5ht2a, 5ht2c Antagonists

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Mar 17, 2018
Messages
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Any recommendations on natural 5ht2a, 5ht2c antagonists?
preferably high affinity, 3 years ago I took LSD and it seems like my 5ht levels are always high and I've got eye problems and vision change along with a dull personality and no adrenaline rush, because of that, I waited 3 years and nothing happened. Since then I've had high issues with anxiety, not able to function, and a lot of other issues like high prolactin.

What I already take (started 2 months ago):
Alpha GPC
Phosphatidyl choline
Uridine monophosphate
CoQ10 400 mg/day (mitochondrial function)
Pyrroloquinoline quinone (mitochondrial function)
Vitamin D
Vitamin A
Vitamin MK-7
Vitamin B12
Glycine
D-aspartic acid
omega 3,6,9
zinc gluconate
magnesium citrate
Acetylcysteine
Acetylcarnitine
Glutathione reduced
Centrophenoxine
Ashwaghandha
Lions Mane
L-lysine
L-carnocine
Curcumin
Gingko Biloba

Every single one of the above I have a supplement for it in moderate dosage that I take everyday.

I also smoke around 30 cigs a day (carbon dioxide & nicotine)

I also on occasion take: phenylpiracetam, aniracetam
(are these good for lowering serotonin?), I also have modafinil tablets ( but I get depressed on them sometimes I think that due to modafinil effect on prolactin or serotonin increased).


I'm also ordering the following next in hopes of lowering serotonin:
Yohimbine
White willow bark
Magnosteen
Melatonin
Berberine
FeverFew
Benadryl
BCAA
Whey Protein

However I've heard mixed things about yohimbine that through blocking alpa-2 adrenergic receptor it will actually increase serotonin? what do you think?

I've also thought about antipsychotics and tried (olanzapine, risperdone, aripiprazole, seroquel) for no more than a month, they all worked however they also antagonized d2 which I don't want to. Aside form their H1 affinity they made me sleepy and highly sedated, also most are antichlonergic, and they have a lot of negative side effects like diabetes and Hyperprolactinemia also I couldn't concentrate while on them. Unless I took modafinil

And once I've tried l-tyrosine a precursor to dopamine and I've had a psychotic episode.

I've heard about some products on this forum but they are out of stock and one of them was h1 antagonist and anitchlonergic which won't work for me.

Mirtazapine block 5ht2a and 5ht2c however it got high affinity for histamine and it will make me sedated and sleepy which I don't want.

I've also got a prescription for Klonopin (clonazepam) and I can take it everyday but I took for a month
and it made me a bit depressed in the end, so I stopped it.

I've also tried Lamotrigine as it helps vision but I also stopped it.

I've heared about Nuplazid (Pimavanserin) it's a potent 5ht2a and 5ht2c antagonist with no affinity for any other receptor however it's highly expensive sold at 2k for 60 days supply.

What are your other suggestions?
 
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OP
5ht Antagonist
Joined
Mar 17, 2018
Messages
13
I've also been thinking about estrogen blockers - Anti-Estrogen ( aromatase inhibitors) usually these meds are used for breast cancer. But I don't know if I can take them?


if so, what would you recommend from the following list:
-Anastrazole
-Arimidex
-Aromasin
-Clomid
-Evista (selective estrogen receptor modulator)
-Exemestane
-Femara
 
OP
5ht Antagonist
Joined
Mar 17, 2018
Messages
13
I know I've got all the issue since I've took that blotter of LSD 3 years ago, and something in my brain seems to have stayed high on serotonin, the trip was bad and all the effects were negative.

I was an ambitious hacker and now I'm a neuro hacker trying to fix what went wrong

I've never heard music as I've once ever since due to mild tinnitus and change in perception, my vision health was affected too, I was demotivated and my personality massively changed, I've lost contact with reality for a while and I had
mild migraines along with reduced sexual function and motivation in life, I was always high and sedated since then.

It was like the best way to destroy someone ( I was reckless when I decided I can take that not knowing what it affects), now the only positive thing is that I'm not as curious as I was but that's actually demotivating.

The current list of nootropics are having a good effect on me, however I think there's room for more improvement.

I don't know if it was lsd or another recreational thing like 25-nbome however they all seem to target 5ht receptors and fully activate them.

LSD is a 5-HT1A, 5-HT2A, 5-HT2C, 5-HT5A, 5-HT5, 5-HT6 agonist that has psychedelic properties

Any natural compound that is available on amazon or somewhere I can buy it would be appreciated for blocking the above receptors without affecting histamine or chlonergic functions
 
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OP
5ht Antagonist
Joined
Mar 17, 2018
Messages
13
I was looking at Cyproheptadine pharmacodynamics and it appears to be just like an antiphsycotic with all these high potent binding affinities!

Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site (and inhibits/blocks it)

Site Ki (nM) Species Ref
H1 0.06 | Human (very strong block on histamine H1 receptors so I assume I'll be sleepy all day since histamine regulates wakefulness and alertness )
H2 ND ND
H3 >10,000 | Human
H4 202 | Human
M1 12 | Human (that's also very bad block on Muscarinic Acetycholine receptors responsible for smartness, so I assume I'll be dumb all day )
M2 7 | Human (bad)
M3 12 | Human (bad)
M4 8 | Human (bad)
M5 11.8 | Human (bad)
5-HT1A 59 | Human (Good block on serotonin receptor)
5-HT2A 1.67 | Human (Good block on serotonin receptor)
5-HT2B 1.54 | Human (Good block on serotonin receptor)
5-HT2C 2.23 | Human (Good block on serotonin receptor)
5-HT3 228 | Mouse (Good block on serotonin receptor)
5-HT6 142 | Human (Good block on serotonin receptor)
5-HT7 123 | Human (Good block on serotonin receptor)
D1 117 | Human (that's dopamine d1 receptor, again bad block )
D2 112 | Human (dopamine d2 receptor, bad block )
D3 8 | ,Human (dopamine d3 receptor, bad block )
SERT 4,100 |Rat
NET 290 | Rat
DAT | ND ND

Wow, d1/d2/d3 are all affected, precious dopamine receptors are blocked!
Also M1,M2,M3,M4,M5 stands for Muscarinic Acetycholine receptors are highly blocked,

I don't think the advantages outweighs the disadvantages, that drug is just like atypical antipsychotics!
'
I'd prefer Mirtazapine(remeron) over this anytime if I were to choose!
 
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lampofred

Member
Joined
Feb 13, 2016
Messages
3,244
I think improving your progesterone/androgens to estrogen ratio is the healthiest/most fundamental way to reduce serotonin activity.
 
OP
5ht Antagonist
Joined
Mar 17, 2018
Messages
13
I think improving your progesterone/androgens to estrogen ratio is the healthiest/most fundamental way to reduce serotonin activity.

I just got clomid it's sold OTC in my country, it blocks estrogen by signalling there's enough to the brain. I'm looking to get Anastrazole it completely blocks estrogen receptors shutting them down while it isn't cheap it works more powerfully than clomid.

I haven't really got any testosterone tests but I have many reasons to believe mine are low.

5ht2c a subtype of serotonin receptor when it's highly active in someone's brain it impairs sexual function, causing high prolactin, adversely blocking dopamine causes high prolactin and sexual dysfunction, antiphsycotics block d2 receptor and causes high prolactin

When I was on olanzapine (an antipsychotic) even though it blocks most dopamine receptors, my sexual function (mindfully speaking) was slightly improving, not that much but I could notice it, that might be due to blocking all serotonin receptors specially the dangerous 5ht2a,5ht2c subtypes.

With clomid I also got aspirin and will be trying 200mg per day
 
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OP
5ht Antagonist
Joined
Mar 17, 2018
Messages
13
Clomid & Aspirin is working, don't know which one, but I'm already feeling better. However I've came upon something related to aspirin mechanism of action (that suggests serotonin production?):

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lampofred

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Feb 13, 2016
Messages
3,244
I just got clomid it's sold OTC in my country, it blocks estrogen by signalling there's enough to the brain. I'm looking to get Anastrazole it completely blocks estrogen receptors shutting them down while it isn't cheap it works more powerfully than clomid.

I haven't really got any testosterone tests but I have many reasons to believe mine are low.

5ht2c a subtype of serotonin receptor when it's highly active in someone's brain it impairs sexual function, causing high prolactin, adversely blocking dopamine causes high prolactin and sexual dysfunction, antiphsycotics block d2 receptor and causes high prolactin

When I was on olanzapine (an antipsychotic) even though it blocks most dopamine receptors, my sexual function (mindfully speaking) was slightly improving, not that much but I could notice it, that might be due to blocking all serotonin receptors specially the dangerous 5ht2a,5ht2c subtypes.

With clomid I also got aspirin and will be trying 200mg per day

Glad it seems to be working, but I'm not sure if aromatase inhibiting drugs are truly the ideal anti-estrogen solution. There are numerous ways for estrogen receptors to be activated in your body and estradiol via aromatization from testosterone is only one of them. For example another way for estrogen to be activated is for DHT to be metabolized into 3b-androstanediol which powerfully activates the estrogen receptor (even more strongly than estradiol I think). So if you take aromatase inhibitors, you reduce E2 which increases testosterone which increases DHT which increases 3b-androstanediol. So in areas where there is a high amount of 5alpha reductase (prostate gland and hair follicles for example), you will actually be severely worsening the progesterone to estrogen ratio. That is probably why aromatase inhibitors don't work for MPB even though the fundamental issue is progesterone to estrogen. I'm not sure about the brain specifically since that's what your question was about, but overall I think just natural ways of estrogen reduction even though they will take a long time would be healthier.
 
