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anhalonium9
13-05-2006, 08:37
http://www.talkaboutdrugsnetwork.com/group/alt.drugs/messages/473472.html

anyone know anything more about this stuff? anyone ever tried it?

BilZ0r
13-05-2006, 09:09
It just looks like another research grade dopamine reuptake inhibitor, here's a big ole list of them

http://www.tocris.com/catalogue.php?Type=Pharm&ItemId=5007

Smyth
13-05-2006, 09:33
I remember C6H6 specifically mentioning this compound about a year ago.

Other than that ive never heard any mention of it.

anhalonium9
13-05-2006, 10:00
It just looks like another research grade dopamine reuptake inhibitor

actually, the reason i was asking is cuz i've heard limited reports of ppl using it recreationally....

fastandbulbous
13-05-2006, 23:36
Reuptake inhibitor, almost zero peripheral effects, very euphoric effect; basically if it wasn't such a complex synthesis this would def be a serious drug of abuse (pretty much in the same group as fencamfamine in terms of effects etc).

It's one of those compounds, along with fencamfamine, that if I had access to I'd never even consider crude drugs like amphetamines again!

EN21
15-05-2006, 17:20
The structure reminds me very, very much of gyrase inhibitors such as enoxycin or ciproflixacin. I am pretty sure amfonelic acid was originally synthesized as an antibiotic compound.
-weird!

vecktor
16-05-2006, 17:49
its the benzyl analogue of nalidixic acid and synthed the same way. part of a huge family of napthoquinones of which cipro is just one, I think they all inhibit bacterial topioisomerase. there are concerns regarding carcinogenicity of some and photosensitisation and other side effect for others, apparently many of these antibiotics cause CNS disturbances in some cases though this is probably through a different mechanism to DA reuptake inhibition.
-v

fastandbulbous
17-05-2006, 01:16
^ Is it a similar mechanism in play with chlorethromycin? It's just on the list of side effects, when it was prescribed for my wife, was 'psychotic episodes possibly leading to hospitalization'! It was also fairly high up in the list indicating that it wasn't a really rare side effect.

vecktor
17-05-2006, 02:33
I think the cns side effects of the napthoquinones are something to do with their affinity for GABA receptors. they are also quite good chelators, so could interfere with ion concentrations.
I would be suprised if the clorethromycin, which i assume is some chloro derivative of the macrolide anti biotic erythromycin causes side effects through the same mechanism.
v

Refluxer
07-09-2006, 00:21
What's is the approximate dosage, how long does it last, hard crash, etc?

Dr.Heckyll
17-09-2006, 19:00
I had a chance to try it. It's a very nice stimulant at 25mg orally. Mentally clean and no body effect. Comes on quickly and doesn't last too long, maybe 4 - 6 hours. Excellent!

nanobrain
18-09-2006, 02:01
^i smell benzene

Helios.
18-09-2006, 02:10
^ever smelled the R subunit of phenylalanine, one of the 20 naturally occurring amino acids?

Refluxer
18-09-2006, 16:18
Mmmm, sounds fantastic. Too bad the structure isn't exactly the frendliest.

Helios.
18-09-2006, 20:31
that's what pharmaceutical companies are for

Dr.Heckyll
18-09-2006, 21:10
There's a related compound, Foxolinic Acid, which is about 4 times as potent as Amfonelic acid, and I've heard that some people are working on bringning that out on the market. That will be the end of MDPV i guess...

Dr.Heckyll
18-09-2006, 22:08
Helios: The benzyl of Amfonelic acid is replaced with a phenoxy group.
(Can't reply to PM until I'm a Bluelighter :( )

specialrelativity
18-09-2006, 22:17
Dangerous? Toxic? Don't get into world poltics.

p.s. Don't try to tell this to the Europeans:)

Helios.
18-09-2006, 22:49
I remain skeptical about this class of compounds as well.

vecktor
19-09-2006, 01:25
There's a related compound, Foxolinic Acid, which is about 4 times as potent as Amfonelic acid, and I've heard that some people are working on bringning that out on the market. That will be the end of MDPV i guess...

the compound you name foxolinic acid, 1-ethyl-1,4-dihydro-7-phenoxy-1,8 napthyridine-3-carboxylic acid is approximately 10 less potent than the 7 benzyl cpd. Source: sterling drug company.

foxolinic acid as a name has echoes of oxolinic acid a very useful methylenedioxy containing antibiotic. Can we not use potentially confusing nomenclature?

