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Looking for research chem synthesis, any recommendations?

5ht2c inverse agonist synthesis laboratory research

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#1 StevesPetMacaque

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Posted 26 May 2020 - 04:33 PM


This board might be a bit more active given the ongoing pandemic, so I'm back seeking leads on synthesis of a couple compounds. If anyone has worked with a lab before or even has a friend of a friend getting a PhD in organic chemistry, please let me know (a DM is fine, if you prefer not to reply publicly).

 

I'm not looking for anything too exotic:

  • Relatively "clean" 5HT2C inverse agonists; in particular, SB-206,553 or SB-242084
  • Long-acting kappa opioid receptor antagonists, such as norbinaltorphimine or JDTic
  • Related to the above, the "inactive" R-form enantiomers of opioid antagonists often are potent TLR4 antagonists. Dextro-naltrexone, -naloxone, and -norbinaltorphimine (or any reasonably high enantiomeric excess thereof) would all work.

I'm able to pay upfront for synthesis from a trusted source. If there is a better subforum in which to ask about this, that's useful too.


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#2 Rorororo

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Posted 26 May 2020 - 07:57 PM

For kor antagonists:

 

I would get cerc 501 if I had a choice.

 

JDTic had their trials disconnected from safety reasons (VT issues)

 

JDTic was sold on TeamTLR and TeamTLR is a very sketchy company....they stopped selling it.  That should tell you enough. 



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#3 Daniel Cooper

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Posted 26 May 2020 - 09:15 PM

For kor antagonists:

 

I would get cerc 501 if I had a choice.

 

JDTic had their trials disconnected from safety reasons (VT issues)

 

JDTic was sold on TeamTLR and TeamTLR is a very sketchy company....they stopped selling it.  That should tell you enough. 

 

 

If you don't mind, can you expound on the sketchiness of TeamTLR?  In a sketchy market segment, my perception was they were less sketchy than most.  



#4 Rorororo

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Posted 26 May 2020 - 09:18 PM

If you don't mind, can you expound on the sketchiness of TeamTLR?  In a sketchy market segment, my perception was they were less sketchy than most.  

 

 

Sure.  They are a lot of posts about them but this one stands out the most:

https://www.reddit.c...esting_results/

 

Looks like they are faking their products and selling them to people.  My assumption would be that some of these people are trying to get this for a medication but to be fooled instead. Thats the lowest of the low, in my opinion.  Regardless of my opinion, you will get fake products from them. 



#5 Daniel Cooper

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Posted 26 May 2020 - 09:50 PM

I figured that's the incident that you were talking about.  Here's my recollection about the resolution of that issue.

 

Almost every vendor uses a filler to bulk up their active compound so that it fully fills whatever capsule they are going in.  TeamTLR pretty consistently uses taurine.  Whoever was running that test (I think it was Nootropics Depot running the test rather than someone running on their equipment), they were doing IR spectroscopy and the taurine filler completely swamped out the signal of the active compound.  The person running the test should have been aware of this issue but wasn't.  In my mind, it made ND look worse than TeamTLR since they didn't understand the test they were running.  In fairness to Nootropics Depot I believe they had recently acquired their IR spectroscopy gear and had not had a lot of time on it.  Nevertheless, if you're going to accuse a competitor company of fraud, you better make sure you know what you're talking about.

 

You can chase multiple threads down the rabbit hole but I'm pretty sure that was the ultimate conclusion of that issue.  I also avoided TeamTLR for this same reason for a time but now believe it was an unfair smear on their name.

 

 


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#6 Rorororo

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Posted 26 May 2020 - 10:48 PM

I figured that's the incident that you were talking about.  Here's my recollection about the resolution of that issue.

 

Almost every vendor uses a filler to bulk up their active compound so that it fully fills whatever capsule they are going in.  TeamTLR pretty consistently uses taurine.  Whoever was running that test (I think it was Nootropics Depot running the test rather than someone running on their equipment), they were doing IR spectroscopy and the taurine filler completely swamped out the signal of the active compound.  The person running the test should have been aware of this issue but wasn't.  In my mind, it made ND look worse than TeamTLR since they didn't understand the test they were running.  In fairness to Nootropics Depot I believe they had recently acquired their IR spectroscopy gear and had not had a lot of time on it.  Nevertheless, if you're going to accuse a competitor company of fraud, you better make sure you know what you're talking about.

