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Stimulants of the Future III

Maybe i should correct myself, I meant to say 'intriguing' rather than 'promising' (the oxygen heterocycle looks interesting).
Unfortunately I don't have any reference on the compound.

It's a Chinese research stimulant, that's all i know.
You could try to ask them for some information if your Cantonese is good enough =D
 
The compound above was nicknamed "robalzotan", "AZD 7371" resp. "NAD 299" and is said to be a selective 5HT1A-antagonist. See one of the following for further info:

J Pharmacol Exp Ther 2009, 329(3), p.1048
J Pharmacol Exp Ther 1997, 283(1), p.216

And it's definitely NOT chinese. The oldest patent that I could find was from Astra-Zeneca, Sweden. Where the heck do you get your infos from? Vendor's catalogues? And since when are 5HT1A-agonist decent stimulants?

- Murphy
 
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I guess google isn't such a good source of information, thanks for the tempestuous information though. You're like a patent machine :D

EDIT: Anyway if you remove the fluorine, the amide group and possibly change the amine alkylation it could turn up to be an interesting substance.
 
RTI-51

220px-RTI-51.png


http://en.wikipedia.org/wiki/RTI-51
 
RTI-51
Click to expand...

I've also been thinking that out of all phenyltropanes this one will probably be a winner...

Compound [3H]CFT [3H]DA [3H]Nisoxetine [3H]NE [3H]Paroxetine [3H]5-HT
Cocaine[8] 89.1 275 c.f. 241 3300 (1990) 119 c.f. 161 1050 (45) 177 c.f. 112

RTI-31 1.1 3.68 37 (22) 5.86 44.5 (4.0) 5.00

RTI-51 1.7 ? 37.4 (23) ? 10.6 (0.96) ?
RTI-55 1.3 1.96 36 (22) 7.51 4.21 (0.38) 1.74

31 = chlorine, 51 = bromine, 55 = iodine
 
PCP, DP2MP, MPH hybrids

i've been thinking a lot about the structures of PCP, DP2MP and MPH - there are a lot of stimulant hybrids which have not been explored according to pubchem. this seems like very fertile (if not original) ground given the extraordinary potency of these three compounds as DARIs. my first question is simple - what happens when you move the nitrogen in MPH so that it has a tertiary amine (methyl 2-phenyl-2-piperidin-1-ylacetate) this has been made but i don't know about its activity. secondly what happens if you move the nitrogen in PCP so it has a secondary amine and contains the PEA skeleton?

thanks
 
I'm pretty sure that the most winningest phenyltropane is going to turn out to be the one with an R3 of -CH2OCH3 and an R4 of -3,4-dichlorobenzene, and you're welcome to quote me on that.
 
The main question lies on 2 distinct type of drugs. Should we aim towards releasers or reuptake inhibitors.
Honestly I don't know which ones is worse from a toxicological POV.
 
releasers are bad, just think is it healthy to get DA levels 1000% from baseline(methamphetamine)?
 
how about 500 percent? classical stimulants are 'bad'.

ebola
 
Question fer' you guys..
1. whar do you acquire this knowledge, of halogens and whatnot. I know what a halogen is..but not the effects of structures on effects and whatnot..halp?
2. Is cocaine both a releasing agent and a DNRI? I thought that cocaine had a weak releasing effect (dopamine) compared to d-amphetamine, but it increased dopamine levels by the DNRI effect by keeping dopamine in the syapse longer. In terms of DNRIs, ive only tried methylphenidate, but i do tend to like d-amphetamine a lot..are the DNRI's generally considered "more chill" stims, compared to strong releasing agents like amphetamine and substituted amphetamines, and since, in theory, DNRIs dont force out a ton of dopamine at once, they just prolong your supply (if i understand properly), then wouldnt they be much less toxic than releasing agents and also be slower to gain tolerance to (as opposed to amphetamine, which if i understand right the tolerance you get is just having less dopamine..)?
3. Would it be possible to somehow make a MD4-MAR? as in, methylenedioxymethylaminorex?
Someone tutor me plz..nuffin too complicated though, im at about a high school chemistry level, in terms of talking about methyl groups and this and that..you know?
 
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boohigh said:
releasers are bad, just think is it healthy to get DA levels 1000% from baseline(methamphetamine)?
Click to expand...

releasers are less desirable more because they increase the cytoplasmic concentration of neurotransmitters and inhibit the storage of these monoamines. Oxidation of these monoamines in particular dopamine is associated with toxicity.
 
A halogen is simply an element that is a member of the seventh (VII) row, or column, of Mendeleev's periodic table of the elements. F, Cl, Br, and I are some common examples in ascending order of molecular weight. Any heavier than that, and they are naturally radioactive.
 
And 3,4-MDO-U4EUh is an entirely possible compound; it's just that I read somewhere (hearsay, admittedly) that research has showed it not to substitute for MDMA.

MDMA is such a special and unique drug that I think I would find it rather surprising if 3',4'-md-4-methyl-aminorex did.
 
What do we know about the SAR for substituted aminoreces (other than that the 4-methyl yields increased potency)?

ebola
 
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