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Salvinorin-A analogs

MattPsy

Bluelighter
Joined
Jan 15, 2006
Messages
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Just came across this a little while ago, got me pretty interested.

SalvAkappaanalog.gif


(I've put the two structures next to each other for easy comparison)

Here's an abstract: Synthesis and in vitro pharmacological studies of new C(2) modified salvinorin A analogues
What do you think about these type of compounds in terms of their psychedelic effect, and their future? Sally-A is certainly unlike any other psychedelics i've tried, which isn't at all surprising (duh) since it works it's magic at the opiate kappa receptor, rather than the more traditional 5-HT2A or NMDA.
One of the more interesting things about Salvinorin-A is that it seems to exhibit reverse-tolerance...
 
Well, considering Salvinorin-A has threshold-slight effects at around 350 micrograms, I would say about 1/7th that dose would be required.

HOWEVER

Just because a ligand shows a higher binding affinity doesn't mean it'll actually BE 7 times more potent. However, when one compares the binding affinities of 5HT2A ligands and their required dosages in the human, it IS actually quite scaleable. Don't know if this too will be the case with these Kappa-agonist ligands.

I'd like to try them out :) (as i'm sure quite a lot of you lot would too, actually ;) ).
 
Wouldn't that make it the most potent psychadelic known? I think I'd be scared to ingest this stuff.....if you know the potency, does that mean you know the legnth of duration?
 
I think Salvinorin can be enjoyable only because it's very short acting....
Long-acting kappa agonists like Pentazocine or Nalbuphine (which is a partial agonist) can be dysphoric, unpleasant...
 
And it looks a bit more stable as there is one ester group less
 
Yeah, I certainly wouldn't want to be the first to try it; Salvia scares the shit out of me, and we all know how short a time it lasts!
Much of the really potent 5HT2A agonists like the 2,5-dimethoxy-amphetamines (DOB, DOI and the like) are really long lasting. Not sure on the difuran analogs of these - the FLY and DFLY compounds- how long do they last again? Those are much more potent than than DOB though, and there are ones stronger than those DFLY ones anyway, heh :) .

Personally, I get sick of tripping after about the 6th hour, no matter how amazing, weak, strong, intense etc the trip may be. I would hope the above Kappa agonist wouldn't last long. Just from the structure of it however, i'd say it'd be metabolized pretty rapidly.
 
I would kill to get my hands on a salvia analogue. Maybe not kill, but at least volunteer myself as a guniea pig.
 
MattPsy said:
Personally, I get sick of tripping after about the 6th hour, no matter how amazing, weak, strong, intense etc the trip may be.

i am the same.

so i always keep risperidone, or chlorpromazine in my pocket when tripping, and if something bad happens, or it is no fun anymore, then i just take an anti-psychotic, and 30-60 minutes later i feel totally straight.

I just got Zyprexa (olanzapine) from a friend, so i will keep that in my pocket instead cause i heard it is much better than the older anti-psychotics.

Also having zanax in the pocket is really good cause if something upsets me but i want to keep tripping, i just take 1 zanax and i feel good and relaxed, but still a bit trippy - it stops the circular loop thinking.

i also dont smoke dope anymore on trips cause it gets too messy by the end.
 
I was reading some stuff Shulgin wrote from 2002 and someone asked him about future possibilities in new psycdelic discoveries and he mentioned Salvinorin A would be a good candidate (LINK)

Shulgin
“But consider the structure of Salvinorin A, the active component of Salvia divinorum. It presents a treasure house of sites just begging to be chemically modified. There is an acetic acid ester that has been removed by hydrolysis and successfully replaced. What about other esters such as a formate or a propionate? There is a carboxylic acid methyl ester there. Maybe the ethyl or the propyl ester homologues might be interesting. Remember that the parent compound is active in man at less than a milligram total dose -- these minor modifications might very well change both the potency as well as the nature of its effects.”
 
Where do you start when you're playing with ultra potent salvinorin analogues? When 50ug is likely a threshold dose, how much lower do you start for safety.
 
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