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Chemical structures like tianeptine, A possibility

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mike.vick

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I have been looking for drugs with similar structure to tianeptine, and w-18 has kind of a similar structure with the phenyl chlorine attached to the Sulfer dioxide, with 2 nitrogens in similar positions and with a chain that has to oxygenated at the end (albeit connected to a nitrogen attached to a phenyl ring).

What do yall science people think?
Not many opiates with Sulfer dioxides w/ a chlorine ring. These are the only 2 I've seen.

https://en.m.wikipedia.org/wiki/W-18
https://en.m.wikipedia.org/wiki/Tianeptine
 
TriCyclic Antidepressants? (TCAs?) like Amineptine, Imipramine, Amitriptyline, Amitriptylinoxide, Butriptyline, Clomipramine, Demexiptiline, Desipramine, Dibenzepin, Dimetacrine, Dosulepin, Doxepin, Imipramine, Imipraminoxide, Iprindole, Lofepramine, Melitracen, Metapramine, Nitroxazepine, Nortriptyline, Noxiptiline, Opipramol, Pipofezine, Propizepine, Protriptyline, Quinupramine, Trimipramine?

Do you mean structurally similar or some specific function? If so what functionality are you looking for in a shared compound, opioids? Have you seen this opioid table:

Click *show* on 'table of non-morphinan opioids'

Oddly enough, Loperamide has a para-chloro-benzene (but no sulfur dioxide)

Methiodone has a sulfur dioxide, no reason why a para-chloro group couldn't be added to the arene/aryl functionality.

Don't see why you're looking for a sulfur dioxide in particular, I'm sure many of those substances could have such added to them, and the chloro as well, both in tandem, without any loss of opioid binding ability, but why are we looking to do that? Could probably add Au atoms on all of these somewhere too, but what would be the point except for requiring extra, unnecessary to function, synthesis steps; making it harder to synth and unavailable to most of those even with the necessary skills to create them?
 
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mike.vick said:
.... uh, yeah it is - seized in fake oxys
Click to expand...
That doesn't mean that it is an opioid, just that people have been selling it in pills that IIRC may have contained other opioids. When it was assessed by the PDSP, neither W-18 nor its likely metabolites had affinity for opioid receptors or produced opioid responses in in vitro assays.

The assays origionally used to detect the analgesic effects of W-18 are not specific for opioid-induced analgesia. In the absence of actual evidence that W-18 is an opioid (including a trip report from someone who has actually taken real W-18 ). I don't see any justification for classifying W-18 as an opioid.
 
Nagelfar said:
TriCyclic Antidepressants? (TCAs?) like Amineptine, Imipramine, Amitriptyline, Amitriptylinoxide, Butriptyline, Clomipramine, Demexiptiline, Desipramine, Dibenzepin, Dimetacrine, Dosulepin, Doxepin, Imipramine, Imipraminoxide, Iprindole, Lofepramine, Melitracen, Metapramine, Nitroxazepine, Nortriptyline, Noxiptiline, Opipramol, Pipofezine, Propizepine, Protriptyline, Quinupramine, Trimipramine?

Do you mean structurally similar or some specific function? If so what functionality are you looking for in a shared compound, opioids? Have you seen this opioid table:

Click *show* on 'table of non-morphinan opioids'

Oddly enough, Loperamide has a para-chloro-benzene (but no sulfur dioxide)

Methiodone has a sulfur dioxide, no reason why a para-chloro group couldn't be added to the arene/aryl functionality.

Don't see why you're looking for a sulfur dioxide in particular, I'm sure many of those substances could have such added to them, and the chloro as well, both in tandem, without any loss of opioid binding ability, but why are we looking to do that? Could probably add Au atoms on all of these somewhere too, but what would be the point except for requiring extra, unnecessary to function, synthesis steps; making it harder to synth and unavailable to most of those even with the necessary skills to create them?
Click to expand...

Just cause w.18 is the only opiate I've seen that could share structural Similarities , and there are not other substances out there that do, like u said the can have the phenyl chlorine, but that's the only other one, And the one you mentioned, with silver dioxide- especially a chlorphenyl attached to a sulfer dioxide attached to a tertiary amine that is right under another amine and has two oxygens at the tail in a similar manner.

