• Neuroscience & Pharmacology Discussion Welcome Guest
    Posting Rules Bluelight Rules
    Recent Journal Articles Chemistry Mega-Thread
    FREE Chemistry Databases! Self-Education Guide

  • N&PD Moderators: Skorpio

maybe ketamine isnt as useful as we think?

Even a short-term effective treatment for suicidal thoughts that works in a large portion of patients is incredibly useful and rare. I think that you are really underestimating how powerful that can be to someone struggling with severe depression. I have used ketamine a few times when at/near rock bottom and it has honestly most likely saved my life.

EDIT: Ketamine + therapy/usual treatment had a 63% effectiveness rate for full remission of suicidal thoughts vs. 32% for saline + therapy/usual treatment. That is HUGE.
 
If you ask me, ket indeed isn't the best useful antidepressant, it's kinda the worst arylcyclohexylamine you could find for that. It's impotent, urotoxic, short-lived etc. Let's test MXE and you'll see a 85% full remission of suicidal thoughts in a matter of hours. Just, to sustain this, one needs to do chronic bumps every few days, which isn't guaranteed/possible yet afaik.
 
plumbus-nine said:
If you ask me, ket indeed isn't the best useful antidepressant, it's kinda the worst arylcyclohexylamine you could find for that. It's impotent, urotoxic, short-lived etc. Let's test MXE and you'll see a 85% full remission of suicidal thoughts in a matter of hours. Just, to sustain this, one needs to do chronic bumps every few days, which isn't guaranteed/possible yet afaik.
Click to expand...
It was chosen because it is already widely-produced and used medically, well-studied, and likely has a lower risk of triggering mania in bipolar people (40-60% of those with mood disorders are bipolar) than other dissos such as MXE would.
 
arrall said:
It was chosen because it is already widely-produced and used medically, well-studied, and likely has a lower risk of triggering mania in bipolar people (40-60% of those with mood disorders are bipolar) than other dissos such as MXE would.
Click to expand...
Yeah, I know the point about K being already widely used medicinally (even when it's like a total different drug when used at threshold dosages vs anesthetic ones) which will probably aid fast approbation in many countries but MXE isn't exactly the most mania inducing disso, and there are two or three papers stating acute and sustained antidepressant effects, in, granted, mice. But these two features, NMDAr antagonism and SERT blockade, in one molecule makes it a good candidate. E.g. 3-MeO-PCx would be the candidate for mania. When it's about relieving suicidality, you want a certain amount of hypomania.
 
Maybe usefulness isn't as useful as we think.

Maybe awesome is good enough (by far).
 
I suppose ketamine is used because it has already been licenced for other medical uses. MXE or indeed any other NMDA ligand would require a regulatory pathway that could easily take 10-15 years.

Lanicemine - World Patent 9320052 is a typical example of rigid endpoints to decide on the continued development of a medicine. If it's only effective for 25% of people but it works WONDERFULLY for that 25%, it will still be dropped. I have seen this again and again.

I almost think that somebody wrote the structure down incorrectly & the pyridine ring should be the 1-aryl moiety. It also would have been interesting to try alkylating the amine. I discovered that the N-methyl & N-ethyl do not produce typical K-like effects. The pyrrolidine & piperidine analogues were dull and it was only the N-isopropyl that had significant NMDA & DRI activity - put simply, VERY like MXE if not as potent weight for weight.
 
Feretile said:
Lanicemine - World Patent 9320052 is a typical example of rigid endpoints to decide on the continued development of a medicine. If it's only effective for 25% of people but it works WONDERFULLY for that 25%, it will still be dropped. I have seen this again and again.
Click to expand...
Yeah. unfortunately. I even saw lanicemine available from some RC supply but it was too expensive for me to try it, but it sounds very promising to me. Just from skimming through wikipedia I found quite a few such candidates which were dropped all over, instead they license the x-th SSRI (vortioxetine) or D2 partial agonist (granted, these are an improvement over the antagonists but they could do better today imo).

Feretile said:
I almost think that somebody wrote the structure down incorrectly & the pyridine ring should be the 1-aryl moiety. It also would have been interesting to try alkylating the amine. I discovered that the N-methyl & N-ethyl do not produce typical K-like effects. The pyrrolidine & piperidine analogues were dull and it was only the N-isopropyl that had significant NMDA & DRI activity - put simply, VERY like MXE if not as potent weight for weight.
Click to expand...
Would love to sample this. But even if they care to make it, price is prohibitive nowadays given my permatolerance to dissociatives. New synths are easily 3x the price of good old MXE and I need like 5-10x the amount, so it's a 15-30-fold increase for me.
 
plumbus-nine said:
Yeah. unfortunately. I even saw lanicemine available from some RC supply but it was too expensive for me to try it, but it sounds very promising to me. Just from skimming through wikipedia I found quite a few such candidates which were dropped all over, instead they license the x-th SSRI (vortioxetine) or D2 partial agonist (granted, these are an improvement over the antagonists but they could do better today imo).


Would love to sample this. But even if they care to make it, price is prohibitive nowadays given my permatolerance to dissociatives. New synths are easily 3x the price of good old MXE and I need like 5-10x the amount, so it's a 15-30-fold increase for me.
Click to expand...
Did you ever get chance to try isophenidine? It was WAY better than diphenidine, methoxyphenidine (not my design & killed people) or ethylphenidine.

It was not a potent as MXE by weight, but the effects were the same.

1 SIMPLE RT chemical synthesis step. So why was it not huge. Because the company we set up had bought 200L of piperidine and they came up with RUBBISH reasons why they could not make isophenidine. The truth was 'because we aren't very good; was not mentioned.I
I stole the route from a sertralone--->sertraline patent. I wanted to find the cheapest reductive amination so I spent 50 hours going through ALL the patents. IF I could post route, I would. Easier & safer than making meth,



BTW toon to cheer you up.
 
You must log in or register to reply here.
Top