 

You can chase multiple threads down the rabbit hole but I'm pretty sure that was the ultimate conclusion of that issue.  I also avoided TeamTLR for this same reason for a time but now believe it was an unfair smear on their name.

 

chase multiple threads down the rabbit hole

 

This.  You are correct.  There are multiple incidents and multiple threads on them.  I don't want waste my time doing so to prove a point.  That one by ND is concrete proof though. I would stay away.

 

If you want to defend them then go ahead. I don't think its fair (for whatever incentive you have) to cast doubt on this matter for people.  It's not just one incident, anyone can do a simple search and find multiple. 

 

For goodness sake, take a look at their website!  They pretend that they are an actual research lab and conduct trials. They lie that they trial out their products on animals then gather results.  You know the amount of work and equipment (which they don't have) is required?  They have an outdated website with sketchy payment methods.  Seriously, how on earth can they act like a research facility?  They really expect people to buy into this?

 

ACTUALLY, this is from a recently 'bumped' thread. The 9 Me Bc one.  I stumbled inside it and found this, it cracked me up LOL

 

https://www.longecit...ndpost&p=867368

 

Stay away from TeamTLR


Edited by Rorororo, 26 May 2020 - 11:25 PM.


#7 pro-v

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Posted 27 May 2020 - 12:14 AM

THT.CO used to. They still have a website but dropped off the map in regards to nootropics a while back. It’s worth dropping them an email.

#8 Rorororo

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Posted 27 May 2020 - 04:46 AM

Also, JDTic is available on https://www.alibaba.com/

 

If you buy some, ill split it with you.  

 

If you want custom synth then ill defn split CERC 501 with you.

 

I know people that will make it but it has to be bulk. I think 1kg min?  I am not too sure. Also, by people, I mean labs in china.  If you just message people on Aliaba you will find actual labs.  


Edited by Rorororo, 27 May 2020 - 04:54 AM.


#9 StevesPetMacaque

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Posted 30 May 2020 - 08:00 PM

For kor antagonists:

 

I would get cerc 501 if I had a choice.

 

JDTic had their trials disconnected from safety reasons (VT issues)

 

JDTic was sold on TeamTLR and TeamTLR is a very sketchy company....they stopped selling it.  That should tell you enough. 

 

I plan on using about 1/50th of the oral dose intranasally in my experimental animals; I have not had any problems using norBNI this way. The irregularity is mediated by KORs on the heart itself rather than central effects.

 

I think TeamTLR is as worried about liability as anybody. It's a shame; these long-acting KOR antagonists are a potent way to reverse the cognitive effects of chronic chemical, stress, or sensory overstimulation. What most people call "dopamine receptor downregulation" is actually KOR upregulation; the number of dopamine receptors is actually relatively stable.

 

THT.CO used to. They still have a website but dropped off the map in regards to nootropics a while back. It’s worth dropping them an email.

 

Thanks for the reminder! I bought something obscure from them back when they were a more standard noot company. I will reach out about a synth.

 

Also, JDTic is available on https://www.alibaba.com/

 

If you buy some, ill split it with you.  

 

If you want custom synth then ill defn split CERC 501 with you.

 

I know people that will make it but it has to be bulk. I think 1kg min?  I am not too sure. Also, by people, I mean labs in china.  If you just message people on Aliaba you will find actual labs.  

 

I have family and friends who've done extensive business in China, so I am a little skeptical of that business culture. I would be willing to work with a lab in China, but I would strongly prefer a good reference to a specific lab from someone who's had synthesis done before. That said, I am happy to share any compounds synthesized with other Longecity experimenters. (Caveat emptor, of course)

 

Thanks all for the feedback and discussion.


Edited by StevesPetMacaque, 30 May 2020 - 08:02 PM.


#10 Rorororo

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Posted 06 June 2020 - 04:54 AM

I think every lab that is willing to synthesize chemicals for research are going to be in china.  The best bet is having it synthesized and tested.  Unless you find a post doc student willing to do it.  I would also test that too, of course. 

 

Let me know if you get any progress with this!

 

 

I plan on using about 1/50th of the oral dose intranasally in my experimental animals; I have not had any problems using norBNI this way. The irregularity is mediated by KORs on the heart itself rather than central effects.

