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question on Salvia D2 receptor agonism

golden1

Bluelighter
Joined
Oct 12, 2009
Messages
186
Salvinorin A
Research has shown that salvinorin A is a potent κ-opioid receptor agonist.[2] It has been reported that the effects of salvinorin A in mice are blocked by κ-opioid receptor antagonists.[6] This makes it unlikely that another mechanism contributes independently to the compound’s observed effects in mice.[original research?] However, salvinorin A has recently been found to act as an even more potent D2 receptor partial agonist, with an affinity of 5-10 nM, an intrinsic activity of 40-60%, and an EC50 of 50-90 nM, which is several-fold higher than its EC50 of 235 nM for the κ-opioid receptor.[7] This suggests that the D2 receptor may also play an important role in its effects.[7]
-- http://en.wikipedia.org/wiki/Salvinorin_A

Thinking about it I do feel like I may have felt an weird dopamine like undertone to the experience especially on lower doses. Anyone notice this too? What effects do you think are from the D2 partial agonism?

I think the dissasociative state and general fear reaction are from the kappa receptor, but I have to wonder how much it is colored by the D2 receptor especially since it may even be noticeable at low doses. any thoughts are welcome

:)
 
Yeah, Salvinorin A is pretty damn selective (for the Kappa Opiod). Interestingly, it has been shown that it stimulates the activity dopamine transporter down stream of activating the KOR. I don't know if that has anything to do with anything though.
 
what are D2Long and D2High receptors? I realize that just about all of these receptors are more complicated that D1, D2, etc, but D2Long D2Short D2High??? all news to me.
 
I just can add to this the knowledge of that Naltrexone (and naloxone, I guess) were enough to blockade the effects of salvia and salvinorina.

The psychologist and neuro-scientist Jose Carlos Bouso (if I remember the right one who informed about) that long time ago began the studies about the use of MDMA as pharm to help in the therapy process in Spain, was the one who bio-assayed himself till that conclusion.

The source is a trustworthy person (see MAPS reference link) with a lot of work done in the area of psychedelic drugs (not only, but mainly).

Maybe I'm saying something that is perfectly known (as I mean to a communication about two years ago) or maybe that info is not as known as I have it in my mind.

If someone needs more info about this (I really don't know if that's accepted science nowadays ) I can take a look in some Spanish forums or (if needed) ask the man itself about that matter.

If I'm posting offtopic, my apologies.
 
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