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

[endotropic]

Hi, can anyone recommend a sort of "for dummies" text on neuropharmacology? I'd like to have a better understanding of the basics ie neurotransmitters etc

Have you found the Erowid/BlueLight Neuropharmacology Text? Depending on the balance of thorough/simple you're looking for that could help you get your foot in the door. Most texts published on neuropharmacology these days assume you have a basic understanding of neuroscience, molecular biology and physiology before you open them.

 

[Jabberwocky]

^damn i hadn't seen that, thnx
[edit: LOL that's too funny:

If you "don't know what enzymes has to do with the neuropharmacology", then it's probably best if you don't write the section specifically dealing with that question.

poor bliz0r setting that up lol]

puzzled- instead of a specific, i'll just say that if you search on bluelight in this subforum (and its archives. they may be called ADD still), and on reddit (subreddits r/drugs and r/drugnerds), you'll find many threads of the same question as yours, w/ many many answers

 

[DL-ark]

Any chance some of Leonurine's activity is through dopamine reuptake a la dimethocaine? Their structures are fairly similar but Leonurine has an extra carbon in between the ester and the nitrogen. I have really found some good effects with an unknown species of leonotus. I find boiling the flowers/large quantity of leaves in a small amount of water, and taking small 5ml doses of this water leaves me with a moderate euphoria which lasts anywhere from 3-5 hours. Interestingly higher doses result in a longer duration with only slightly stronger subjective effects.

Leonotus does not feel that stimulating, but I really would like to discover the pharmacology of this plant. Of course, I think I first need to determine what species I have in my possession, as it looks vastly different from the ornamental dagga plants that people grow.

http://www.bluelight.org/vb/threads...(Dagga-alkaloid)-adenosine-reuptake-inhibitor

This analysis of leonurine seems sound, but I would like to point out that the chemical structure on the wikipedia page is different from the actual chemical. The double bond is from the central carbon to one of the terminal nitrogens, rather than the one after the carbon chain. If I'm not making sense compare this: http://www.chemspider.com/Chemical-Structure.23089765.html with the structure on basement_shaman's post. Although I don't believe this would vastly change how leonurine binds to receptors, it does make the actual chemical much less water soluble than the one seen on wikipedia.

If anyone has any information on the alkaloids/terpenes of leonotus sp. or any information on the pharmacology of any of the chemicals found in this plant, I'd be very, very happy to see it.

I really don't know why so many people have felt that dagga is so lackluster, while I have found it quite a boon.

 

[pharmakos]

i believe that dagga needs to be pretty fresh in order to achieve effects from it. i had one supplier a few years ago that could get dagga petals to my mailbox within a week of harvest and that stuff produced a really nice effect. other times the same vendor would admit his stock had been sitting for a few months, and that older stuff was never as good.

 

[DL-ark]

i believe that dagga needs to be pretty fresh in order to achieve effects from it. i had one supplier a few years ago that could get dagga petals to my mailbox within a week of harvest and that stuff produced a really nice effect. other times the same vendor would admit his stock had been sitting for a few months, and that older stuff was never as good.

Yup, mine comes straight out of my backyard (more or less)! Fresh as can be!

 

[ParappaTheRapper]

Altering Serotonin Levels Changes Monkey Behavior and Status



I am curious to peoples' reactions to the lecture.

 

[...]

What could we do to caffeine's structure to shorten its duration of action? I am interested in developing a xanthine derivative geared towards late-night studying: something you could take for a boost at 10 pm yet be in bed by 1 am. Any ideas?

 

[AlphaMethylPhenyl]

uhhh, melatonin?

Sorry I don't know. I think you should just titrate your caffeine earlier.

I have a few questions:

Is MXE neurotoxic? (I read the study concluding acute toxicity, but only with three subjects and in the acute phase). Any other toxicities?

What dose/ratio of dexamphetamine is neurotoxic in chronic usage? cardiotoxic? I'm thinking anything that exceeds .5-2mg/kg? But I'm looking for a smaller margin of error. And methylphenidate is neuroprotective at reasonable doses, got that. I'm just wondering because I'm looking out for a friend. I take the safer route.

