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GYKI-52895 methylenedioxy-Benzo

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is this an ampa antagonist or an agonist apakine type thing? it looks a lot like some of palantins much hyped but dissapointing ampakines, these often have a md or ethylenedioxy benzene moety.
 
Yeah I'm slightly confused on this one. I think it was in a chem catalogue under dopamine agonists (or reuptake) but also I read the ampa thing. 8(

It looks like a benzo agonist. For no other reason it would be cool to have a benzo with the methylenedioxy (I know I know its not the be all and end all but still it would be cool :p :)
 
Reminisant B said:
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3539

Very information on this chemical but is a methylene-dioxy benzodiazepine type structure.

Does anyone know if its a Dopamine reuptake inhibitor or a benzo type chemical?
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Well you can see the amphetamine skeleton (MDA skeleton actually) in the structure. My other half's lecturer at uni had something to do with the development of a benzodiazepine with stimulant activity - this might be the very compound (will check)
 
Do you mean stimulant in terms similar to amphetamine or stimulant in terms of benzo antagonism or another route via glutamate?

If it is a chemical that has some qualities of amphetamine as well as benzo agonsim that sure sounds interesting if slightly addictive. 8o
 
^ Stimulant as in psychomotor stimulant - yeah apparently it got dropped from the rosta when a pharm firm used some of the paper in question as the basis of a series of benzo related anxiolytics... wonder why? =D


Christ! A cental stimulant with anxiolytic proberties would be horribly addictive, not surprised it never got even onto the starting platform.
 
don't gyki and tofisopam look similar to rhoeadin (too lazy to look it up now)?

rhoeadin (or papaver rhoeas) is also known to be both stimulant and sedative.
 
The id part of me is suddenly VERY interested in this drug, GYKI-52895. F&B -- Would you mind checking with your other half? I know I'm being a pedant here, but I think it's a 3,4 benzodiazepine, not 2,3.
 
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There's no good reason to believe this is related to the pharmacophore of anxiolytic benzodiazepines, or any benzodioxole entactogens. The 2,3-benzodiazepine ring is very different from the 1,4-benzodiazepine you're used to seeing; for one thing, in GYKI-54895, the substituent numbering moves counterclockwise whereas in Valium it moves clockwise, so the 2-position was the 4-position and the 3-position... well, okay. It's hard to compare the molecules even on a purely structural basis.

It is in fact a negative allosteric modulator of the AMPA receptors, along with other 2,3-benzodiazepines, and also a dopamine reuptake inhibitor:

http://onlinelibrary.wiley.com/doi/10.1111/j.1527-3458.1996.tb00292.x/pdf

If Piracetam/Aniracetam are any indication this compound makes you dumb! :p
 
Woah, just thinkin about a methylenedioxy benzo is crazy. What would be even more crazy is a methylenedioxy opiate..
 
Swisss said:
Woah, just thinkin about a methylenedioxy benzo is crazy. What would be even more crazy is a methylenedioxy opiate..
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Lol, throwing a methylene group bridged between two oxygens doesn't make everything magical. It just so happens that doing it on a certain part of a methamphetamine molecule drastically changes the pharmacology, and doing it on the right place of a pyrovalerone molecule seems to reduce the toxicity as well as altering slightly the pharmacology.

You do it to certain other things, you may not even have those properties any longer.
 
lolwhatzdrugs said:
Lol, throwing a methylene group bridged between two oxygens doesn't make everything magical. It just so happens that doing it on a certain part of a methamphetamine molecule drastically changes the pharmacology, and doing it on the right place of a pyrovalerone molecule seems to reduce the toxicity as well as altering slightly the pharmacology.

You do it to certain other things, you may not even have those properties any longer.
Click to expand...


Actually popping a 3,4 methylenedioxy on Tapentadol(an opioid) looks fairly promising as far as it creating an element of this "methylenedioxy"(SERT) effect combined with mu-opioid effects.
 
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