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OP
5ht Antagonist
Joined
Mar 17, 2018
Messages
13
I would like to analyze a situation, if LSD triggers serotonin release and acts as a full agonist at all 5ht receptors, wouldn't my mind come back to normal after all these years?
Since before the ingestion of LSD, I was complete normal and had higher DA to serotonin ratio. and higher testosterone ( I was like a ******* wild wolf on all levels especially financially).

I think the reason my mind didn't go back to normal perception was because of my smoking habit.

How that correlates, I'll explain:

Smoking cigarettes have been studied to activate MOAI (Monoamine Oxidase Inhibitor) that when inhibited doesn't break serotonin, dopamine, norepinephrine.
like acetycholinesterase inhibitors delays the break of acetycholine in the brain,
similarly does MOAI's for serotonin,dopamine, norepinephrine.

I discovered this through a realization that when I stopped smoking for 21 days once I had a good mood uplift and positive symptoms despite the nicotine horrible withdrawal effects.
And a some sort of back to "old days" pre-LSD.
Monoamine Oxidase are known to come back in action after 2 weeks, after being inhibited by irreversible inhibitors.

However, I returned to smoking.

Another thing I'd like to shed a light about is that I started again on l-tyrosine, It had a very good benefit which proves even further that I'm exceptionally high on 5ht.
another thing cleared for me, was that psychotic episode might not have been from l-tyrosine after all.

I think someone poured something into my water for malicious reasons. like liquid LSD or something else, I have a lot of reasons personally to feel this was the case, because that episode was just like a trip report from someone who took a psychedelic. Where I had a death fear at the end of it and loss of appetite along with dilated pupils, hallucinations, panic, anxiety, welp, tyrosine isn't making that now. and actually it's making the opposite of all the above especially tinnitus relief, why?

I have a doubt in someone in particular. Who I cut my relationship with after that happened.
Anyways I shall not die before I revenge that. And I know exactly how.

Back on topic, I'm going to get another thing next to tyrosine, from RP, hint: 5ht antagonism and dopamine agonism sounds good. Heck I already made my mind a lab after all that list of nootropics I'm on. I'll also follow a serotonin depletion technique rp spoke about.

along with another thing to manage estrogen that results from 5ht activation, ai's with androgen agonism agent, that way I'll have pure testosterone. and the estrogen will be blocked by ai, don't know after stopping AI would a rebound happen?

I'm also considering tianeptine to modulate glutamate.
 
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M

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inositol blocks 5ht2a. But you seem obsessed with decreasing serotonin to the point it might be unhealthy.
 

Frankdee20

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Sun Coast, USA
inositol blocks 5ht2a. But you seem obsessed with decreasing serotonin to the point it might be unhealthy.
Why does Inositol paradoxically cause anxiety in some individuals then ? It is used for relief of anxiety.
 

Lokzo

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I was looking at Cyproheptadine pharmacodynamics and it appears to be just like an antiphsycotic with all these high potent binding affinities!

Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site (and inhibits/blocks it)

Site Ki (nM) Species Ref
H1 0.06 | Human (very strong block on histamine H1 receptors so I assume I'll be sleepy all day since histamine regulates wakefulness and alertness )
H2 ND ND
H3 >10,000 | Human
H4 202 | Human
M1 12 | Human (that's also very bad block on Muscarinic Acetycholine receptors responsible for smartness, so I assume I'll be dumb all day )
M2 7 | Human (bad)
M3 12 | Human (bad)
M4 8 | Human (bad)
M5 11.8 | Human (bad)
5-HT1A 59 | Human (Good block on serotonin receptor)
5-HT2A 1.67 | Human (Good block on serotonin receptor)
5-HT2B 1.54 | Human (Good block on serotonin receptor)
5-HT2C 2.23 | Human (Good block on serotonin receptor)
5-HT3 228 | Mouse (Good block on serotonin receptor)
5-HT6 142 | Human (Good block on serotonin receptor)
5-HT7 123 | Human (Good block on serotonin receptor)
D1 117 | Human (that's dopamine d1 receptor, again bad block )
D2 112 | Human (dopamine d2 receptor, bad block )
D3 8 | ,Human (dopamine d3 receptor, bad block )
SERT 4,100 |Rat
NET 290 | Rat
DAT | ND ND

Wow, d1/d2/d3 are all affected, precious dopamine receptors are blocked!
Also M1,M2,M3,M4,M5 stands for Muscarinic Acetycholine receptors are highly blocked,

I don't think the advantages outweighs the disadvantages, that drug is just like atypical antipsychotics!
'
I'd prefer Mirtazapine(remeron) over this anytime if I were to choose!


I had some more Cypro last night, only 500mcg, and it reminds me of how much it SUCKS the life out of me.

Literally feel so numb, low motivated and horrible on cypro, but its worth it, because I get this amazing rebound that lasts many many weeks.

It's like ultimate reset. Like restarting your Nintendo 64. But the horrible 2-3 days after is so bad, I just push through it, knowing I will snap back a brand new man.
 
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