Ritanserin - Serotonin Antagonist For R&D Use Only

[haidut]

Checking a few posts back, it's not in stock.

It's not in stock currently. Also, if you look at the other posts I am not very keen on keeping selling it as there is not much unique effect to it and Peat is concerned about the fluorine molecules in it.

 

[chimdp]

@haidut Quick question for you. Trying to make sure I'm understanding the Ki numbers. For Ritanserin on wikipedia it says "The affinity of ritanserin for the 5-HT1A receptor is less than 1 µM" Does this mean that ritanserin has little effect there compared with something with a low Ki measured in nM say 20 nM? Or more specifically does the 1 micromolar unit Ki for ritanserin mean the drug has less effect or binding affinity there than say Buspar which is an agonist for the 5-HT1A receptor at a Ki of 20nM?

 

[haidut]

@haidut Quick question for you. Trying to make sure I'm understanding the Ki numbers. For Ritanserin on wikipedia it says "The affinity of ritanserin for the 5-HT1A receptor is less than 1 µM" Does this mean that ritanserin has little effect there compared with something with a low Ki measured in nM say 20 nM? Or more specifically does the 1 micromolar unit Ki for ritanserin mean the drug has less effect or binding affinity there than say Buspar which is an agonist for the 5-HT1A receptor at a Ki of 20nM?

I think I answered over PM, so if you want please post the response here.

 

[chimdp]

I think I answered over PM, so if you want please post the response here.

Response from haidut...

I think the Ki is more reliable than IC50 as it shows both effect and structural match (i.e. receptor fit/binding). So, a higher Ki (1uM) means weaker effect AND binding than a lower Ki (20nM).

What is an inhibitory constant (Ki) and how does it relate to understanding drug interactions?

"...The inhibitory constant (Ki) and the IC50 of a drug that is known to cause inhibition of a cytochrome P450 (CYP) enzyme have to do with the concentration needed to reduce the activity of that enzyme by half. More specifically the Ki is reflective of the binding affinity and the IC50 is more reflective of the functional strength of the inhibitor for a drug. Since the Ki takes into account the IC50 is its calculation, the Ki is being reported more often by drug companies. "

 

[ddjd]

@haidut is Ritanserin the strongest h1 antagonist you offer apart from cypro?

 

[haidut]

@haidut is Ritanserin the strongest h1 antagonist you offer apart from cypro?

We don't have ritanserin any more. In the absence of it, ketotifen, doxylamine, cypro, and diphenhydramine are the most potent ones that are safe.

 

[VelvetNerves]

@haidut would you consider stocking a different (non flouridic) selective 5-HT2a antagonist? it's an important class of drug/treatment — especially for sleep — and the uniqueness is that it doesn't mess with dopamine/histamine/cholinergic etc., so no side effects/rebound (5-HT2a antagonism, by the good antagonists, actually leads to down-regulation which is what ones after while taking it anyway..)..

 

[haidut]

@haidut would you consider stocking a different (non flouridic) selective 5-HT2a antagonist? it's an important class of drug/treatment — especially for sleep — and the uniqueness is that it doesn't mess with dopamine/histamine/cholinergic etc., so no side effects/rebound (5-HT2a antagonism, by the good antagonists, actually leads to down-regulation which is what ones after while taking it anyway..)..

I try to stay away from selective antagonists but there is a chemical I am looking lately at that is a 5-HT2A/5-HT2C antagonist and GABA reuptake inhibitor. So, if I manage to find an affordable bulk vendor then I will release it.

 

[VelvetNerves]

I try to stay away from selective antagonists but there is a chemical I am looking lately at that is a 5-HT2A/5-HT2C antagonist and GABA reuptake inhibitor. So, if I manage to find an affordable bulk vendor then I will release it.

That's unfortunate, but fair enough. Any recommendations for a desperate pursuit to get ahold of one of the main 5-HT2a/c antagonists? Vendors you know of? Feel free to PM. Thanks!

 

[haidut]

That's unfortunate, but fair enough. Any recommendations for a desperate pursuit to get ahold of one of the main 5-HT2a/c antagonists? Vendors you know of? Feel free to PM. Thanks!

I can't recommend any vendors but here is the chemical I had in mind.
https://en.wikipedia.org/wiki/Deramciclane

You can try to buy it from major chemical vendors like Sigma or Tocris. It is NOT a controlled substance and it has no serious side effects in clinical trials on humans.

 

[Regina]

I try to stay away from selective antagonists but there is a chemical I am looking lately at that is a 5-HT2A/5-HT2C antagonist and GABA reuptake inhibitor. So, if I manage to find an affordable bulk vendor then I will release it.

 

[VelvetNerves]

I can't recommend any vendors but here is the chemical I had in mind.
https://en.wikipedia.org/wiki/Deramciclane

You can try to buy it from major chemical vendors like Sigma or Tocris. It is NOT a controlled substance and it has no serious side effects in clinical trials on humans.

