Hammilton
Bluelighter
- Joined
- Sep 2, 2008
- Messages
- 3,435
Since I started looking into the development of semi synthetic mitragynine analogues and their probable inclusion in some products, I got to looking into what could be used, and while MPI seems fairly likely because it's 30x stronger than morphine, there are other possibilities.
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3714104/
This study looks at some of them and its full text for free, so please give it a look, I've not finished it yet, but immediately an additional compound comes to mind.
Assuming that the methoxy substitution functions similarly to the analogous methoxy on codeine, it's possible that mitragynine is a prodrug for o-desmethylmitragynine, which would help explain the efficacy of the plant despite mitragynine's low potency and the very low levels of 7-OH-mitragynine. Also it's worth noting that o-desmethylmitragynine is a known metabolite in humans.
If it follows a pattern similar to codeine - morphine, you'd expect o-desmethylmitragynine to be ten times stronger than the parent. I'm not sure what the mit to morph conversion is, but for 7-OH-mitragynine to 7-oh-o-desmethylmitragynine you could be looking at something possibly 170x stronger than morphine. 300x for the same mod done to MPI. Of course the numbers won't work out so perfectly, but if I were testing these on myself that's where I'd be starting from.
The synthesis for all of these things seem to be quite accessible, making these likely targets for someone skilled at doing extractions and capable of the fairly easy syntheses. At, say, 2 percent mitragynine a kilo gives you 2 grams pure mitragynine. If you're able to turn that into something even 50x stronger than morphine, and orally active, that could be the equivalent of 1000 100mg doses of morphine. It's easy to see why such extracts would be pursued. If they retain the safety profile of whatever is indeed in UEI they should be immediately studied by a pharmaceutical company looking into safer opioids. One can only hope that they do, but opioids with good safety profiles and limited effect on respiratory depression are known, the metopon derivative springs to mind immediately and for some reason its modification reminds me of the 7-OH.
Does anyone else have mitragynine analogue SAR speculation or comment on the article? This is one of the few opioid SAR areas that interest me any longer, and not for personal use, they just haven't been studied all that much despite being natural. Were I a pharmaceutical company I'd be interested, the production of mitragynine is fairly cheap and not exactly labor intense, unlike opium, and unlike opium poppies, these provide year round harvests. Start a plantation and harvest the leaves as they grow. I would think the fertilizer use would be limited and you could start a plantation in the southern US if you wanted, which can't be done for opium.
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3714104/
This study looks at some of them and its full text for free, so please give it a look, I've not finished it yet, but immediately an additional compound comes to mind.
Assuming that the methoxy substitution functions similarly to the analogous methoxy on codeine, it's possible that mitragynine is a prodrug for o-desmethylmitragynine, which would help explain the efficacy of the plant despite mitragynine's low potency and the very low levels of 7-OH-mitragynine. Also it's worth noting that o-desmethylmitragynine is a known metabolite in humans.
If it follows a pattern similar to codeine - morphine, you'd expect o-desmethylmitragynine to be ten times stronger than the parent. I'm not sure what the mit to morph conversion is, but for 7-OH-mitragynine to 7-oh-o-desmethylmitragynine you could be looking at something possibly 170x stronger than morphine. 300x for the same mod done to MPI. Of course the numbers won't work out so perfectly, but if I were testing these on myself that's where I'd be starting from.
The synthesis for all of these things seem to be quite accessible, making these likely targets for someone skilled at doing extractions and capable of the fairly easy syntheses. At, say, 2 percent mitragynine a kilo gives you 2 grams pure mitragynine. If you're able to turn that into something even 50x stronger than morphine, and orally active, that could be the equivalent of 1000 100mg doses of morphine. It's easy to see why such extracts would be pursued. If they retain the safety profile of whatever is indeed in UEI they should be immediately studied by a pharmaceutical company looking into safer opioids. One can only hope that they do, but opioids with good safety profiles and limited effect on respiratory depression are known, the metopon derivative springs to mind immediately and for some reason its modification reminds me of the 7-OH.
Does anyone else have mitragynine analogue SAR speculation or comment on the article? This is one of the few opioid SAR areas that interest me any longer, and not for personal use, they just haven't been studied all that much despite being natural. Were I a pharmaceutical company I'd be interested, the production of mitragynine is fairly cheap and not exactly labor intense, unlike opium, and unlike opium poppies, these provide year round harvests. Start a plantation and harvest the leaves as they grow. I would think the fertilizer use would be limited and you could start a plantation in the southern US if you wanted, which can't be done for opium.
