New opioid, PZM21; pain killing without raising tolerance.

[Nagelfar]

DOI: 10.1038/nature19112

 

[aced126]

Thanks for sharing

 

[Solipsis]

Wow, almost looks like you could make 12 from methiopropamine (yeah wrong connectivity), meth (yeah the dimethyl) and ureum...
The urea group novelty is a nice twist anyway. What would making the urea amines (or one of them) tertiary do, what is the influence of that on the binding properties of the carbonyl and its intended function for H-bonding?

Am curious to see more about this G_i vs beta arrestin 2 pathways and effects in humans of biased MOR agonists.

Thnx

 

[solidsnake77]

Somebody knows when this will be comercialized approx on a international level? It's quite interesting for who living with chronic pain and don't want back to opiates, like it's my case.

 

[Nagelfar]

My question is, is the very last plate from the article a misprint? It says "N.D." is 'not determined', and "N.A." is no activity, but one of the "N.A."s (the important one, the beta arrestin recruitment ratio) is called "not determined", now, that would be some witty juggling in a paper that is trying to somehow insinuate a drug has no affect on arrestin when it does by omitting testing for it, but from what the article claims, it should say no activity.

 

[Solipsis]

My question is, is the very last plate from the article a misprint? It says "N.D." is 'not determined', and "N.A." is no activity, but one of the "N.A."s (the important one, the beta arrestin recruitment ratio) is called "not determined", now, that would be some witty juggling in a paper that is trying to somehow insinuate a drug has no affect on arrestin when it does by omitting testing for it, but from what the article claims, it should say no activity.

It isn't "not determined", check figure 3g and you will see the screening for beta arrestin recruitment and PZM-21 indeed showing no detectable effect. If the legenda for N.A and N.D isn't consistently 'no detectable activity' and 'not determined' respectively it would be a pretty big mindfuck.

"Yeah let's occasionally say no detectable activity with the reason being that we just didn't even measure it. Preferably when the subtitle compound is concerned."
- no one ever, let's hope.

 

[Nagelfar]

"Yeah let's occasionally say no detectable activity with the reason being that we just didn't even measure it. Preferably when the subtitle compound is concerned."
- no one ever, let's hope.

lol

...still, either way, I found a misprint. My mother always told me I should be a proof-reader for a newspaper.

 

[Solipsis]

My mother always told me I should be a proof-reader for a newspaper.

Maybe you read too much into that?

jk a quirk like that was definitely worth double checking!

 

[S.J.B.]

Bump... this one's still "in the pipeline," might come up again.