Why does US prescribe stimulants so much?

Do benzos really cause brain damage after chronic use?

 

[Solipsis]

I thought MXE shows only acute celebellar toxicity which is just a way of saying severe intoxication affecting some motoric / semi autonomic functions. But nothing that says it isn't reversible or related to dangerous CNS depression.

 

[endotropic]

Why does US prescribe stimulants so much?

Because it's cheaper and easier than any other method of controlling rambunctious children, combined with an extremely powerful pharmaceutical lobby with direct marketing to parents, teachers and doctors. My guess anyways.

 

[Dresden]

Does anybody know an explaination of why I only seem to get tachycardia and some minor arrhytmia near the tail end of an mixed levo/dextro amphetamine experience? Whilst the experience lastst minor tachycardia (80->90 bpm) but near the and a few double/ empty beats and more tachycardia (ranging from 95 to 130bpm) I cant seem to find an explaination.


I mean with methamphetamine you could blame it on the conversion from methamphetamine to amphetamine but thats bit the case here.

I wonder why I have these things at the end of the experience.

I would venture that it's because the amphetamine is, albeit in small quantities, being metabolized into 4-OH-amphetamine, which is structurally very similar to PMA, and as PMA is known to be responsible for increased blood pressure, so probably is 4-OH-AMP.

As for the tobacco smoke component of this thread, tobacco smoke is known to contain over 7000 chemicals. Who knows what they all do?

 

[~QuirKyNai~]

If something is a suicide substrate (like a covalently binding agonist) then eventually receptor internalization will occur (and the receptor is replaced eventually). However until internalization occurs signal transduction can usually still take place so the effect of an irreversible agonist is not that of an antagonist, effectively, because the receptor population is not immediately destroyed.

I found this paper that demonstrated inhibition of CYP2D6 and CYP3A4 enzymes by kratom.

Does anyone know how to compare the concentrations of extract used in the paper to plain leaf dosages? I'm wondering at what dose this sort of inhibition becomes relevant.

I wonder if.that.can be used to.potentiate suboxone.in my.experiences i.dont really feel like taking.subixone after kratom precipitates withdrawl.
I.know there's a book.that shows the binding affinity at mu,delta,and.kappa receptors.
Anyway.i..have been on .25-.50mg suboxone daily,and.have taken kratom.about.3-4 hrs later with me def. feeling the antidepressant.qualities for sure and maybe.some pain relief....one the last time i had taken kratom i.took .25mcg about 3-4hrs later...what i felt i think was some knocking off the kratoms antidepressant effect,and def felt pain relief again..so im not sure how strongly kratom.binds at.mu..or how much the delta attaches.but i think that delta plays more.of a role in the analgesislc amd.amtidepressant effects of kratim....but dont hold me to that

I think kratom shud be looked at more,especially in.conjunction with sunoxone/subutex.

 

[~QuirKyNai~]

Also...can kratoms mitrigynine and 7-hydroxy-mitrigynine.be.turned into.base.form in the.stomach.with tums?.
Or.can it be turned into.base.form in any way.for ingestion..NOT for smoking...
I was wondering of basifying.the alkaloids cud possibly have a.better effect.
If anyone wants.to chime in on this one,id appreciate it

 

[nickfurry]

Readily available inert gasses for storage

Since I'm not a chemist I don't have access to lab grade argon gas. If I jump through the hoops to be allowed to buy it, it is still ridiculously expensive to get a large tube and it would probably get me on some watch list. Same thing with helium in my country.

So I'm trying to figure out the best alternative that can be easily bought OTC and used to create an inert environment for very long term storage of chemical substances to prevent them from degrading into poisonous compounds.

Would any of these work?

CO2 bulbs for soda machines
N2O whippets
Pure argon used for welding ('technical grade')
85% Argon + 15% CO2 for welding
Anything else?

