine (no personal experience), altogether with the high addictive potential and some extra hepatoxicity for free.

Furthermore, if the purity of this stuff is like it used to be with other chinese custom synthesis, we can expect some related (and not necessarily more benign) sideproducts as contaminants. Yammi yammi!


It's just a sick development. I really hope that one day or another one of those faggot vendor dies of his own 'remedy'...

- Murphy

 

[any major dude]

i'm still not sure if the vendor offering with that description is actually a vendor. time will tell i suppose.

Also, would anyone care to speculate as to about what size doses the 5-10mg/kg in rats would equate to in humans? Seems like it might be a bit large for most people's recreational usage, but its obviously not a 1:1 comparison.

 

[vecktor]

people keep asking this for correcting animal mg/kg doses to human doses see the fda guidlines on initial human trials

http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm078932.pdf

rat to human is divide by 6.2

obviously YMMV

if you like your internal organs don't take this substance frequently do not binge on it etc blah blah just ignore me what the fuck do I know.

 

[any major dude]

thanks for that link vecktor, definitely useful info. I'm not really interested in taking this chemical myself, only in how much damage its going to do to others, and by proxy the rc community, availability of chemicals, etc.

I'm not sure what recreational doses of this would be, but it looks like one would start to experience hepatoxicity at around ~50mgs. my math could be off, but that seems like a pretty thin margin of safety before seeing toxic effects, especially with a dopaminergic drug. here's to hoping that vendor is full of bullshit

 

[ebola?]

It's just a sick development. I really hope that one day or another one of those faggot vendor dies of his own 'remedy'...

You do a disservice to "faggots", linking them to such vendors.

ebola

 

[MurphyClox]

^Oh, it was really just for the sake of expressing my disgust. No homophobia intended. - Murphy

 

[any major dude]

You do a disservice to "faggots", linking them to such vendors.

ebola

lol

So does anyone know anything else on this yet? cardiotoxic? potential for death or injury via other mechanisms? any novel characteristics or just another stimulant?

 

[vecktor]

lol

So does anyone know anything else on this yet? cardiotoxic? potential for death or injury via other mechanisms? any novel characteristics or just another stimulant?

a large amount of this substance dropped from a height can cause death through kinetic effects..
we know the metabolites in rats and a few other things about it

who knows what else it might do in humans, it is after all an UNresearched chemical.


there is some interesting pharmacology here because some experiments have found indications that the BTCP active site might not fully overlay the cocaine or mazindol site, which tells us more about the active sites on DAT.

 

[onmyway]

im curious as to what a low recreational dose would be.

what did the rat studies show about reinforcement? more or less than cocaine at similar doses?

there is more going on here than just hepatotoxicity. this looks like some extreme inflammatory process with the peritonitis and mesenteric node involvement. i wouldnt be surprised if this was carcinogenic.

i wonder what parenteral administration would look like.

 

[atara]

Too late, I'm afraid. It's already offered to ridiculous low prices. This stuff WILL become popular and I'm convinced that we WILL see the casualties. Activity is said to emulate cocaine (no personal experience), altogether with the high addictive potential and some extra hepatoxicity for free.

Emulating cocaine with no serotonin activity seems quite unlikely. If MDPV didn't cut it, why would this, and lacking norepinephrine besides?

It's just a sick development. I really hope that one day or another one of those faggot vendor dies of his own 'remedy'...

It's definitely not the first recreational drug to show hepatotoxicity, I can think of one that has a higher death toll every month than this will ever reach.