 

I think TeamTLR is as worried about liability as anybody. It's a shame; these long-acting KOR antagonists are a potent way to reverse the cognitive effects of chronic chemical, stress, or sensory overstimulation. What most people call "dopamine receptor downregulation" is actually KOR upregulation; the number of dopamine receptors is actually relatively stable.

 

 

Thanks for the reminder! I bought something obscure from them back when they were a more standard noot company. I will reach out about a synth.

 

 

I have family and friends who've done extensive business in China, so I am a little skeptical of that business culture. I would be willing to work with a lab in China, but I would strongly prefer a good reference to a specific lab from someone who's had synthesis done before. That said, I am happy to share any compounds synthesized with other Longecity experimenters. (Caveat emptor, of course)

 

Thanks all for the feedback and discussion.

 



#11 Rorororo

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Posted 07 June 2020 - 01:32 AM

Nor-bni seems cheap, you can get 25mg for $240 (90-day supply with your regimen) 

 

 

I am thinking you can pair it with a natural opioid agonist. Like ALKS-5461 was trying to go for. 

 

Passion flower seems promising but I don't know its exact values - it is just one that I found out about today. 


Edited by Rorororo, 07 June 2020 - 01:33 AM.


#12 StevesPetMacaque

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Posted 07 June 2020 - 05:36 PM

Nor-bni seems cheap, you can get 25mg for $240 (90-day supply with your regimen) 

 

 

I am thinking you can pair it with a natural opioid agonist. Like ALKS-5461 was trying to go for. 

 

Passion flower seems promising but I don't know its exact values - it is just one that I found out about today. 

 

Where did you see that price? It's better than what I found - though still consistent with what an analytics supplier might charge. nor-BNI is just 2 naltrexone molecules joined together, and that stuff is literally 200 times cheaper.



#13 Rorororo

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Posted 07 June 2020 - 05:41 PM

Where did you see that price? It's better than what I found - though still consistent with what an analytics supplier might charge. nor-BNI is just 2 naltrexone molecules joined together, and that stuff is literally 200 times cheaper.

 

I forgot the vendor. If you type the CAS number in google (which is what I did) you will then find it =)



#14 Targz

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Posted 07 June 2020 - 11:42 PM

I'm quite interested in these as well. I contacted David Pearce just today before seeing this to see if he has any connections or a supply of JDTic and I also sent an email to science.bio concerning the addition of the product to their store which they said they're possibly looking in to. I'm in the same boat as you as far as finding the kappa antagonists since I don't have any university creds and I'm unemployed.

 

I'm willing to drop a significant chunk of money to fund a group buy if you can find a reliable source. I've got 2 grand to burn so if you can find a supplier that's very reliable that can at least send a sample first I'd be willing to fund most of the group buy and sell off my supply to the rest of you. I understand this sounds sketchy as I'm a new member but I'm a long time lurker and this thread caught my eye enough to make me make an account. You add me on discord (Targz#8589) if you're interested (new member message limit), there's a pretty large server I'm in where several people are also interested in buying a kappa antagonist and many of the members there can vouch for me that I'm no scammer.

 

I have a very close friend with TRD and DP/DR that could really benefit for this, and I've been scouring the internet hopelessly for the most of the day.

 

As per your 5-HT2C issue though, you may be able to get a quick fix with a sigma-1 agonist, which counteracts the effects of inflammatory cytokines in the brain. Inflammatory cytokines upregulate 5-HT2C receptors and the SERT, and sigma-1 agonists block the effects cytokines have on serotonin reuptake and 5-HT2C receptor sensitivity. Considering 5-HT2C supersensitivity may be a product of inflammation in the brain and body, a sigma-1 agonist such as DXM might come in handy. I can vouch that low doses of DXM (75-120 mg to start depending on your weight, taken on an empty stomach) give several hours of increased motivation before requiring a smaller redose whereas SSRIs have always caused lethargy and fatigue in me. Fluvoxamine may also be an option but I found the "sigmaergic" effects to require too much serotonin reuptake activity before becoming relevant whereas DXM (without a CYP2D6 inhibitor) caused a more reasonable, balanced effect rather than feeling "off" or "chemical."