As afa or one of its analogs have great potential as treatment in dementia and other neurodegenerative disease, I for one would be pissed if it appeared on the rc market
V

Dr.Heckyll
19-09-2006, 19:10
Do you have a reference for this?

vecktor
19-09-2006, 20:49
Do you have a reference for this?


Substance is described by George Lesher (discoverer of nalidixic acid)in US pat 3 590 036

jah
30-01-2007, 22:58
Has anyone else tried Amfonelic acid?I'v read the attachment that anhalonium9 offered , one guy had gone on a 10 day binge and said he preffered it over nomifensine,(wish i new why?). He said ," AFA made methamphetamine look like caffiene" those are some powerfull words!
Anyone know if AFA, can have those affects?Dr.heckyll was the only one to have any experiance with this one first handed.
If this guy(not Dr.Heckyl) is telling the truth, i would think more people would be familiar with it!!!!

haribo1
30-01-2007, 23:05
http://www.pennbio.com/IMAGES/Image405.gif

This looks like a pain to make, to me. But that's just me...

jah
30-01-2007, 23:20
Yes it does, F&B and Dr.Heckyll both had really good things to say about it. Maybe this guy wasn't to far off the mark!!!


Thanks.

Jamshyd
30-01-2007, 23:22
^ That DOES look ugly. It reminds me a bit of a NSAID, I just can't remember which one for the life of me.

haribo1
30-01-2007, 23:30
Now you say that, it sort of does. I don't think it's ugly per-se, just a pain. Actually, the ugliest molecule, to me, is heroin. Looks like a scorpion with the 2 acetyl groups as pincers & the piperidine ring as the sting in the tail.

http://www.farmakologija.com/materia/images/heroin.gif

It's like a magic-eye picture... can you see it?

Jamshyd
30-01-2007, 23:51
LOL.

I always thought of the Heroin molecule as someone pictured from above reaching out for a hug ;)

But now that you mention it, yes it does seem like a scorpion!!

A general organic chem blonde question: How difficult is it in general to nitrogenate an aromatic ring?

Btw, I just remembered which NSAID it reminded me of: Naproxen. No, it actually only looks vaguely close. But that brought on my question, actually.

phase_dancer
31-01-2007, 00:38
A general organic chem blonde question: How difficult is it in general to nitrogenate an aromatic ring?

Basically aromatic + HNO3/H2SO4, although if other ring substitutes are present, depending upon whether they are activating or deactivating, the Nitro group will either be directed to para/ ortho or meta positions.

vecktor
31-01-2007, 00:51
Basically aromatic + HNO3/H2SO4, although if other ring substitutes are present, depending upon whether they are activating or deactivating, the Nitro group will either be directed to para/ ortho or meta positions.
I suspect that what he is asking is whether nitrogen can be inserted into the benzene ring as part of the ring... benzene to pyridine, or naphthaline to quinoline, which is what is required to convert the NSAI into AFA. this is essentially impossible.

fastandbulbous
31-01-2007, 03:01
Yes it does, F&B and Dr.Heckyll both had really good things to say about it. Maybe this guy wasn't to far off the mark!!!


Thanks.

I was going off a report that a friend sent me about AFA, I've not got the experience needed with it myself - one off doses can;t really be used to give a picture of its activity - several doses of differing sizes spaced by at least several days are required for a full assessment of a compound, especially ones that exhibit next to no body load (I have extensive experience with all manner of stimulants, but accurately assessing the potential of desoxypipradrol, which has almost no physical impact is proving to be a lot more difficult than with a stimulant with some physical aspect, such as MDPV). If anyone else has experience with AFA (5+ doses), we'd all like to hear about it (don't think there'll be too many as it's bloody expensive).



