List of 5-HT2B Antagonists Available As Supplements (Supplements that Antagonize/Block Serotonin 2B Receptors)

5-HT2B Receptors are a type of Serotonin Receptor (GPCR; G-Protein-Coupled-Receptor); they are evident mostly in blood vessels/human atrium (heart) (1) and in the small intestine (2) , however, they play a minor role in the ((CNS)), and activating them tends to increase serotonin release and blocking them reduces serotonin release {(3)}.

Applications and Benefits of antagonizing the Receptor would include.

• Improvement of Cardiac Function and Reduction in Blood Pressure [4]
• Alleviation of Chronic Diarrhea and other intestinal complaints associated with I.B.S. -(5)-
• Improvement in side-effects associated with SSRI-medications for Depression (particularly, bowel complaints) {6}
• Enhancement of Muscle Pump during Exercise ~{7}~
• Utility in k+-mediated- augmentations; to reduce the effects of SSRI's on Potassium-related depolarization and thus to enhance Potassium-electrical currents (K+).(*8*)
• Possible use, adjunct in Migraine treatment , lesser so than other uses, though. <(9)>
• Transient reduction in Plasma Serotonin level/s, and significant reduction in Serotonin Release. ~!(10)!~

The main TWO only EFFECTIVE Over-the-Counter 5-HT2B-Receptor Antagonists are.....

• GINGER (can be bought as Chewy Candies, Tea or Capsules, as well as Liquid Solution).
• YOHIMBINE (a stimulant supplement, used as a fat burner with aphrodisiac properties)

Is Desensitization of Nervous System Receptors A Good Thing ? Is 'Desensitization' A Natural Process?

A : It depends on the Receptor being Desensitized - It's impossible to generalize the effects of 'desensitization' if we do not define the Receptor being desensitized.

Additionally, it depends on the *reason* and pathway of desensitization.


Example ::: 5-HT(1)A Autoreceptors may be desensitized by Stress; in which case, serotonin release is increased pathologically, but , in addition to this, other important receptors are downregulated thus discriminating the two effects under the blanket of one central stress response becomes difficult. 

Under other physiological conditions, such as depressed neural connections and synaptic connectivity, certain receptors being desensitized can be beneficial to bridging new connections and creating new neurons.

Is Desensitization A Natural Process?

1. It certainly can be, some Receptors can get desensitized after being exposed to endogenous hormones Cortisol and Estrogen; which are secreted during Stress and hormone surges/ovulation - Respectively.
2. Many natural compounds and pharmaceutical agents produce desensitization of certain receptors; keep in mind , this is not always a bad thing, again, it depends on what receptors are being desensitized.
3. Desensitization , thus, is NOT purely a pharmaceutical - induced - process...it is both natural, and chemical induced , depending on other factors ; both endogenous (natural, within the body) and external factors (from the outside, dietary etc, exposure to chemicals, like heavy metals).

IS DE-SENSITIZATION NECESSARY TO TREAT DEPRESSION?

A: Much of the Research of Depression is botched based on conflicting pharmacology's of researched compounds - in essence, there aren't enough  'CLEAN' pharmaceutical agents to produce a higher 'absolute consistency' in study results. 

• Research shows that desensitization is not necessary in terms of one receptor OR another to treat Depression, but under certain gene conditions; where one has a family history of Depression and specific allele's / gene alterations , defined by science, then desensitization may be the way to Go..
• However, desensitization can be beneficial because it bypasses the need for multiple mechanisms to be used in increasing one neurotransmitter; specifically with the serotonin system (1A,1B).
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Can Someone Live Without Serotonin? (Short-Answer & In-Depth Explanation) (Possible Symptoms Included)

Short-Answer : Yes. But one may need to still supplement with Melatonin if Serotonin is unable to be produced in the brain/body.

**There may be significant alterations in synaptic plasticity, altered cognition, constipation and abnormal aggression, as well as odd developments in neural fibers and skeletal mass ([but not bad, necessarily])**

                               `~~~GOING FURTHER~~~`
Sepiapterin Reductase Deficiency is a condition which causes a loss of monoamine neurotransmitters; like Serotonin and Dopamine - one case, where a 28-year old Man was studied in France with this particular genetic mutation ,,,  showed that low levels of Serotonin, AFTER dopamine deficiency was reversed with L-Dopa treatment - revealed no significant Depressive-symptoms..BEFORE & AFTER - Interestingly, the man who had virtually no serotonin or dopamine; he slept WAY TOO MUCH; so I guess that puts a wrench in the  Prozac Pusher's Happy {medium}. You know, they go off saying "Serotonin is good for Sleep" .... ''good for depression/mood''.

