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Isoquinoline opioid

Well, getting a domain and 4000 meg of space is about 5 quid per month. If we had space for people to add stuff and someone compiling it and so on, it could be a real winner. I mean, stuff Rhodium, PihKal & Tihkal in there for a start.
There is a free java applet called JME editor allowing people to draw nice structures. Give eveyone a 2MB sandbox and, when everyone agrees, someone makes a definative article and we place that in our list of topics.

Back on topic: Can this stuff be MADE in an optically active way, or is it a simple case of partial crystalization or whatnot?
 
Why not just setup an alternate forum for ADD where chemically oriented discussions are allowed and people can attach files including articles etc? Heavily moderated by knowledgable members and categorized for different drug types. And I don't mean for it to compete with Bluelight, but the no-synthesis-rule is actually rather crippeling for such a forum.

On-Topic: Everything can be made asymmetrically. Just a question of cost and labour. :)
 
Yes, I fully understand and respect their policy.
However as said it is a policy that somewhat cripples "advanced" drug discussions. :)

If anyone is up for starting an alternative forum with focus on such discussions (without restrictions and with more structure) I'm in, and I have good computer knowledge and have run forums before. (I hope noone of the Bluelight staff takes this the wrong way, as I love this forum and how it is run but as vecktor said it sounded like a good idea I guess it's ok to discuss).
 
Well - who has a webserver in a location where such discussion/content storage will be permitted?
The rest is fairly easy.

edit: Added some info I found on these. Linked pics on tinypic.

2ufc07d.jpg


25thu76.jpg


The (R) isomers are the active ones for the 4-Cl, 4-NO2 and 3,4-diCl variants, showing that there is some stereoselectivity in their binding.
 
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it seems strange that a nitro group is the most potent, doesn't it?

Anyone know if there's any activity with substitutions at the methoxies?
 
^ thinking the same and aslo thinking why they did not list on that chart the number for the R-isomer and only listed the racemate being they do so for other ones...
 
This nitro-tetrahydroisoquinoline compound certainly looks somewhat decent. I've been waiting for Shulgin to release a book on cyclized PEA's following "Bischler-Napieralski" cyclization but it never happened. PEA's are a doddle to make (theoretically) in an equipped laboratory. Intuitively, the structure of papaverine springs to mind when I see this molecule. You have to appreciate the similarities, even though their are distinct deviations. I think this is tangible chemistry meaning, in principle (pragmatic considerations aside), I could see myself working with it.

It's shady that this series has not been reported in any books by Dan Lednicer and others who are experts in the field of opioid analgetics. Some more info seems appropriated before it is possible to make informed decisions. The drop in potency upon changing the nitro group to other pharmacophores is somewhat discouraging if not downright ugly.
 
meh, there are nitro groups on all sorts of things without any inherent toxicity. Look at all the benzos.
 
the fascinating thing about this class of opioids is the possibility that they also inhibit phosphodiesterase activity, like papaverine, moxaverine and others and could be thus one step towards nootropic opiates (which i'm most interested in researching)
 
Sorry for being so dumb, but exactly what does nootropic MEAN? The term seems to be a little vague. I mean, I know the original definition, but it's being bandied about so much these days...
 
by the term "nootropic", i mean properties like enhancement of cognitive capabilities, accelerated learning, protection/growth-stimulation of neurons and so on.

the pde-inhibiting features of these compounds could have another possible advantage (if you're interested in cellular biology): since opiates usually decrease the concentration of camp in neurons, which is one of the reasons for developing tolerance, pde-inhibition would counteract this by causing an elevation of camp-levels and thus maybe also counteract the development of addiction.
 
Yes, the Pictet-Spengler reaction looks like a good place for budding chemists to try their hand at making relatively more sophisticated molecules than the simpler entries embodied in TIHKAL.

Pictet-Spengler_Reaction_Scheme.png
I had at one time been led to believe that tricyclics were going to be a starting point for a Shulgin trilogy, but this idea seems to have been thrown out the window now with other projects such as some sort of psychedelic encyclopedia.

One thing that is for sure, is that this type of chemistry appears to have a good amount of meat on the bones!
 
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