Deramciclane isn't (https://link.springer.com/article/10.1007/s002130050544) one of the 5-HT2a/c antagonists/inverse-agonists that down-regulate the receptors (like many of the -anserins) so I'd have to take it permanently to keep getting the effect I need.

GABA-RI's also slowly down-regulate GABA, which is also very counterproductive for my needs.

 

[haidut]

Deramciclane isn't (https://link.springer.com/article/10.1007/s002130050544) one of the 5-HT2a/c antagonists/inverse-agonists that down-regulate the receptors (like many of the -anserins) so I'd have to take it permanently to keep getting the effect I need.

GABA-RI's also slowly down-regulate GABA, which is also very counterproductive for my needs.

Then you may want to try pizotifen. It is pretty similar in structure to cypro but does not seem to have the same risk of liver side effects.

 

[VelvetNerves]

Then you may want to try pizotifen. It is pretty similar in structure to cypro but does not seem to have the same risk of liver side effects.

Huh, why Pizotifen? I don't know much about it. From cursory googling I'm not seeing it being one of the down-regulating 5-HT2a/c antagonists, and on top of that it's anti-histaminergic (which isn't optimal, but I can throw a down-regulating inverse-agonist on top for safety) and anticholinergic (super.. suboptimal...; #brainrot).

I don't have binding affinity numbers in front of me yet though (still looking)... so I'll hold final judgement..

 

[haidut]

Huh, why Pizotifen? I don't know much about it. From cursory googling I'm not seeing it being one of the down-regulating 5-HT2a/c antagonists, and on top of that it's anti-histaminergic (which isn't optimal, but I can throw a down-regulating inverse-agonist on top for safety) and anticholinergic (super.. suboptimal...; #brainrot).

I don't have binding affinity numbers in front of me yet though (still looking)... so I'll hold final judgement..

Pzitofen does downregulate at least 5-HT2A, possibly 5-HT2C as well - similar to cypro. Look at Table 2 (p. 446) in the link below.
https://pdfs.semanticscholar.org/4805/330811ade05381e1d985c8c443ae69bbd65f.pdf

 

[chimdp]

I can't recommend any vendors but here is the chemical I had in mind.
https://en.wikipedia.org/wiki/Deramciclane

You can try to buy it from major chemical vendors like Sigma or Tocris. It is NOT a controlled substance and it has no serious side effects in clinical trials on humans.

@haidut This drug looks very interesting, I'd definitely buy it if you offered it the future. On the wiki page is mentions it also has affinity moderate affinity for D2 receptors. Do we assume this means as an inverse agonist or antagonist as well? If so, being that I feel like I'm lower on dopamine than the average person I feel like this quality might worry me a little.

 

[haidut]

@haidut This drug looks very interesting, I'd definitely buy it if you offered it the future. On the wiki page is mentions it also has affinity moderate affinity for D2 receptors. Do we assume this means as an inverse agonist or antagonist as well? If so, being that I feel like I'm lower on dopamine than the average person I feel like this quality might worry me a little.

Actually, there are studies comparing it with ritanserin and it had a slight dopaminergic effects (weaker than ritanserin). So, it is not a dopamine antagonist like cypro. It is also a camphor derivative, which piqued my interest given the many beneficial properties of camphor and the related adamantanes, which Peat wrote about as well. It also seems to have no known side effects except mild nausea, which is rare in the pharma world.
I am trying to get a source for it and if I succeed I will release it as a product.

 

[Koveras]

I can't recommend any vendors but here is the chemical I had in mind.
https://en.wikipedia.org/wiki/Deramciclane

You can try to buy it from major chemical vendors like Sigma or Tocris. It is NOT a controlled substance and it has no serious side effects in clinical trials on humans.

What's that drug Tropoxin some of the russian articles talk about?

 

[chimdp]

Actually, there are studies comparing it with ritanserin and it had a slight dopaminergic effects (weaker than ritanserin). So, it is not a dopamine antagonist like cypro. It is also a camphor derivative, which piqued my interest given the many beneficial properties of camphor and the related adamantanes, which Peat wrote about as well. It also seems to have no known side effects except mild nausea, which is rare in the pharma world.
I am trying to get a source for it and if I succeed I will release it as a product.

Awesome thank you! I'll be the first to buy it!

I assume you'll have better sources than me googling, but I see what you mean about finding a cost effective source...

https://www.medchemexpress.com/Deramciclane.html
Size Price Stock
1 mg USD 240 Get quote
5 mg USD 480 Get quote
10 mg USD 816 Get quote
20 mg USD 1440

Based on what I read you'd need to take about 60mg/day, which would be at the low low price of $4320/day from that website...

 

[haidut]

What's that drug Tropoxin some of the russian articles talk about?

I had forgotten about that, thanks for reminding me. When I looked at it some time ago I thought it is promising but it seems to accelerate dopamine breakdown. So, I don't know if its overall effects would be anti-serotonin or that plus anti-dopamine as well (which would be undesirable).
https://www.ncbi.nlm.nih.gov/pubmed/27159949