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amfonelic acid

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

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  • foxolinic.gif
    foxolinic.gif
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almost- said:
There must be some kind of SAR studies about amfonelic acid type of compounds?
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SAR is not some panacea, often SAR and QSAR do not work, it is often impossible to predict what the effect of a substance will be, or whether it will be more or less potent than another. If SAR worked then we wouldn't have HTS or combinatorial chemistry would we? big pharma would just have even bigger computers and much fewer researchers.

Do a search for rationally designed pharmaceuticals and you will find that very very few pharmaceuticals come from rational design based on SAR, the only one I can think of at the moment is ranitidine. Most blockbuster pharmaceuticals come from shot gun modification of existing substances, and pure serendipity, for example viagra. SAR is most often used backwards to identify structural features linked to side effects or adverse events in drugs that are already out there.

sorry to be the bearer of bad news.
V
 
Both of these interesting acids seem like great stimulants. Pity you cannot smoke them. I wonder, can you form an ester to lower the BP to allow smoking?
 
kidamnesiac said:
The HIV protease inhibitors were rationally designed...
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and so was ranitidine... however rational design has not lived up to the hype if rational design was so good then why are the pharma companies still running parallel and combi chem? all they would need is a big computer.
 
hey im 100% with you, i think computational methods are severely lacking in the bio- and chemical fields, but they are not useless. I do a little structural biology work and I trust the data derived from computational work about as far as I can spit a ferret.

If someone wanted an undergrad thesis project, it would be neat to do a computational approach to pihkal to see what results would manifest that are overlooked without a mathematical eye.

On the other hand, I interact with a lab doing real biochemistry on DNA methyltransferases and one of the classic big names in biochemistry, TC Bruice, has done some computational work to calculate the transition state and other parameters of the enzyme which has turned out to be almost 100% accurate.
 
kidamnesiac said:
hey im 100% with you, i think computational methods are severely lacking in the bio- and chemical fields, but they are not useless. I do a little structural biology work and I trust the data derived from computational work about as far as I can spit a ferret.

If someone wanted an undergrad thesis project, it would be neat to do a computational approach to pihkal to see what results would manifest that are overlooked without a mathematical eye.
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that is a great idea, there should be enough data points from pihkal and the rest of the literature, it might be very interesting and most likely more revealing than the hand waving descriptions of the receptor done up until now....:)
 
one would think nichols could find some goofy asian student to pull this off with at least one class of his compounds
 
^I should think some goofy BLer would be a)Easier to find & b)More likely to co-operate....
 
a. no way, why would they want to sit in front of a computer all day when they could be making, and subsequently obtaining *cough low yields cough*?
b. foreign grad students get the absolute shit jobs in academia and do whatever it takes to get that phd, or even BS.

this thread has gone on quite the tangent aye?
 
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