Nothing is that simple in brain chemistry, EVER.

• Serotonin Depletion *usually* causes some degree of behavioral changes in all study types/subjects, however, some do not really show any significant changes.
• In HEALTHY Humans without a genetic/family history of Major Depressive Disorder; serotonin depletion does not cause any mood disturbance(!).
• In HEALTHY Humans with a genetic/family history of Depression - there is only a *slight* reduction in mood(!).
• It is demonstrated that low serotonin levels may induce gastrointestinal complaints (like Constipation), but otherwise do not prominently affect gut health if everything else is in check.
• Serotonin plays a LARGE role in vascular/heart health, however, much of the evidence points towards serotonin contributing to pulmonary hypertension/high blood pressure..
• Low Serotonin theoretically could lead to alterations in bone mass - but i t may, again, be irrelevant if the individual is healthy, otherwise (R1) (R2) (R3)

5 Herbs that Have Similar Effects to Cocaine (Herbs that Mimic / Match Potency of Cocaine)

Within the World of Euphoria-inducing Substances, there lies a choice; a ''proven street-known buzz'' or a ''alternative legal high''... each have their own Risks. Each have potential side-effects. Each have their own 'subjective' effects. Each have their own long-term effects...

However, what most want to know in terms of 'natural' highs is whether they have *comparable* Effects. For the science-geeks and regimented pharmacological enthusiasts; the same , but in terms of 'mechanism of action'...of course, it is Possible, perhaps, even probable, to be a drug-head and a pharmaceutical genius...but , enough of that...


Here are 5 herbs that demonstrate selectivity and EFFICIENCY in the same behavioral paradigms as Cocaine - and they all produce the same dopaminergic effects, perhaps *slightly* less Potent, though.


The FIRST is known as Thunbergia laurifolia, which is shown to INCREASE (rapidly and efficiently) the amount of and release of DOPAMINE in the NAc/NAcc; the Nucleus Accumbens (1) (2) - it has memory-boosting effects as well and can block the effects of memory-dulling drugs such as Scopolamine (3) (4) (5). It also can help in detoxifying poisons such as Arsenic and Strychnine, and even Alcohol (6) (7).

It can be bought by clicking the IMAGE/LINK Below or clicking ~HERE~.

The SECOND is CATUABA Extract.


Which acts as a DIRECT Dopamine-Serotonin Reuptake Inhibitor; lacking only the norepinephrine property of the Coca alkaloids.
({<see Here>})

Supplements to Counteract Tardive Dyskinesia (Alternative Suggestions in Treating AntiPsychotic-EPS)

T.D - Tardive Dyskinesia : weakly defined by WIKIPEDIA as "a disorder resulting in involuntary, repetitive body movements" but more accurately described as.....

Touche, though, on WIKI appropriately addressing T.D's causes as " the result of long-term or high-dose use of antipsychotic drugs,^{[Note 1]} or in children and infants as a side effect from usage of drugs for gastrointestinal disorders."


Biochemically, or more correctly, Physiologically; {of neurophysiology} ; describes the disorder as a result of "unfavorable VTA-DA transmission" and the result of a poor ratio of D2:5-HT2A blockade in an antipsychotic drug...essentially, this means TOO MUCH Dopamine receptor blockade and NOT ENOUGH Serotonin blockade (particularly 5-HT2A receptors which are implicated and connected, directly , with motor circuitry and muscle-kinetic-gating neuronal networks)...

Supplements to COUNTER-ACT Tardive Dyskinesia's ( AND EVEN PREVENT T.D )

• VITAMIN B6
• Manganese
• Vitamine E

! (**SOURCE**) !

https://books.google.com/books?id=erPADTyyKj0C&pg=PA21&lpg=PA21&dq=ratio+of+dopamine+5-ht2a+dopamine+d2+in+tardive+dyskinesias&source=bl&ots=f9LRViu29G&sig=kZqnf0W-iBBTMTQwMmxBdwD_f40&hl=en&sa=X&ved=0ahUKEwj33u6_ieDKAhUX0GMKHTKXDpMQ6AEIRDAF#v=onepage&q=ratio%20of%20dopamine%205-ht2a%20dopamine%20d2%20in%20tardive%20dyskinesias&f=false

How to Increase 5-HT1A Receptors (A Detailed , but Easy to Understand Guide) (Includes Supplement Suggestions)

5-HT(1)A receptors are designated as one of the most important receptor types in the human physiology; especially in regards to Stress Adaptation (1) (2) and Depression (3) (4) (5). They make for such a popular topic, that they are written about extensively , by not just medical professionals and researchers (6) (7), but by bloggers, health enthusiasts and 'recreational thinkers' alike (8) (9) (10). The sheer fascination with them and their ligands - stamps them as some of the most revered topics in longevity and anti-aging forums (11) (12) and even fitness / bodybuilding forums (13) (14).

