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Tuesday, August 26, 2014

Natural Serotonin Receptor Blockers / Antagonists


This article has been Published with the valuable input of the_apollo at longecity, thanks again.
:: http://www.longecity.org/forum/topic/72744-need-to-find-5ht1b-antagonist-drugherbal-to-treat-ocd-behavior/  ::

This article will explain specifically serotonin receptor blockers, as opposed to just serotonin reducers (by means of level of as opposed to receptor function). These remedies are all natural and can be bought OTC - Over the Counter.


I'm going to go into the lesser known ones first.
The first one is a natural 5-HT6 antagonist (producing pro-cognitive/nootropic effects). It also can rapidly deplete overall serotonin levels by antagonizing potassium-induced serotonin release.

The product is known as "Magnolia Bark Extract" - it should be noted however that it's effects are not purely serotonin antagonism - it also acts as a Benzodiazepine receptor potentiator/agonist.






Interactions of Magnolia and Ziziphus extracts with selected central nervous system receptors.

Koetter U1, Barrett M, Lacher S, Abdelrahman A, Dolnick D



 ETHNOPHARMACOLOGICAL RELEVANCE: Magnolia officinalis Rehder and Wilson [Magnoliaceae] bark and Ziziphus spinosa (Buhge) Hu ex. Chen. [Fam. Rhamnaceae] seed have a history of use in traditional Asian medicine for mild anxiety, nervousness and sleep-related problems.

AIM OF THE STUDY: To identify pharmacological targets, extracts of Magnolia officinalis (ME), Ziziphus spinosa (ZE), and a proprietary fixed combination (MZE) were tested for affinity with central nervous system receptors associated with relaxation and sleep.

METHODS: In vitro radioligand binding and cellular functional assays were conducted on: adenosine A(1), dopamine (transporter, D(1), D(2S), D(3), D(4.4) and D(5)), serotonin (transporter, 5-HT(1A), 5-HT(1B), 5-HT(4e), 5-HT(6) and 5-HT(7)) and the GABA benzodiazepine receptor. RESULTS: Interactions were demonstrated with the adenosine A(1) receptor, dopamine transporter and dopamine D(5) receptor (antagonist activity), serotonin receptors (5-HT(1B) and 5-HT(6) antagonist activity) and the GABA benzodiazepine receptor at a concentration of 100 microg/ml or lower. ME had an affinity with adenosine A(1) (K(i) of 9.2+/-1.1 microg/ml) and potentiated the GABA activated chloride current at the benzodiazepine subunits of the GABA receptor (maximum effect at 50 microg/ml). ME had a modest antagonist action with 5-HT(6) and ZE with the 5-HT(1B) receptor. CONCLUSION: The interactions in the receptor binding models are consistent with the traditional anxiolytic and sleep-inducing activities of Magnolia officinalis bark and Ziziphus spinosa seed.



   WHERE TO BUY NATURAL 5-HT6 Antagonist : Magnolia Bark Extract 
 
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RECEPTOR BLOCKER #2
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The next one is natural 5-HT2A antagonist  - which can aid in depression and may also lower cortisol and prolactin levels - consistent with effects of 5-HT2A blockade.
It's known as NANTENINE - from the herb known as "Heavenly Bamboo" or "Sacred Bamboo".
Other Names : Nandina (Nandina Domestica)

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2677726/

 Analogs of (±)-nantenine were synthesized and evaluated for antagonist activity at human 5-HT2Areceptors in a calcium mobilization assay. This work has resulted in the identification of the most potent 5-HT2Aantagonist known based on an aporphine. Our results also suggest that the C1 position may be a key site for increasing 5-HT2A antagonist activity in this compound series. In addition, the structural rigidity of the aporphine core appears to be required for nantenine to function as a 5-HT2A antagonist.

I have not found a valid product yet with solely Nadina but I will update this page when I find it.
You can buy the seeds below.


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RECEPTOR BLOCKER #3
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The third natural serotonin receptor blocker is known as Wild Jujube Extract.
It contains chemicals that antagonize 5-HT1B receptors, this will produce effects on behavior and may alleviate depressive disorders.
 ETHNOPHARMACOLOGICAL RELEVANCE: Magnolia officinalis Rehder and Wilson [Magnoliaceae] bark and Ziziphus spinosa (Buhge) Hu ex. Chen. [Fam. Rhamnaceae] seed have a history of use in traditional Asian medicine for mild anxiety, nervousness and sleep-related problems.