 

Though a 5-HT2C inverse agonist would be ideal (even the sigma-1 agonist option would likely decrease the amount of 5-HT2C receptors depending on the dose rather than just blocking them neutrally, meaning less constitutive activity overall, though at what point this effect becomes relevant compared to a clean antagonist is unknown), I think a kappa antagonist is far more interesting and has far more merit, especially considering that 5-HT2C receptors also mediate oxytocin signalling in parts of the brain, so blocking them outright might be undesirable compared to decreasing pathological effects of cytokine-induced overexpression through sigma-1 agonism which also has BDNF boosting antidepressant effects, boosts NMDA receptor expression in prefrontal cortical working memory networks, and increases acetylcholine release in the cortices, contributing nootropic effects as well. Kappa agonists seem to be the most in demand, and are probably what you'll find more people interested in.



#15 Rorororo

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Posted 08 June 2020 - 01:17 AM

Risky but you can go to Alibaba and message a bunch of random suppliers to see if they can synth something like cerc 501...then 2k should get you a large batch from a lab on alibaba......you might have enough to get it tested...

 

 

Then once you have it made and tested then you can resell to members.  You might even make some profit!

 

I'm quite interested in these as well. I contacted David Pearce just today before seeing this to see if he has any connections or a supply of JDTic and I also sent an email to science.bio concerning the addition of the product to their store which they said they're possibly looking in to. I'm in the same boat as you as far as finding the kappa antagonists since I don't have any university creds and I'm unemployed.

 

I'm willing to drop a significant chunk of money to fund a group buy if you can find a reliable source. I've got 2 grand to burn so if you can find a supplier that's very reliable that can at least send a sample first I'd be willing to fund most of the group buy and sell off my supply to the rest of you. I understand this sounds sketchy as I'm a new member but I'm a long time lurker and this thread caught my eye enough to make me make an account. You add me on discord (Targz#8589) if you're interested (new member message limit), there's a pretty large server I'm in where several people are also interested in buying a kappa antagonist and many of the members there can vouch for me that I'm no scammer.

 

I have a very close friend with TRD and DP/DR that could really benefit for this, and I've been scouring the internet hopelessly for the most of the day.

 

As per your 5-HT2C issue though, you may be able to get a quick fix with a sigma-1 agonist, which counteracts the effects of inflammatory cytokines in the brain. Inflammatory cytokines upregulate 5-HT2C receptors and the SERT, and sigma-1 agonists block the effects cytokines have on serotonin reuptake and 5-HT2C receptor sensitivity. Considering 5-HT2C supersensitivity may be a product of inflammation in the brain and body, a sigma-1 agonist such as DXM might come in handy. I can vouch that low doses of DXM (75-120 mg to start depending on your weight, taken on an empty stomach) give several hours of increased motivation before requiring a smaller redose whereas SSRIs have always caused lethargy and fatigue in me. Fluvoxamine may also be an option but I found the "sigmaergic" effects to require too much serotonin reuptake activity before becoming relevant whereas DXM (without a CYP2D6 inhibitor) caused a more reasonable, balanced effect rather than feeling "off" or "chemical."

 

Though a 5-HT2C inverse agonist would be ideal (even the sigma-1 agonist option would likely decrease the amount of 5-HT2C receptors depending on the dose rather than just blocking them neutrally, meaning less constitutive activity overall, though at what point this effect becomes relevant compared to a clean antagonist is unknown), I think a kappa antagonist is far more interesting and has far more merit, especially considering that 5-HT2C receptors also mediate oxytocin signalling in parts of the brain, so blocking them outright might be undesirable compared to decreasing pathological effects of cytokine-induced overexpression through sigma-1 agonism which also has BDNF boosting antidepressant effects, boosts NMDA receptor expression in prefrontal cortical working memory networks, and increases acetylcholine release in the cortices, contributing nootropic effects as well. Kappa agonists seem to be the most in demand, and are probably what you'll find more people interested in.

 



#16 Targz

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Posted 08 June 2020 - 02:12 AM

Risky but you can go to Alibaba and message a bunch of random suppliers to see if they can synth something like cerc 501...then 2k should get you a large batch from a lab on alibaba......you might have enough to get it tested...

 

 

Then once you have it made and tested then you can resell to members.  You might even make some profit!

