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Drug designs. (MedicinalUser SAR thread)

Or maby I'm looking at it the wrong way. Maby I need to change the end and design a gamma-Butyroamine. Anyone got any ideas ? Would gamma-Hydroxybutric acid amide be Psychoactive ?
 
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Starting this week I decided to study what makes things stronger and last longer. I looked at MDMA and 4-methylaminorex and figured the 4-methyaminorex last longer than Methamphetamine. I was also comparing Methlene dioxy to Dioxolane which is structurally similar. Putting two and two together. I came to the conclusion that Dioxolane-4-Methylaminorex would possibly be more potent and last longer than MDMA, but thats just a hypothesis and it hasn't been tested. I how ever would like to test out my designs and see how well Dioxolane-4-Methylaminorex works. And if did turn out to be something better than MDMA then that would just make my day.
 
If I drew them they would look identical. Just take a look at a Methylene dioxy and then look at a Dioxolane.
 
If you drew them and they look identical that probably means they're identical

Methylenedioxy is describing the part of the dioxolane structure that would be attached to the benzene ring as far as I'm aware
 
Well there could possibly be a way of making it stronger and that's starting with gamma-Butyrolactone and designing an analog beginning with looking at that structure and see what can be added from there. What molecule that could be I don't know. Maby something absurd such as gamma-Butyrophenethylamine, but I dought that would work. For it to work it's got to be structurally correct and able to pass the blood brain barrier and be actually stronger than G.H.B. This design has been on my mind for awile. What are your thoughts on this ?
 
Well, I came up with another idea. Tell me what you think. The idea I came up with is a compound called gamma-Hydroxybutric aldehyde. It's hypothetically stronger than G.H.B. where the acid of G.H.B. is replaced by an Aldehyde. In organic chemistry, an Aldehyde is an organic compound containing a functional group with the structure R-CH=O. The functional group itself, without the "R" side chain, can be referred to as an Aldehyde. Replacing the acid with an Aldehyde in G.H.B. hypothetically strengthens the G.H.B. compound. It's effects are unknown, but it's predicted to have the same, but stronger effects of G.H.B. The Aldehyde is placed on the Hydroxy radical of the G.H.B. compound with the replacement of the acid with the Aldehyde. Hypothetically creating a new form of G.H.B. Unlike G.H.B. though It's a synthetic compound and not a naturally occurring neurotransmitter, but more of a depressant drug. This in conclusion shows a new design of G.H.B., whether it's ever created is unknown.
 
  • (RS)-1-(1,3-Benzodioxol-5-yl)-N-methylpropan-2-amine
That is the formal name of mdma. You are describing mdma.
 
arrall said:
What do you mean by this in relation to the context of your thesis?
Serotonin is not the most potent agonist of human serotonin receptors, not by a long shot.
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okay, I stand corrected. Is it just because it has so wide range of targets in the human body, it is so much more life-threatening to use molly than LSD (if you don't know what you're doing)?
 
Pissed_and_messed said:
okay, I stand corrected. Is it just because it has so wide range of targets in the human body, it is so much more life-threatening to use molly than LSD (if you don't know what you're doing)?
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This is a super interesting question. Even moving past LSD, to the NBOMe family, you don't see serotonin syndrome, you see seizures. That implies that a non-5ht2a/5ht2c receptor mediates the hyperthermia and other toxic effects.

I wonder if @someguyontheinternet or @AlsoTapered has any idea. I'm no neuroscientist so I've got no clue other than the exclusion of the two mentioned above.
 
Pissed_and_messed said:
okay, I stand corrected. Is it just because it has so wide range of targets in the human body, it is so much more life-threatening to use molly than LSD (if you don't know what you're doing)?
Click to expand...
GABA is the most abundant neuroreceptor, and also the most important to basic bodily function.

But unlike GABA (may be wrong), there are serotonin receptors all over the body in every organ, which is why loperamide has been implicated in serotonin syndrome. It doesn't cross BBB, but releases serotonin in the gut, which travels to the brain.

I do not think LSD causes significant levels of superfluous serotonin like MDMA does. I always feel more of a dopamine high from LSD, with visuals lol.

arrall said:
I do not think that the human body has created the most potent possible analogues of its receptors.
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Because there is no evolutionary need to, but when it comes to potent chemicals, nature always beats us in creativity.

This peptide from a poison frog is 40x morphine. I wouldn't doubt nature could produce something as potent as fentanyl.

en.wikipedia.org

Dermorphin - Wikipedia

en.wikipedia.org en.wikipedia.org
 
www.ncbi.nlm.nih.gov

Serotonin Syndrome

Serotonin syndrome is a potentially life-threatening syndrome that is precipitated by the use of serotonergic drugs and overactivation of both the peripheral and central postsynaptic 5HT-1A and, most notably, 5HT-2A receptors. This syndrome consists of ...
www.ncbi.nlm.nih.gov www.ncbi.nlm.nih.gov

This review on serotonin syndrome fingers 5ht1a,5ht2a,and 5ht3 receptors. I don't feel like it explains why psychadelic overdoses have a completely different set of sequalae than releaser/reuptake inhibitor overdoses, but some of the idiosyncrasies are alluded to (like how antipsychotics can both cause and treat serotonin syndrome).
 
someguyontheinternet said:
Why does an aldehyde strengthen it? What is the theoretical mechanism?
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That's a good question. I kind of look at chemical structures and just put them together like a puzzle. In this case I just looked at G.H.B.'s chemical structure and looked at another depressant structure then added it to the structure of G.H.B. That's why I said it's all a hypothesis.
 
MedicinalUser247 said:
Starting this week I decided to study what makes things stronger and last longer. I looked at MDMA and 4-methylaminorex and figured the 4-methyaminorex last longer than Methamphetamine. I was also comparing Methlene dioxy to Dioxolane which is structurally similar. Putting two and two together. I came to the conclusion that Dioxolane-4-Methylaminorex would possibly be more potent and last longer than MDMA, but thats just a hypothesis and it hasn't been tested. I how ever would like to test out my designs and see how well Dioxolane-4-Methylaminorex works. And if did turn out to be something better than MDMA then that would just make my day.
Click to expand...


These are interesting concepts but unfortunately, my comprehension of chemistry is extremely bad. also, whilst I don’t want to discourage you from posting your excellent knowledge, I was hoping this thread would be more for the discussion of biological pathways and how they link to effects on human behaviour or metabolism. examples would be things like transcription factors, enzymes, ion channels, receptors and Epigenetics.
What I hope to do is simplifying clarify how exactly these biological pathways lead to their impact of interest.
You are welcome to carry on posting here although it’s probably much more effective if we create a new thread for your chemistry related topic. that way, the two topics won’t get mixed up and to be honest, i’m sure you’ll get a lot of responses because many people on here have a deep interest in chemistry.
 
Well, It binds to the GABA receptor. And I got the idea from looking at simple Alcohols. I did have another idea for another G.H.B analog, but I decided the go with a simpler molecule. My other idea for a G.H.B. analog was gamma-Hydroxybutyropryrimidine. I got that idea from looking at Barbiturates. But I decided not to go with that because I was afraid of it being too potent.
 
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