The structure reminds me very, very much of gyrase inhibitors such as enoxycin or ciproflixacin. I am pretty sure amfonelic acid was originally synthesized as an antibiotic compound.

That's the one thing that really worries me about AFA - if it has significant antibiotic activity, repeated, irregular use could lead to development of very nasty strains of normal body flora, the ones to really worry about being the opportune pathogens (like Staph. aureus) or could sizably upset the gut's normal flora leading to all manner of digestive tract problems.

Problems of the sort outlined above can lead to life threatening conditions, which is why I'd much rather persue less exotic stimulants (like desoxypipradrol, which has a similar activity profile other than it last quite a long time 10+ from a 5mg dose), but if anyone else is fearless and wants to report back, I wish them good luck and await experience reports

mad_scientist
01-02-2007, 00:47
That's the one thing that really worries me about AFA - if it has significant antibiotic activity, repeated, irregular use could lead to development of very nasty strains of normal body flora, the ones to really worry about being the opportune pathogens (like Staph. aureus) or could sizably upset the gut's normal flora leading to all manner of digestive tract problems.


Ok im not an expert in antibiotic resistant bacteria, but surely theres nothing about becoming antibiotic resistant that actually causes bacteria to become more pathogenic in their own right? I thought it just means that its harder to treat infections because the drugs don't work.

If a person was taking amfonelic acid then sure any bacteria in their body may become resistent to amfonelic acid, and probably to nalidixic acid as well, but neither of those are commonly used as antibiotics. How broad is drug resistance, AFA wouldn't make them become resistant to say amoxycillin or vancomycin would it?

I think oppotune pathogens would be more of a concern, taking AFA orally might kill off your normal gut flora and make you more prone to intestinal infections the same way how people who use too much antibacterial soap can get skin infections. But the normal doses for antibiotics are hundreds of milligrams, taking 20mg of AFA shouldn't be enough to cause genocide throughout your bowels...

Correct me if im wrong though, microbiology isn't really my field. But im not sure that the antibiotic effects of AFA would be that significant if a stimulant dose is 1/10 or less of an antibiotic dose.

Refluxer
01-02-2007, 18:13
...but if someone develops a habit and steps up the doses, it could go way wrong. I remember getting mild, temporary edema in my dick in conjunction with drugs/supplements once. It made me think once again on the risk to seriously fuck yourself up with unresearched substances (and researched ones of course).

vecktor
01-02-2007, 18:30
quinolone antibiotic resistance would also apply to cipro and other useful antibiotics in the same class.

fastandbulbous
02-02-2007, 02:50
Any of the above two happening, then say you receive an injury to your nose that leaves wounds in mucous membranes, like getting accidentally whacked in the face due to lots of people being rat-arsed on beer/alcohol (40% of the UK population have Staph aureus as normal flora of the upper respiratory tract) then all it needs is for one of those antibiotic resistant strains to be an opportune pathogen like S. aureus and you can end up with all sorts if trouble due to the time it takes to find an antibiotic that is effective.

You only have to see what MRSA can do to people to see that a drug of abuse with the capacity to induce preferential development of antibiotic resistant strains could turn out to be a monumental problem

Dr.Heckyll
07-08-2007, 17:23
There's a related compound, Foxolinic Acid, which is about 4 times as potent as Amfonelic acid, and I've heard that some people are working on bringning that out on the market. That will be the end of MDPV i guess...
In the meantime I had the opportunity to try foxolinic acid. It's a powerful and long lasting (~24h) stimulant at a dose of 5mg in some people, while others show little response to it. Like with AFA, there's no body lead at all, but AFA is more euphorigenic, lasts shorter and is more reliable. AFA is clearly the better choice. AFA is the absolutely best stimulant I've ever had, and I've had quite a few. Compared to AFA, MDPV is just shit which you wouldn't touch again if you had the choice. source discussion removed

PS: According to http://discovery.mdsps.com/Catalog/Services/Profiling/Assays/AssayDetails.aspx?id=316000 AFA has the extraordinarily low IC50 of 0.45 nM for dopamine reuptake inhibition.