And sulfer dioxides are interesting because I think most opiates have to have oxygen'(s) attached, but only 3 opies have the sulfer dioxide.
 
ALSO tianeptine is much different than all TCAs - and the only one that is an opiate - including it's most similar relative, Amineptine - INFACT the chloro-phenyl attached to a sulferdioxide attached to a tertiary amine is what separates TIANEPEINE from AMINEPTINE and all other TCA's, and I suspect- GIVE IT OPIATE ACTION. Based on opiates needing strategically placed oxygen'(s) and nitrogen.

AMINEPTINE really is not very similar, but it is the CLOSEST thing. That is what is SOO interesting about tianeptine's QSAR.
 
SEE methiodone SHOWS that sulferdioxides can be the source for oxygen molecules need for opiate activity. AS it is basically replacing the oxygen in methadone and replacing it with a sulferdioxide.
 
mike.vick said:
And sulfer dioxides are interesting because I think most opiates have to have oxygen'(s) attached, but only 3 opies have the sulfer dioxide.
Click to expand...

Where are you getting this information?

Isoaminile has no oxygens or sulfurs, and is an opioid:

203px-Isoaminile.png


Same thing with Lefetamine:
203px-Lefetamine.svg.png



and MT-45:
203px-MT-45_svg.svg.png


and MCOPPB:

203px-MCOPPB_structure.png

Diethylthiambutene is an opioid, no oxygens whatsoever, no di-oxide-sulfurs either, but two (separate) sulurs:

203px-Diethylthiambutene_structure.svg.png


also check out Tipepidine:

203px-Tipepidine.svg.png


Thiambutene:

203px-Thiambutene.png




I think you see oxygens, because oxygens are in most large-to-small molecular compounds, period. It's mostly 3D steric considerations that work for any molecule, excluding electron donating or accepting groups which can be various things, hydrazones can be covalent bonds, etc. that are the contributing factor to what binding site will be activated by a specific molecule drug-like compound. Opioid or not.
 
NIce, I just know the classic, morphine derived opiates, all have Oxygen'(s) and Nitrogen in specific positions for qsar.
And it seems that the few yoo have listed are exceptions, not rules, as 98% of the opiates will have to have specific configuration of Nitrogen and Oxygen'(s) to fit the opiate recepter - the same time of molecules, in similar places, as the endogenous opiod peptides, to fit the QSAR.
 
And the exceptions that you listed seem to be weaker opiods, and could possibly undergo metabolism that added needed oxygen atoms for effect.
 
ACTUALLY A LOT OF THOSE YOU LISTED ARE NOT OPIATES AT ALL: Isoaminile - NOT Tipepidine -NOT , I am having a hard time finding one of the molecules you listed as being an actual opiod

Besides the tiniest class of opiates, Thiambutenes, which have a few, week, non-oxygen containg opiates, which could VERY WELL be active due to metabolism into something that DID contain oxygen(s) in the appropriate place.

IF YOU LOOK AT A GENERAL QSAR FOR OPIATES, YOU WILL SEE OXYGEN(S) AND NITROGEN NEEDED.
 
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Thought isoaminile was an opioid, or am I barking up the wrong tree?


Nitrogen ain't needed, look at herkinorin, not a nitrogen in sight in this funky mofo of a terpenoid.
 
Limpet_Chicken said:
http://www.entheology.org/edoto/anmviewer.asp?a=90&z=5


Here is another cyanide-filled plant used as a psychotropic, the native name is 'koribo' and many shamans have ended up paralyzed from the waist down as they get older, due to repeated cyanide ingestion causing neurological damage. The plant is full of HCN.
Click to expand...
The HCN probably isn't responsible for the neurological damage. The plant is roasted before use, which would remove most of the cyanide. In the literature about the plant, ethnopharmacologists think there may be a neurotoxin present.

Additionally, the symptoms of paralysis induced by chronic cyanide exposure (Konzo, for example) are not confined to the legs
 
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