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I Like to Draw Pictures of Random Molecules

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Thx for all your explanation. Does this little variation of already know compound make sense ?

lQwzq8p.png


naphmetrazine :

gy0rHou.png


MHP like :

mMX2b7A.png


various stuff :

k2DTCm0.png
 
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Idea taken from another thread. Why no more lysine based prodrugs ?

0DDOpSg.png


Also i have another, maybe naive question :

It is possible to create a pro-drug metabolized by some process that will be inhibited by the drug or need time to be regenerated ? So it limit the possibility of becoming dependent because after taking too much in a too short time frame there is no more effect at all.
 
various stuff :
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some of these are known compounds, the methylphenidate morpholine analog has been sighted in the wild, the top 2 morpholines are known pharmacologically too

not sure about benzyl ritalinate or the thio esters but it'd be interesting to see what they would do (hey, have you heard the latest band the kids are listening to, Benzyl Ritalinate and the Phenidate Thioesters?)

Wouldn't the above not work due to free rotation?
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logically as long it can still conform to the binding pocket, it's all good, even though it may be less potent than others

Why no more lysine based prodrugs
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I think lysine-MDA has been made, maybe that was just a hallucination though. As for how useful it was, I suspect delaying release is not going to make it any more intense. I also think the latter 2 (mephedrone & MDMA) work best as bolus doses with fast administration rather than gradual slow releases over time. Methamphetamine is already long duration enough, look how unpopular stuff like benzphetamine & its analogs seem to be

It is possible to create a pro-drug metabolized by some process that will be inhibited by the drug or need time to be regenerated ?
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Sure, you could find compounds such that one of the downstream metabolites of the drug would inhibit the enzyme/process that converts inactive prodrug to active drug. You would be liable to mess up metabolism of a lot of other things in hat case though... its rare to have an enzyme in the body with an affinity for only one compoud.
 
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sekio said:
You would be liable to mess up metabolism of a lot of other things in hat case though... its rare to have an enzyme in the body with an affinity for only one compoud.
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I think I will say something controversial but I think short term hardcore side effect or not necessary a bad thing, maybe a good thing. I was addicted to a few substance in the past, tobacco, weeds and benzos. I think it's very easy to fall addict to this substance because there is very few short term side affects. On the other side, when I did binge on 4-MMC, the hardcore crash that happened next prevented me from abusing the substance and taking too much of it. The ideal would be to mess up things that give uncomfortable but not dangerous side effect.
 
5%2C6-dichloro-2-aminoindane.png



How would ether/thioether bridges fair in these analogues. Idea stolen from paroxetine

1%2C3-benzodioxol-5-yloxyethanamine.png


1%2C3-benzodioxol-5-ylthioethanamine.png



Would this resist MAO metabolism?

phenyldithioamine.png
 
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%5Bbicyclo%5B4.2.0%5Docta-1%2C3%2C5-trien-7-yl%5Dmethanamine.png


4-fluoro%5Bbicyclo%5B4.2.0%5Docta-1%2C3%2C5-trien-7-yl%5Dmethanamine.png


3%2C4-methylenedioxy%5Bbicyclo%5B4.2.0%5Docta-1%2C3%2C5-trien-7-yl%5Dmethanamine.png


I know there is very little tolerance for substitution on the methylenedioxy ring but could this be active?

1-(2-ketobenzo-1%2C3-dioxol-5-yl)-propan-2-amine.png


1-(2-fluorobenzo-1%2C3-dioxol-5-yl)-propan-2-amine.png


I know the difluoro has already been made but it is less potent I think
 
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1-phenyl-2-amino-cyclobutane.png


The distance of amine to benzene in the below molecule should be relatively the same to normal amphetamine

1-phenyl-3-amino-cyclobutane.png
 
The lower LogP is the issue. The QSAR of cathinones is actually quite different to the amphetamines. Dimethyl analogues of cathinones are active, for example, due to lone-pair interaction. In Chemoffice they overlay so I would be quite surprised if it were inactive.

The synthesis of this one is the sticking point for RC-grade chemists, especially the lazy ones. There is a simple, 2 step route from the right precursors - I cannot give details but I presume you can see it. Now, THAT was too much like hard work!
 
What do you mean by dimethyl analogues for cathinones? Where are the subsequent methyls you're talking about placed? On the alpha carbon? On the nitrogen?
 
aced126 said:
What do you mean by dimethyl analogues for cathinones? Where are the subsequent methyls you're talking about placed? On the alpha carbon? On the nitrogen?
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Sorry - on the nitrogen.

As for diphenidine analogues, having a flexible amine group (like the N-ethyl) gives the greatest affinity. The problem with the class is that they are generally too low-catching evidenced by the high dosages. If you make the sulfate, diphenidine works much better when snorted but the optimal compound (by a country mile) in the class is the N-isopropyl. A lot of experienced K users thought it was K. Same dosage as K and so forth. Why didn't we see it? Apparently the chemistry was too hard. I don't think I even need to describe a route, it's so simple.
 
Are you sure n,n-dimethyl cathinones are intrinsically active, or are active due to cyp3a4? I thought it was the latter
 
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