AIM OF THE STUDY: To identify pharmacological targets, extracts of Magnolia officinalis (ME), Ziziphus spinosa (ZE), and a proprietary fixed combination (MZE) were tested for affinity with central nervous system receptors associated with relaxation and sleep.

METHODS: In vitro radioligand binding and cellular functional assays were conducted on: adenosine A(1), dopamine (transporter, D(1), D(2S), D(3), D(4.4) and D(5)), serotonin (transporter, 5-HT(1A), 5-HT(1B), 5-HT(4e), 5-HT(6) and 5-HT(7)) and the GABA benzodiazepine receptor. RESULTS: Interactions were demonstrated with the adenosine A(1) receptor, dopamine transporter and dopamine D(5) receptor (antagonist activity), serotonin receptors (5-HT(1B) and 5-HT(6) antagonist activity) and the GABA benzodiazepine receptor at a concentration of 100 microg/ml or lower. ME had an affinity with adenosine A(1) (K(i) of 9.2+/-1.1 microg/ml) and potentiated the GABA activated chloride current at the benzodiazepine subunits of the GABA receptor (maximum effect at 50 microg/ml). ME had a modest antagonist action with 5-HT(6) and ZE with the 5-HT(1B) receptor.

CONCLUSION: The interactions in the receptor binding models are consistent with the traditional anxiolytic and sleep-inducing activities of Magnolia officinalis bark and Ziziphus spinosa seed.



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RECEPTOR BLOCKER #4
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Yohimbine HCL

ACTS as a competitive antagonist at multiple serotonin receptor subtypes - with the highest affinity being for 5-HT1B and 5-HT1D receptors - produces potent anti-depressant and aphrodisiac effects by this mechanism among others.

WHERE TO BUY YOHIMBINE HCL
~ DIFFERENT PRODUCTS BELOW








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14 comments:

  1. This comment has been removed by the author.

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  2. Also. Feverfew is a 5ht2a antagonist.

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  3. Nandina is highly toxic. Even birds die when they eat enough of the berries. What you need would be a high nantenine extract screened for toxins.

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    Replies
    1. Right, but some extracts like that are relatively easy to produce. There's teas of it that are non-toxic. They come from other countries though.

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  4. Is there anything I could take during a shrooms trip that would prevent heart issues from the shrooms. I have been researching this but I've had no luck. Many of the items I have came across can be potentially dangerous so does anyone know I safe one. Particularly one than affects 5ht 2a/2b/2c and it would also be good if it did not cross the blood brain barrier

    ReplyDelete
    Replies
    1. Not really sure, there's plenty of antagonists available, but most of them will stop your ''trip'' in its tracks. That's the point of serotonin antagonists, they reverse/block hallucinations and visual dissociation. So for agents that block serotonin receptors, you will be mostly looking at antipsychotics and perhaps some anxiolytic agents. Ritanserin by Idea Labs DC produced by @Haidut from Ray Peat forum. Other than that, look into the drug Terguride.

      Here's the paper on 2B-antagonism in relation to heart valve issues. Read all of it. Especially the last paragraph and under conclusions.

      https://www.hindawi.com/journals/bmri/2015/438403/

      Here's the store page for Ritanserin : http://www.idealabsdc.com/lab/

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  5. Out of sarpogrelate terguride and ritanserin which would be the safest to take

    ReplyDelete
    Replies
    1. Ritanserin, without a doubt.

      --> https://www.ncbi.nlm.nih.gov/pubmed/3095082
      --> http://onlinelibrary.wiley.com/doi/10.1111/j.1530-0277.1999.tb04105.x/full
      --> http://link.springer.com/article/10.1007/BF02245441

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  6. Which would be safer ritanserin or metdoxine. Also do you know any natural supplements you could take to prevent potential damage through 5HT2b. Agonism. That would be good for your heart

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    Replies
    1. Feverfew with high percentage of Parthenolide; inhibits 5-HT2B activity. https://www.ncbi.nlm.nih.gov/pubmed/11603284

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    2. I would still use Ritanserin or Metergoline over Feverfew though, nothing is guaranteed with Feverfew AND it takes a while to build up in the system.

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    3. I mean that Feverfew works but that it does not definitely 100% reduce/eliminate serotonin-related issues.

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  7. hi @JayZinDeRusso

    what would you suggest is the best thing to reduce/block serotonin?

    ReplyDelete