I'm not interested in CERC-501 because it's unsustainable long term in that it very likely upregulates the receptors after withdrawal, requires constant daily dosing, and has mu affinity at not much higher than the lowest effective dose, meaning the therapeutic window is absolute garbage. For this reason, I'm only interested in JDTic and Nor-BNI. The GNTI analogs don't cross the BBB so they're not practical. JDTic would be ideal, I'm not afraid of the cardiac effects due to poor methodology, a sample size not large enough for statistical significance, and not screening for cardiovascular health and matching to controls in a double blind placebo-controlled fashion. The long acting isn't worrying for me, it's a plus, and CERC also has really high therapeutic doses in addition to the short half life (10-25mg) while Nor-BNI and JDTic doses are in the microgram range, with JDTic being the most potent (doses as low as 100mcg). Additionally, JDTic doesn't have a morphinan backbone in its structure unlike nor-BNI, so it is potentially less of an issue on the regulatory side.

 

If you have dealt with severe mental issues you'll know the issue with drugs with short half life and tolerance being your only way out, compared to something that causes long-lasting effects that you don't need to dose every day. Waking up feeling like all your progress is gone and not knowing if it'll work that day is terrifying, but something that nukes your receptors for weeks and guarantees you sustained anxiolytic, antidepressant, and anti-depersonalization effects is solid. I know the kind of person I'm dealing with and CERC is absolutely not on the table.

 

I already searched on alibaba and I couldn't find any suppliers that seemed reasonably safe. I don't want to take any big risks with this. This isn't money I'm willing to gamble, only spend if I'm absolutely guaranteed to get either JDTic or Nor-BNI out of it in significant quantities that I'll never have to worry about buying again. This is basically all of my spendable money and I'm unemployed and living at home so this is the big charade for me, and I'm only doing it because I can't let the people I care about keep suffering.



#17 Rorororo

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Posted 08 June 2020 - 10:49 PM

I'm not interested in CERC-501 because it's unsustainable long term in that it very likely upregulates the receptors after withdrawal, requires constant daily dosing, and has mu affinity at not much higher than the lowest effective dose, meaning the therapeutic window is absolute garbage. For this reason, I'm only interested in JDTic and Nor-BNI. The GNTI analogs don't cross the BBB so they're not practical. JDTic would be ideal, I'm not afraid of the cardiac effects due to poor methodology, a sample size not large enough for statistical significance, and not screening for cardiovascular health and matching to controls in a double blind placebo-controlled fashion. The long acting isn't worrying for me, it's a plus, and CERC also has really high therapeutic doses in addition to the short half life (10-25mg) while Nor-BNI and JDTic doses are in the microgram range, with JDTic being the most potent (doses as low as 100mcg). Additionally, JDTic doesn't have a morphinan backbone in its structure unlike nor-BNI, so it is potentially less of an issue on the regulatory side.

 

If you have dealt with severe mental issues you'll know the issue with drugs with short half life and tolerance being your only way out, compared to something that causes long-lasting effects that you don't need to dose every day. Waking up feeling like all your progress is gone and not knowing if it'll work that day is terrifying, but something that nukes your receptors for weeks and guarantees you sustained anxiolytic, antidepressant, and anti-depersonalization effects is solid. I know the kind of person I'm dealing with and CERC is absolutely not on the table.

 

I already searched on alibaba and I couldn't find any suppliers that seemed reasonably safe. I don't want to take any big risks with this. This isn't money I'm willing to gamble, only spend if I'm absolutely guaranteed to get either JDTic or Nor-BNI out of it in significant quantities that I'll never have to worry about buying again. This is basically all of my spendable money and I'm unemployed and living at home so this is the big charade for me, and I'm only doing it because I can't let the people I care about keep suffering.

 

 

What makes you state that CERC-501 will upregulate the receptors and not JD Tic?   I am asking because I am curious. There doesn't seem any studies that I can find that show or doesn't show that KOR antagonism causes down-regulation.  There is alot of contradicting information out there. 



#18 Targz

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Posted 09 June 2020 - 03:19 AM

What makes you state that CERC-501 will upregulate the receptors and not JD Tic?   I am asking because I am curious. There doesn't seem any studies that I can find that show or doesn't show that KOR antagonism causes down-regulation.  There is alot of contradicting information out there. 

JDTic is marked as an irreversable antagonist. It activates JNK to deactivate KORs which leaves them disabled for weeks. CERC-501 is just a classical antagonist.


