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The Big and Bangin' Pseudo-Advanced Drug Chemistry, Pharmacology and More Thread, V.2

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Bloody hell. I'm shocked to just see the phenetylamine skeleton in Phenylpiracetam.

Anybody want's to speculate on what that means for it's SAR?

piracetam:
150px-Piracetam.svg.png


Phenylpiracetam:
200px-Phenylpiracetam.svg.png
 
That's really a great lot of bulk on the nitrogen for one to expect activities related to phenethylamine SAR.

ebola
Yes, of cause, I see what you mean. But how is it metabolized? What parts come off in the body? If you remove the amide part it starts looking a bit like aminorex.

Anyway, just thought it was a funny coincedence, did't think it would have any real bearing on it's effects. Or it would propably have been known already.

imo it also bares a striking resemblance to Placebomine

Phenylpiracetam is actually supposed to be one of the racetams that really work. Stimulation from just one dose is supposed to be on par with a cup of coffe, just different obvisously.

I'm about to find out.
 
Yes, of cause, I see what you mean. But how is it metabolized? What parts come off in the body? If you remove the amide part it starts looking a bit like aminorex.

Yeah, I think it is metabolized the same way as piracetam, which ends up 2-(2-oxopyrrolidin-1-yl) acetic acid.

You end up with this funky-ass molecule:
(2-oxo-4-phenylpyrrolidin-1-yl)acetic acid
imagefly.cgi


...and what does Pubchem have to say about it?

High throughput screening has shown it doesn't kill a few scary types of bacteria.

Thanks, Obama! =D

Yet it seems like every supplier under the sun offers it, and has no idea what it does. I'm guessing none of them actually have it on hand, and no one ever orders it.

Anyway, just thought it was a funny coincedence, did't think it would have any real bearing on it's effects. Or it would propably have been known already.

Definitely don't jump to conclusions like that with the racetams! In my opinion they as interesting a class as phenethylamines and tryptamines (albeit mostly in different ways), but horribly under-researched. You look through pubchem and see the occasional assay here and there, and almost nothing on SARs or finding new derivatives. It's almost like some kind of conspiracy to keep smart drugs under wraps 8o I'm only half kidding

There are even only a few papers on phenylpiracetam, and afaik none exploring potential derivatives despite showing pretty amazing effects in clinical trials. I'd love to see what happens when you start substituting on the phenyl ring.

Really the only two racetams that have been heavily researched are Piracetam and Keppra, and we still barely have any idea how the fuck they work. Heck, Keppra is still the only known drug to target SV2A. And there are some really interesting ones out there, like Coluracetam... another first in class drug as a high-affinity choline uptake enhancer now in clinical trials that I'm also a big fan of.

Phenylpiracetam is actually supposed to be one of the racetams that really work. Stimulation from just one dose is supposed to be on par with a cup of coffe, just different obvisously.

I'm about to find out.

Yeah, it's pretty stimulating. I'd compare it more to dexedrine than coffee, it won't get you jittery. Most people claiming racetams don't work are expecting to notice some change in perception, and phenylpiracetam+oxiracetam+coluracetam are really the only ones that do that to any real degree, the former two as stimulants and the latter as a very, very weak psychedelic (just color enhancement, I wonder if that's why the named it). The stimulation on phenylpiracetam is pretty unlike anything else I've tried in the stimulant world, its very smooth and slightly euphoric, gives a big increase in heat/cold+exercise tolerance (why its banned in competition) despite being weakly adrenergic at most, increases cognitive tempo and reasoning abilities a lot, and has modest improvements in both short and long term memory retention. I'd compare it to dexedrine but it's less euphoric, less focusing and far more pro-cognitive. I'd compare it to 2-FMA, but it's more euphoric and pro-cognitive, but less adrenergic and far less focusing. I'd compare it to Armodafinil, but it's far more effective at enhancing physical performance and less wake-promoting+focusing.

Yeah, it's basically just... phenylpiracetam.

The only downside is tolerance builds pretty fast, I have to cycle 3 days on and 5 off to return to baseline. The wikipedia article on it is a good summery of all the known info on it.

Racetams, Y U NO RESEARCHED BETTER!? :!

Edit:
In Soviet Russia, Carphedon research you! =D
 
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Alright so my rant on lack of racetam research got me thinking... how does one get into computational modeling of drug-receptor binding?

Anyone care to point me in the right direction?

