RCs Novel opioid U-51754

[muie]

New Information On U- Series

To the OP, structurally nearly identical yes, but as you will come to find out in any further research with the U-compounds, that while they all have a similar structure but in effects they vary drastically particularly in the therapeutic index and 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, one link is provided as reference for further reading.

- 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."

Source:
https://rcwatch.wordpress.com/2015/...nyl-acetyl-fentanyl-parafluorobutyr-fentanyl/

*Imagine if MT-45 had been as euphoric & easily available!*

By the time we would have gotten in this far both in respect to with time & frequency, *it would make Krokodil look like child play*
Think, how long has the U series been around guys? Almost 8 - 10 months, lets say 1yr, right...now think of how many hundreds of grams have been used in that period! Hopefully more knowledge will be illuminated on the pharmacokinetics & pharmacology of this class of compounds before everybody gets excited & it too late!


p.s. just learned how to use quotes & been posting since 01 (advanced, look where u align the text like in Word, there's 'quotes', its formatted automatically in Italic)

 

[roi]

That quote is copied from wikipedia

But yeah, that extra methylene spacer leads too much more kappa activity.