More illumination has been shed on the U-series!
You will come to find out in further research with the U-compounds that they differ from one another significantly. While they all share a similar structure, in effects they vary drastically particularly in the therapeutic index & toxicity profile! The team at UpJohn university was working to create the holy grail of analgesics! I've gathered this very reliable information from several places.
- U-50488 is a pure kappa agonist with a structure similar to that of U-47700
- U-47 is the lead compound of selective kappa ligands such as U-50488 & U-69, U-593 with similar structures
- The U is derived from UpJohn - which later merged with Ciba
More on this I posted in the thread on U-51754, and I had to post it on here as well in case others wouldn't be interested in looking at that other thread! I did it as my duty to harm reduction as well I'm hoping others would have done the same with a very new chemical that can have devastating effects not unlike those of Krokodil! Hopefully it doesn't but knowledge is power & its our duty to share this knowledge. I know in the opioid circles esp. in the RC scene people have tendency to stay quiet b/c they are afraid of 'blowing the whistle' & ruining it forever for everybody, but in some cases like with MT-45, we could have known a little earlier. Also this is the point - by the time you find out what the side effects are, its already too late!
http://www.bluelight.org/vb/threads/793107-Novel-opioid-U-51754?p=13716730#post13716730
You will come to find out in further research with the U-compounds that they differ from one another significantly. While they all share a similar structure, in effects they vary drastically particularly in the therapeutic index & toxicity profile! The team at UpJohn university was working to create the holy grail of analgesics! I've gathered this very reliable information from several places.
- U-50488 is a pure kappa agonist with a structure similar to that of U-47700
- U-47 is the lead compound of selective kappa ligands such as U-50488 & U-69, U-593 with similar structures
- The U is derived from UpJohn - which later merged with Ciba
"U-47700 is the result of a great deal of work elucidating the quantitative structure–activity relationship of the scaffold. The team looked for the key moieties which gave the greatest activity. Upjohn posted over a dozen patents on related compounds, each optimizing one moiety until they discovered that U-47700 was the most active.
U-47700 became the lead-compound of selective kappa ligands such as U-50488 and U-69, U-593, which share a very similar structure (a single methylene spacer difference). Its structure lead to other chemists experimenting with it to see if rigid analogues would retain activity."
Although not used medically, the selective kappa ligands are used in research.
U-47700 has never been studied in humans, but would be expected to produce effects similar to those of other potent opioid agonists, including strong analgesia, sedation, euphoria, constipation, itching and respiratory depression which could be harmful or fatal. Tolerance and dependence would be expected to develop. Since affinity to kappa receptors has not been measured, it may also induce dysphoria and other unwanted side-effects but it’s 3DQSAR, make it this most unlikely. Its structure is somewhat similar to U-50488, a pure kappa agonist."
More on this I posted in the thread on U-51754, and I had to post it on here as well in case others wouldn't be interested in looking at that other thread! I did it as my duty to harm reduction as well I'm hoping others would have done the same with a very new chemical that can have devastating effects not unlike those of Krokodil! Hopefully it doesn't but knowledge is power & its our duty to share this knowledge. I know in the opioid circles esp. in the RC scene people have tendency to stay quiet b/c they are afraid of 'blowing the whistle' & ruining it forever for everybody, but in some cases like with MT-45, we could have known a little earlier. Also this is the point - by the time you find out what the side effects are, its already too late!
http://www.bluelight.org/vb/threads/793107-Novel-opioid-U-51754?p=13716730#post13716730
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