Comment · Mon, April 20, 2020
Any chance of offering kappa antagonist in your store?
Original post in this thread
Azetinho · 8 points
Hello!
It’s a pity that there’s no easy way to obtain a potent kappa-opioid antagonist on the market. There are a bunch of compounds such as Norbinaltorphimine, JDTic or CERC-501 but none of them can be bought in traditional way. I know that there are probably some obstacles but Nor-BNI seems like a good candidate to offer. There’s such a big potential in these noots for uplifting mood, reducing anhedonia and dissociation.
What they were answering
CyberTheBoss · 3 points
Even if it were listed as something that blocked opioid receptors? If it's a synthetic compound that's the issue I urge you to look at this paper, which lists some flavonoids and derivatives with kappa antagonistic properties https://doi.org/10.1021/np070194x, though these flavonoids like amentoflavone don't cross the BBB well without assistance (hint hint). Likewise, consider Pawhuskin A (https://en.wikipedia.org/wiki/Pawhuskin\_A), which is a constituent of Dalea Purpurea. In this paper (https://dx.doi.org/10.1021%2Fnp4009046), compound 29 is of particular interest having significant selectivity for the kappa opioid receptor and negligible affinity for other opioid receptors, and it wouldn't be the first time a semi-synthetic analog of a natural plant constituent hit the market as a major supplement.
If semi-synthetic is pushing it too far, a BBB-permeable formulation of amentoflavone from Ginkgo Biloba and St John's Wort, both incredibly common supplements, whose major method of action could be advertised as an energizing agent by blocking the benzodiazepine site among other effects would be a worthy place to start. Amentoflavone binds to the kappa opioid receptor selectively compared to other opioid receptors, and it's already sold in every super…
u/MisterYouAreSoDumb
Yeah, I read that paper. We have been working on solutions to this from the natural side for a while. I was specifically talking about the synthetic ones OP was suggesting. We are doing a lot of R&D in the background on tons of different things. We have a few products that we have been developing for a few years now that are in the process of being patented. We are just sticking to natural products for those efforts.