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#19 StevesPetMacaque

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Posted 20 June 2020 - 02:16 AM

I'm quite interested in these as well. I contacted David Pearce just today before seeing this to see if he has any connections or a supply of JDTic and I also sent an email to science.bio concerning the addition of the product to their store which they said they're possibly looking in to. I'm in the same boat as you as far as finding the kappa antagonists since I don't have any university creds and I'm unemployed.

 

I'm willing to drop a significant chunk of money to fund a group buy if you can find a reliable source. I've got 2 grand to burn so if you can find a supplier that's very reliable that can at least send a sample first I'd be willing to fund most of the group buy and sell off my supply to the rest of you. I understand this sounds sketchy as I'm a new member but I'm a long time lurker and this thread caught my eye enough to make me make an account. You add me on discord (Targz#8589) if you're interested (new member message limit), there's a pretty large server I'm in where several people are also interested in buying a kappa antagonist and many of the members there can vouch for me that I'm no scammer.

 

I have a very close friend with TRD and DP/DR that could really benefit for this, and I've been scouring the internet hopelessly for the most of the day.

 

As per your 5-HT2C issue though, you may be able to get a quick fix with a sigma-1 agonist, which counteracts the effects of inflammatory cytokines in the brain. Inflammatory cytokines upregulate 5-HT2C receptors and the SERT, and sigma-1 agonists block the effects cytokines have on serotonin reuptake and 5-HT2C receptor sensitivity. Considering 5-HT2C supersensitivity may be a product of inflammation in the brain and body, a sigma-1 agonist such as DXM might come in handy. I can vouch that low doses of DXM (75-120 mg to start depending on your weight, taken on an empty stomach) give several hours of increased motivation before requiring a smaller redose whereas SSRIs have always caused lethargy and fatigue in me. Fluvoxamine may also be an option but I found the "sigmaergic" effects to require too much serotonin reuptake activity before becoming relevant whereas DXM (without a CYP2D6 inhibitor) caused a more reasonable, balanced effect rather than feeling "off" or "chemical."

 

Though a 5-HT2C inverse agonist would be ideal (even the sigma-1 agonist option would likely decrease the amount of 5-HT2C receptors depending on the dose rather than just blocking them neutrally, meaning less constitutive activity overall, though at what point this effect becomes relevant compared to a clean antagonist is unknown), I think a kappa antagonist is far more interesting and has far more merit, especially considering that 5-HT2C receptors also mediate oxytocin signalling in parts of the brain, so blocking them outright might be undesirable compared to decreasing pathological effects of cytokine-induced overexpression through sigma-1 agonism which also has BDNF boosting antidepressant effects, boosts NMDA receptor expression in prefrontal cortical working memory networks, and increases acetylcholine release in the cortices, contributing nootropic effects as well. Kappa agonists seem to be the most in demand, and are probably what you'll find more people interested in.

 

Hi Targz, I responded on your other thread and to your PM, yet somehow missed the response you posted here. Doesn't seem like you've been on for a few days, so I can reach out on Discord too.

 

Thanks for the recommendation about sigma-1 agonism. I have tried several doses of ifenprodil, but it always produces an hour or 2 of severe anxiety, so I decided to shelve it for now. Perhaps this can be partially compensated for by increased Mg dosing to help block the Ca influx. It seems like it would take a while (weeks or months?) for reduced central cytokines to translate into reduced 5HT2C expression, though I haven't read up on the timescales involved in any detail.

 

The cytokine connection is precisely what drew my attention to the 5HT2C receptor in the first place. I got mono from EBV at 19, and my motivation levels never returned to baseline (20 years have passed). I coped by, basically, becoming a massive underachiever. After finding papers describing how 5HT2C expression shifted behavior from high-cost, high-reward strategies to low-cost, low-reward strategies, I realized this was a plausible mechanism to explain the change in my personality.

 

It's a funny coincidence that you reached out to David Pearce; he was still enthusiastic about JDTic but unable to help with sourcing when I spoke to him.



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#20 gintrux

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Posted 26 June 2020 - 07:23 PM

I'm also interested in acquiring some JDTic to try. Please organize a group buy and PM me with details.


Edited by gintrux, 26 June 2020 - 07:23 PM.






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