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Phenyltropanes

Then again, UK catchall laws fail to catchall....

1-(2H-1,3-benzodioxol-5-yl)-3-fluoro-N-methylpropan-2-amine

I've EVEN tried telling them but until it turns up, they don't bother!

FREEDOM OF SPEECH
 
clubcard said:
Remove the bits in red. Then there are only 2 isomers. A p-CF3 will be strong but longer acting... but probably safer. The p-NO2 is a dangerous game.
Click to expand...

Here's where I am confused, the 2-beta position carbmethoxy? or on the NO2, the oxygens? (then it wouldn't be N"O"), I know benzoylecgonine is inactive without the carb*meth*oxy "methyl", but becomes more active if you remove it entirely (tropacocaine).

Xa3oi.jpg


Those are stonger, from what I've read of Singh's paper
 
I'm sure they are 0 they are also MUCH harder to make where as the compound I mentioned is synthetic coke - the ester function (which you haven't removed, just made it an alkene). The IUPAC name is clear and there are stacks of IUPAC->Image programs. The tropane ring has NOTHING apart from the (substituted benzene) on it so remove the -C(CH2)CH2CH3.

It's VERY simple.
 
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I'm sure they are 0 they are also MUCH harder to make where as the compound I mentioned is synthetic coke - the ester function (which you haven't removed, just made it an alkene). The IUPAC name is clear and there are stacks of IUPAC->Image programs. The tropane ring has NOTHING apart from the (substituted benzene) on it so remove the -C(CH2)CH2CH3.

It's VERY simple.

Only the nitro is both soluble enough to snort with sufficient freeze so you don't feel it and that instant UP which is broken down at the receptors where the p-NO2 becomes p-NH2 which IS active, but much less so since it's LogP drops a great deal so it redistributes. It's this that is the worry - aromatic amines can be bad. Not always - nitrazepam & friends are all pretty safe (although twice as toxic as benzos with a -Cl or -Br). I think the best example is nitromethaqualone. That nitro on the para position was reduced & the metabolite was mutagenic. It's something that has to be researched. If they had chosen to go for the o-nitro p-methyl, it's actually MORE potent and the nitro is less likely to be reduced. My theory is that by the time they had run all of the trials on THAT compound, benzodiazepines with their massively safer action that killed a BIG seller. An o-CF3 is potent and safe, for example.

FREEDOM OF SPEECH
 
Yes I did it last time, this is it:
lKQEI.jpg


But because I like making things confusing, would this be viable? (e.g. possible from the known synthesis possibilities)

yoHJQ.jpg


Just yours, backward at the 2-beta, probably more of a local anesthetic(?)
 
The top one, remembering there is still a chiral center.

That has effects just like cocaine.....
 
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So I've added Singh's values for the bridged, and a lot of 2-beta-acyl's that weren't from the RTI lists, as well as upgrading the initial table with Singh's selectivity ratios. (@ WP's list of PTs page)
 
Anyone care to help with corresponding Singh's PT values and numbers to the RTI's and others at WPs list? It's kinda a daunting task but all I need is input and I'll do all the work, which are which; anyone can do it; just see what the values are for DAT, SERT & NET and its a good bet they are the same as Singh's findings, sometimes the values are off by a point or two (RTI got 4.07, Singh got 4.05 for DAT; it's easy to tell because how close the other two, the NET and SERT, will be)
 
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