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Propofol and Analogues?

yes your math is about right for the rat extrapolation and while 2g was advised based on a given MSDS and caution on the conservative side is always well advisable with an unknown the number indicated via the mouse extrapoaltion of about 53mg/kg is indeed related to what i noted above at roughly 3000-4000mg for an average human so >10g is well not advisable as a safe figure
 
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LuxEtVeritas said:
uh, ........ ^ -- the below shows somewhere around ~10-15%
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Huh, my source must be wrong then. I admit not looking very hard (I was getting ready to go see A Prairie Home Companion @ The Minnesota State Fair.

Garrison Keillor was everything I ever dreamed of and more (though this is not my first time I've seen him live, actually not even the first state fair edition)
 
Here's a really interesting propfol pro-drug I want to find some more info on.

XP20925

I don't know what it is exactly, other than that it's intended to make use of intestinal transporters to get it in the body. It's intended for the treatment of migraine and (oddly) chemo-vomiting.
 
It's intended for the treatment of migraine and (oddly) chemo-vomiting.
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Interesting, as thymol is evidently an effective antiemetic; it must have something to do with endogenous cannabinoids...
 
Does anyone here know anything about honokiol or magnolol? I was scrolling around through the various phenol derivatives at Wikipedia, looking for any with GABAergic activity, and I came across these two. I guess that (at least the former) has had pretty widespread commercialization already. A Google search for Honokiol pulls up 54,000 results, and a bunch of Google-Ads on the right.

Here's a study I found on these two:

Honokiol and Magnolol Selectively Interact with GABAA Receptor Subtypes in vitro
Jinglu Ai, Xiaomei Wang, Mogens Nielsen

Department of Psychopharmacology, Research Institute of Biological Psychiatry, St. Hans Hospital, Roskilde, Denmark

Address of Corresponding Author

Pharmacology 2001;63:34-41 (DOI: 10.1159/000056110)

goto top of page Key Words

* Honokiol
* Magnolol
* GABAA receptors
* Subtype selectivity

goto top of page Abstract

Honokiol and magnolol have been identified as modulators of the GABAA receptors in vitro. Our previous study suggested a possible selectivity of honokiol and magnolol on GABAA receptor subtypes. This possibility was examined in the current study by 3H-muscimol and 3H-flunitrazepam binding assays on various rat brain membrane preparations and human recombinant GABAA receptor subunit combinations expressed by the Sf-9/baculovirus system. Generally, honokiol and magnolol have a similar enhancing effect on 3H-muscimol binding to various membrane preparations in nonsaturation binding assays. Honokiol and magnolol preferentially increased 3H-muscimol binding to hippocampus compared to cortex and cerebellum (with a maximum enhancement of 400% of control). As for subunit combinations, honokiol and magnolol have a more potent enhancing effect on alpha2 subunit containing combinations (with a maximum enhancement of 400-450% of control). This action was independent of the gamma subunit. In saturation binding assays, magnolol affected either the number of binding sites (ca. 4-fold on alpha2 containing combinations) or the binding affinity (on alpha1 containing combinations) of 3H-muscimol binding to various GABAA receptor subunit combinations. In contrast, honokiol increased only binding sites on alpha2beta3gamma2s and alpha2beta3 combinations, but both the number of binding sites and the binding affinity on alpha1beta2gamma2S and alpha1beta2 combinations. These results indicate that honokiol and magnolol have some selectivity on different GABAA receptor subtypes. The property of interacting with GABAA receptors and their selectivity could be responsible for the reported in vivo effects of these two compounds.

Copyright © 2001 S. Karger AG, Basel

Anyone have access to this particular paper?
 
yes, they are fine, reasonably solid anxiolytics, nothing special...used them quite a long ways back and moved to better

i have a few extractions that are for said purpose probably dead on best stuff you can want for such...and working on one that i think is hopefully even more up your alley (more hypnotic) =D
 
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