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Pharmacology In the Pipeline

This thread contains discussion about a Pharmacology-related topic
Ask him about the 'fluorine azide' or better - man who can tell a good story.
 
Markush structures - could be thousands of things. This annoys me and as a rule-of-thumb, the more structures you cram into one patent, the weaker the legal protections around a specific member of that HUGE groups.

Empathbio is wholly owned by ATAI Life Sciences., itself now owned by AltiBeckley. Is it a patent zombie? Well, hard to fathom the inner workings but we ALL know that the Don AOKed entactogens and psychedelics for treatment of mental health so if nothing else, the stock price will go up as we WILL see a bubble. Hacking down who has what is a nightmare.
 
@charlz - I think someone posted the actual papers a few weeks ago and it certainly is interesting. I keep wondering if this could also be explained as a demonstration of a duelist as no mention is made of the NOP receptors which being very similar to the MOR receptor, was only accidentally discovered by Janssen in the 1960s who could not explain the analgesia of a ligand that by rights should not have been as good as it appeared to be. Of course, he then went on record as saying that the scaffold and those related to it were so synthetically challanging that a decision was made to focus on the phenylpiperidine class i.e. phenoperidine --> fentanyl --> carfentanil/alfentanil/remifentanyl i.e. focus on medications for the 'head of the table' i.e. anesthetists.

It wasn't pure pragmatism but the 3,3-diphenylheptanones were still yielding new medicines BUT it ended up with Janssen's new medicines only competition was other Jannsen medicines.

If you look at the code numbers you can at once see just how deeply he mined both scaffolds but equally note how those numbers thin out. If you wish to, you can draw a graph to see just how thinned out it all became.

He was only pipped at the post as greatest Belgian in history because the poll was a Flemish (regional) TV programme. But being runner-up to a saint is possibly a division between faith and science. Only post mortem was he was awarded Most Important Belgian Scientist. I contest he did more good but that's just one opinion.

I suspect his incredible productivity was in pipelining the development i.e. rational design, Dreiding molecular models, intuition, serendipity and as with all things, sheer hard work. Design, hand off to team, test, iterate, repeat. IF you do that at speed you CAN go quite fast. I don't think any faster would have been safe, and from the little I know of the man, he did consider the end user; rare.
 
4DQSAR said:
https://www.science.org/blogs/pipeline

Derek Lowe, genuine genius, gentleman and gentle man... also hilarous.

IF you REALLY wish to become a medicinal chemist, follow this person. The HTMA story alone is worth it.
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I’ve read this blog daily since 2012. Honestly has helped me catch papers beyond the journals I focused on.

Derek is amazing at writing about science in a way that is easily digestible by lay folk, but also avoids the lies to children a lot of science communicators fall into.
 
I read the quick one about heart cells and cancer. I like how simply he explains things. The stuff he writes about sounds like important stuff, if only I knew more of the terms.
 
streaM Freak said:
I read the quick one about heart cells and cancer. I like how simply he explains things. The stuff he writes about sounds like important stuff, if only I knew more of the terms.
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His posts “things I wouldn’t work with” are a great exploration of some wild chemistry.


I also thought this article is quite interesting regarding how cells make sure that cell death inducing proteins can function even in the face of catastrophic cellular damage.

 
Thomas M. Klapötke - such an odysseian researcher, if you get my drift.
 
@charlz - We did discuss this elsewhere but I suggest what is MORE important is to know if this novel ligand stops AWS. I believe there are fentanyl derivatives that act primarily on the periperal opate receptors and similarly are said to provide analgesia without the associated dangers (specifically respiratory collapse).

I've mentioned it elsewhere but I suspect the model of fentanyl dependence seems somewhat different to that of longer-acting ligands. The 'plastic euphoria' is, in truth, simply contrast. If you are rattling within a few hours, yes, by comparison you WILL feel euphoria mediated by the body adjusting to the drug being required for survival so just as eating, drinking, sex release a small amount of dopamine to 'program' a person's behavior to seeking more, so fentanyl dependence programs users and reward them as if it were a basic need for survival.

It seems so far removed to how WSB described how after using morphine, it's akin to having a good meal i.e. the user doesn't focus on the next dose until they actually want it and the NEED only comes when the AWS hits with with M is generally around 12 hours.

It's also mentioned in the autobiography 'Unforgiving Destiny' by David McMillan that opioids get more 'euphoric' when physical dependence is present. One Swedish dealer apparently asking why non-dependent users even consume the stuff.

Since I live in the UK, I understand WHY diamorphine is still in the BNF. It's described as being able to confir 'mental detachment' in patients who have no experience of opioids. Which does strongly suggest that some opioids are euphoric in the absence of physical dependence.

For what it's worth, I was prescribed fentanyl patches and felt no subjective effects whatsoever and was even given it before several surgeries and again nothing. But one person has no statistical value. I just sense that either a user has to get very close to a fatal dose to feel ANYTHING or a user has to be suffering AWS and the body releases dopamine to signal the NEED.

I just know that every single time a 'none abusable' opioid has turned up, as long as it stops AWS, it has been abused. Every time it's something worse. I mean, nobody eats 200 loperamide if they have the option of taking something else but in high enough doses it overcomes the active transport so becomes centrally active. A terrible and dangerous idea but if it halts AWS, that seems to be enough.

BTW along with the primate study in which place-prefence showed higher animals would still choose S-17018, there is an earlier rodent study which I will locate and upload a hyperlink for you.
 
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