 

[sekio]

Why not nitrogen? Argon would work fine but it's like 100x more expensive than N2. CO2 would work too as long as you're not planning to store anything acid sensitive(!).

Realistically most drugs are fine to be stored under air, they don't oxidise at an appreciable rate.

 

[sekio]

Welding argon is probably fine.

Nitrous oxide is not a good packaging gas as it's an oxidiser under some conditions. CO2 is not a good packaging gas either as it can react with moisture to form carbonic acid & can under some circumstances react with certain functional groups.

How do I find out if a novel drug, such as a cathinone or novel tryptamine, is acid sensitive?

You make it and do long term storage and stability studies. Or read the chemical literature.

Generally speaking, storing compounds as cold as you can get them, in well sealed containers, is more important than storing them under inert gas. The amount of oxygen in a typical vial headspace is not very much, so the extent of oxidation will be limited.

 

[Incunabula]

I don't know where to get N2 apart from in a large liquid nitrogen tube that would cost $$$$ and I would also have to come up with an explanation for why I needed it. Is it sold for any non-medical purpose such as model trains or something?

Is N2O inert?

How do I find out if a novel drug, such as a cathinone or novel tryptamine, is acid sensitive?

Argon, in the form of welding gas, is actually very easy to find even in small quantities. Is this technical grade good enough, or will it contain harmful impurities that might cause oxidation?

I understand an inert gas is usually not necessary, but I'm interested in the theoretical optimum.

Nick, the best thing for you would be to get argon. You can buy it online in containers with easy dispension, made for wine preservation (just google winesave) I'm sure it's pure, since it's intended to be in contact with "food". I don't use it myself, but I'm considering it for my jar of acid blotters.

But as Seiko says, it's not really neccesary for most compounds. If you have vials with proper lids and pack them thightly to the brim, and store them in the freezer, you should be good. The argon is just going to be an unnessecary hassle.

The vials you want to get, would be amber pyrex glass vials, size 5/8 dram. Fits approximately one gram of most compounds, give or take, depending on the density obviously. The lid should be be lined with some kind of foam (it's often PE) Don't get the lids with foil linning, I don't think they seal as tightly. Again, google is your friend

If you need to find out about the stability of a certain compound, ask in the respective threads. Some one there might have first hand experience with its stability. Otherwise, ask around if any one can see any easily reactive groups on the structure. But generally, discussions on the stability of specific chems belongs in their respective threads.

We do have two threads on the topic, though.
The-Big-and-Dandy-Storage-Thread
The-Big-and-Dandy-Solubility-and-Stability-Thread

 

[Incunabula]

What could we do to caffeine's structure to shorten its duration of action? I am interested in developing a xanthine derivative geared towards late-night studying: something you could take for a boost at 10 pm yet be in bed by 1 am. Any ideas?

Wait, this isn't such a bad idea. Coffee has a pretty long half-life, 3-7 hours. If you drink coffee in the afternoon, you still have half of the caffeine in your body when you go to sleep, which can have an impact on the quality of your sleep.

I just remember I once looked at a bunch of methylxanthine analogs that had been made. Might be worth checking out again what is known about caffeines SAR (probably a lot)

 

[Hermetic0ne]

i love calculations and possibilities on my favorite brain boosters. Ive spent a long time reading abstracts, extracts and patents. I learned a lot, kept learning so then i got curious because all these methods cross over in little ways of course. i started wondering things like.. instead of doing azide swaps in a PTC, why not use weight lifting supplements like NO2 in (NaNO) NO Explode?

Or things like Microwave or Electro synthesis and substitutions of starting/ending materials. Ive started to feel like sometimes the possibilities of different routes are endless. Vitamin b and supplements.. and even thought of hypothetical scenarios like oxidation of methocarbamol. Yes, I have slightly talked about several different routes and not to completion.. I know But this is what excites me..talking what ifs and using the citations back to the early 1900s. Anyone here considered any of these?

 

[nickfurry]

Do you guys think Phenetrazine is made from left over N-ethyl-buphedrone by the Chinese? What kind of cyclization and more importantly, what likely impurities?