I've got access to some fairly high end GPU hardware and a decent background in computer science, by the way.
 
Alright so my rant on lack of racetam research got me thinking... how does one get into computational modeling of drug-receptor binding?

Anyone care to point me in the right direction?

I've got access to some fairly high end GPU hardware and a decent background in computer science, by the way.

Check out ISIS Draw for drawing molecules, Accelerys DS Visualiser to slam them into proteins, and RCSB.org to get receptor model files.
 
Substrates and concentration/metabolism

Hi, I posted this in BDD, but I wasn't sure where it belonged, so I suppose I will post it here as well.

I have a question about substrates. If two substrates which are acted upon by the same enzyme are coadministered, (regardless of whether either inhibits or induces that enzyme), what is the effect on the rate of metabolism of those two substrates (substances)? I would assume they would "compete" for the enzyme's attention -- thus possibly causing a raised available concentration of each substance for a shorter amount of time. I am not sure if I got the mechanism reversed, though. Would it be the opposite? Would it make no difference? Could someone help out? I was prescribed new meds and just want to be extra cautious.
 
toastman said:

This compound looks pretty similar to apomorphine, morso than it does to bromocriptine, lsd, or any other known ergoloid, so standard SAR for well known DA agonists applies here.

ebola
 
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SoulSpark said:
I would assume they would "compete" for the enzyme's attention

This is true under conditions where the enzyme is saturated or near-saturated by available substrates. Under conditions where the enzyme is opulent, the presence of one substrate won't have much of an effect on metabolism of the other.

ebola
 
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@Soulspark: If you administer two compounds that compete for the same enzyme, the rate of metabolism of both compounds is slowed down. This effect is stronger if the amount of enzyme is the rate-limiting variable in the metabolism. This is called competitive inhibition.

For example, alcohols are metabolized to the corresponding aldehydes by the enzyme alcohol dehydrogenase. Ethyl alcohol is typically ingested recreationally in amounts that are sufficient to saturate the enzyme and it is eliminated with constant rate instead of having a half-life. Here the amount of enzyme is the rate-limiting variable.

Methanol is also oxidized by alcohol dehydrogenase, but the product of this reaction is formaldehyde, which is toxic and causes damage to the optical nerve, resulting in blindness.

If methanol and ethanol are administered at the same time, ethanol is better at competing for the ADH enzyme. Therefore, if someone goes to the ER with methanol poisoning, they are treated by giving ethanol regularly around the clock, maintaining a BAC of about 0.15 for a couple of days. Because the competitive inhibition, methanol is then not oxidized to toxic formaldehyde, but is instead slowly excreted in the urine and exhaled air. This is an example of a practical application of competitive inhibition.
 
^I have a friend who accidentally ingested antifreeze whilst very drunk, and was hospitalised. The doctors said that, without so much ethanol in his body, he would most likely have been killed.
 
Are there any books specifically dedicated to pharmakonetics and pharmacology that were written/compiled for the education of a novice in the field. I of course can always go look through my organic chem text books from college but I'd like to have some literature that focuses directly on the subject in question instead.
If you guys could compile a list of books I could buy instead of looking into online databases I would greatly appreciate it.
 
Are there any books specifically dedicated to pharmakonetics and pharmacology that were written/compiled for the education of a novice in the field. I of course can always go look through my organic chem text books from college but I'd like to have some literature that focuses directly on the subject in question instead.
If you guys could compile a list of books I could buy instead of looking into online databases I would greatly appreciate it.

Every pharmacology text book I've ever come across expects a basic knowledge of molecular biology and human physiology at least, and usually some chemistry as well. There might be some great resource out there exactly at your level, but I would suggest picking up some books on molecular biology and human physiology first. Everything you learn will be much more meaningful if you have the right foundation to build on.

edit: You are aware of the Erowid/BlueLight Neuropharmacology Text no? That might be around the level you're looking for.
 
Are there any books specifically dedicated to pharmakonetics and pharmacology that were written/compiled for the education of a novice in the field. I of course can always go look through my organic chem text books from college but I'd like to have some literature that focuses directly on the subject in question instead.
If you guys could compile a list of books I could buy instead of looking into online databases I would greatly appreciate it.

Best intro pharmacology book IMHO is Rang and Dales "Pharmacology", and older copies are easy to find online/college book stores. Be warned, you need a basic understanding of cellular biology and chemistry to make sense of a lot of it. However, it does a decent job explaining most of the broader points in those topics.
 
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