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I Like to Draw Pictures of Random Molecules

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was pretty surprised when i looked closer and discovered that diphenidine/methoxphenidine has that amphetamine structure inside it.
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in terms of 3d structure diphenidine is much more like pcp though.

and... putting gaba skeletons into things doesn't necessarily confer gabaergic activity.
 
More boring stimulants, along the lines of αMT/MPA:


Wr5jia4.png

rWNPvPf.png
 
DL-ark said:
Uh, this might be pretty histaminergic. Might be good on TAAR1 though.
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I agree, they could produce uncomfortable gastric effects. The wakefulness promotion could synergise with any TAAR1 activity, but it's hard to predict these things (cf. betazole and histamine).
 
SeenSoFar said:
If you want to go for increased μ-opioid affinity, why not go in this direction?

download5.png


It seems so bloody obvious I'd have to wonder why it hasn't been explored yet... Has it?
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I am fairly certain that what gives pethidine such affinity for mu-opioid are the oxygens as well as the the piperidine. Maybe having a methoxy/hydroxy somewhere on there. Oxygen is essential to opioid activity.

Jonneh said:
I agree, they could produce uncomfortable gastric effects. The wakefulness promotion could synergise with any TAAR1 activity, but it's hard to predict these things (cf. betazole and histamine).
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I was saying it may have some affinity for TAAR1, but im sure it would synergistic even if it wasn't.
 
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DL-ark said:
I am fairly certain that what gives pethidine such affinity for mu-opioid are the oxygens as well as the the piperidine. Maybe having a methoxy/hydroxy somewhere on there. Oxygen is essential to opioid activity.
Click to expand...

You may be right, although I'm fairly certain that I've seen a couple compounds with a similar substitution pattern that have opioid activity. I'd have to go back and find them to be sure though.

On another note, here's a random one. I was messing around drawing a compound that might have opioid and psychedelic activity when I ended up drawing this:

download6.png


I doubt if it would have any psychedelic activity, but it does overlay quite well with many opioids in 3D, such as dextromoramide.
 
The library doesn't allow chemaxon. Only the computer center does. I had to use paint since I'm at the stinking library!
Here's a picture of 2-indolylcyclohexylpiperidine, 2-IOCP. It's a stronger, less toxic version or BTCP.
ot0q51.png

Here's insomfinil. It's a superior wakefulness enhancer because it produces fluorenol as a metabolite! Insomfinil, the superior modafinil.
2448z04.png

Here's InsomfinilPhenylPiracetam, or IPP-48. It's a combination focus enhancer and wakefulness enhancer. It a combination of phenylpiracetam and insomfinil.
28bvgwm.png

Here's 5-Ethyl-MPA, 5-Ethyl-Methiopropamine.
14o3zx4.png
 
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After some further thought on combined MOR/5-HT2A agonists, I came up with the following. It's not a serious effort, it's kind of silly, but it might very well be active as an opioid, it overlays quite well with various fentanyl analogues in 3D.

download8.png


Also, here is another possible mixed opioid/psychedelic, but this one is actually reasonable to assume that it's active. In fact there's no reason for it not to be.

download10.png
 
Jn4VGjd.png

Left to right then down...

Dirty Gabaergic (whether it stays together or not, it should still breach the BBB and have an effect on GABA)
Glutamate antagonist, maybe gabaergic but unlikely. Could possibly have opioid activity. Should be pretty neuroprotective, maybe for alzheimers?
My addition to SeenSoFar's psychedelic opioid quest. The 4-position bromine should be able to be any halogen.
 
That's very interesting! You've come up with a couple very interesting compounds there!

You know, I was doing some skimming of papers, and I found that my 3-acetyl-morphine-miprocin-sulfate-diester monstrosity may actually be a very interesting compound indeed because it may just result in the release of 4-HO-MiPT and 3-O-Acetylmorphine-6-O-sulfate, which apparently is a much more potent compound than morphine, heroin, and the like. I'd really like to sample it now. I'd be excited to see what happens!
 
SeenSoFar said:
That's very interesting! You've come up with a couple very interesting compounds there!

You know, I was doing some skimming of papers, and I found that my 3-acetyl-morphine-miprocin-sulfate-diester monstrosity may actually be a very interesting compound indeed because it may just result in the release of 4-HO-MiPT and 3-O-Acetylmorphine-6-O-sulfate, which apparently is a much more potent compound than morphine, heroin, and the like. I'd really like to sample it now. I'd be excited to see what happens!
Click to expand...

I'm certain that the opioid feel in that case would be fairly overpowering compared to the psychedelia.
 
DL-ark said:
I'm certain that the opioid feel in that case would be fairly overpowering compared to the psychedelia.
Click to expand...
I'm sure it would, but I love the feeling of psychedelia behind a massive opiate high.

Here's another one for you all. It overlays with fentanyl in 3D exactly. I think it would be a very interesting one to have a go with.

download12.png
 
Potential Potency of Flunitrazepam RC?

methylclonazepam_zps986d7b3e.jpg.html


Wouldn't the potency of this "RC" be higher than Flunitrazepam because of the steric hindrance of the chlorinated benzene?

I know the methylamino group makes this RC more "fun" than Clonazepam.

Not sure if this fits in this forum or BDD. Sorry mods.

EDIT: APPARENTLY MY PHOTOBUCKET PICTURE WON'T LOAD, but the point still stands. Imagine the image in your head I suppose.

adder said:
I did my best to imagine what I thought was obvious, but honestly I doubt that anyone could have guessed what you had in mind.:D Look up the structural formulas of flunitrazepam and clonazepam, because these have very little to do with them, one is completely wrong with the nitrogen at position 4. lacking one bond and the other one isn't even a benzodiazepine.
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Fixt :^)

EDIT: apparently it wont load again, but all the double bonds and a nitrogen is now on the second pic

I got lazy when drawing them I guess.
 
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I suppose the compound in question is N-methylclonazepam (that is clonazepam with a methyl group on the nitrogen or flunitrazepam with a chloro group in place of the fluoro group - clonitrazepam?). I won't speculate much, but I would imagine this is a benzodiazepine with a very long half-life just like clonazepam (probably a bit less long-lasting, but it's going to be metabolised into clonazepam anyway), it could be more potent on a weight basis (1.5-2x clonazepam), and even if it's not, the perceivable effects should be stronger and the come-up faster because as a tertiary amine this one should penetrate the blood-brain barrier more effectively than clonazepam. However, I have some doubts that it's superior in effects to flunitrazepam. With that chlorine sticking out at C2' it may still cross the blood-brain barrier slower than flunitrazepam, but perhaps it won't matter.

I don't know the SAR for specific subunits of GABA(A) receptors, but chlorine in place of fluorine can change a lot how a molecule binds to a receptor if the part of a molecule with either takes part in binding. I guess the best example is 4-FA vs. 4-CA.
 
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