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Showing posts with label natural serotonin receptor blockers. Show all posts
Showing posts with label natural serotonin receptor blockers. Show all posts

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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