Jamshyd
08-08-2007, 00:26
^ MDPV is shit compared to anything ;)

Btw, I find all those new, potent, extremely long-lasting stims to be something of a concern.

AnewMan
08-08-2007, 06:38
^^ It is something to be concerned about, but if it is as good as they say perhaps it will win out on every major anti depressant, slaying modafanil and laziness all at once.

I don't really like the idea of 24 + hours of stimulation though. I'm trying to grow, I don't think it will be possible jacked.

Either way I wouldn't even recreationally test this without some no-go pills.

realm
08-08-2007, 07:20
ok im sorry this is way off topic but....

how did u guys get so into drugs? this is insanity lol

hussness
08-08-2007, 22:39
Well for me, I was always insane and have struggled with major depression my whole life, and when I was twelve I read a NIDA pamphlet about how bad drugs are for you, mkay? That's what got me started and the rest is history... ;)

fastandbulbous
09-08-2007, 01:47
how did u guys get so into drugs? this is insanity lol

Had a near death experience when 13 and that triggered an interest in such states. Eventually I'd read about LSD etc and when I got to uni I actually got to try it. After half a decade of studying pharmacology, pharmacokinetics etc (and eating various psychedelics) I realized that my main interest lay in this field, both academic & practical (ie self experimentation!).

As said above, the rest is history

syntelman
26-08-2007, 15:17
This may drift slightly off-topic... but it would be very interesting to hear more about the effects and duration of foxolinic acid (as well as with AFA). :)

LuxEtVeritas
26-08-2007, 19:52
There is also a study that seems to indicate AFA has pronounced efect on 5HT and also one that note an absence of effect on NA:

The effects of amfonelic acid on 5-HT metabolism in rat brain.

Amfonelic acid, a non-amphetamine stimulant, has marked effects on brain dopamine metabolism but not noradrenaline metabolism: association with differences in neuronal storage systems.


Also this seems kind of interesting and is an attribute shared with cocaine:

Support for this interpretation was
provided by the demonstration that one of these psychostimulants,
amfonelic acid, can restore dopamine release after depletion
of newly synthesized dopamine with -methyl-p-tyrosine
(MPT) (Ewing et al., 1983). Although these findings were intriguing,
they were unable to elucidate cellular or molecular substrates
for this postulated cocaine-sensitive storage pool.

and from a separate study:

Administration of alpha-methyl-p-tyrosine terminates the release of dopamine, although tissue stores of dopamine are still present. Thus there appears to be a compartment for dopamine storage that is not available for immediate release. This compartment appears to be mobilized by amfonelic acid, since administration of this agent after alpha-methyl-p-tyrosine returns the concentration of dopamine released by electrical stimulation to 75 percent of the original amount.

Gaian Planes
12-09-2007, 19:32
in regards foxolinic acid, is it stabile in solution long-term for accurate measurements or would it degrade\

syntelman
13-09-2007, 16:00
foxolinic acid is bad for your karma man...
;)

Xorkoth
13-09-2007, 17:19
All this talk of novel stimulants is giving me a headache...

hussness
13-09-2007, 20:40
Do you know whether the headache had any relation to the serotonin effefcts of the drug?

almost-
14-09-2007, 18:30
What's the structure of foxolinic acid? Any pic?

MattPsy
15-09-2007, 00:56
Here is the structure, i've attached it...

Amfonelic acid by comparison has the phenoxy group on the left replaced with a benzyl group... pretty much just a CH2 in place of the O.

almost-
16-09-2007, 23:44
There must be some kind of SAR studies about amfonelic acid type of compounds?