....However, neither mountains of bro-science nor countless hours of theorizing and abstract ideas are sufficient to actually justify a plausible solution to fine-tuning this network.

So lets stick with the FACTS.

• 5-HT(1)A Receptor activity and Receptor Expression is greatly determined by male sex hormones (Testosterone, DHT) (15) (16) (17) (18) (19) as well as Corticosteroids (Cortisol, Cortisone) (20) (21) (22) (23) (24) .
• From that standpoint - our goal should be to decrease cortisol by any means, and to increase Testosterone levels (25) (26).
• Minerals such as Manganese (27) and Magnesium (28) play a HUGE role in increasing AND maintaining 5-HT1A Receptors.

INCREASING 5-HT1A RECEPTORS WITH SUPPLEMENTS

1. Supplement with BOTH Magnesium & Manganese. Preferably @ Night.
2. BLOCK / REDUCE Cortisol & Increase Testosterone by using Barlowe's Benzoflavone/PS/Resveratrol Supplement.
3. If you REALLY Want to Go 'EXTREEeM' , you can use Andractim to reload your potential and shift the 5-HT1A:2A Expression Ratio. (It is a DHT-Analogue)

**The notion behind DHT-Supplements in 5-HT(1)A Regulation is based on DHT's proven Anti-Cortisol/Anti-Stress benefit as outlined in my "DHT & The Brain Article**

`~**MAIN EXCITATIONS & REFERENCES**~'

5-HT1A and beyond: the role of serotonin and its receptors in depression and the antidepressant response.

Allelic variation in 5-HT1A receptor expression is associated with anxiety- and depression-related personality traits

Transcriptional regulation of the 5-HT1A receptor: implications for mental illness

Transcriptional dysregulation of 5-HT1A autoreceptors in mental illness

Chronic Administration of 5-HT1A Receptor Agonist Relieves Depression and Depression-Induced Hypoalgesia

Activation of postsynaptic 5-HT1A receptors improve stress adaptation.

Possible Interactive Effect of Testosterone and Aldosterone Receptor Antagonists on Cardiac Apoptosis

Testosterone level and the effect of levodopa and agonists in early Parkinson disease: results from the INSPECT cohort

What Neurotransmitters Decrease GABA (In Prefrontal Cortex; PFC, Hypothalamus/MPOA/PVN) (Includes Supplement Suggestions)

Perhaps , you want to decrease GABA to create an empathogenic effect (increasing empathy), or perhaps, to increase one's libido, or perhaps, to increase cognition/memory (1) (2). There are tons of reasons one may want to actually DECREASE/INHIBIT GABA in the brain..and believe it or not, there are some who claim ''too little anxiety'' - or perhaps, one is ridded with emotion so much that GABA is their accused culprit. Of course, these are all speculative scenarios...decreasing GABA has never really been proven to increase empathy, but there anecdotal reports and forum based hypothesis (3) (4).

Decreasing GABA though, does have supported applications in.

• Increasing Dopamine release. (4)
• Increasing sexual desire.        (5)
• Increasing Motivation.            (6)
• Improving Memory.                (7)

Some firm guidelines.

1. Serotonin and 5-HTP Increase hypothalamic GABA and this contributes to PRL-release and inhibition of libido and hormone secretion by Serotonin (8)
2. Dopamine D(2) (9) Dopamine D(4) Activation decrease GABA in the VTA and Supraoptic/Magnocellular Area's , respectively (10)
3. Adenosine A1-Receptors remarkably inhibit Striatal GABA Release (11).
4. Alpha-2-Adrenoreceptors enhance GABA release and Beta-adrenoreceptors decrease GABA release (norepinephrine/adrenaline receptors) (12)
5. Alpha-1 Adrenoreceptors reduce GABA in the VTA (13) but also DECREASE it (moreso) in the PVN/Hypothalamus. (14)

Now, here's a good outline of how to use SUPPLEMENTS to DECREASE GABA..

1. Use Tibetan SHILAJIT Paste to decrease Serotonin activity.
2. Use GINKGOLD™ ; A Patented Ginkgo Biloba Extract which directly antagonizes GABA-A Receptors...especially in the Hypothalamus (15) (16)  (17)
3. L-Histidine; which increases HA (Histamine), will decrease HYPOTHALAMUS GABA (18) (19) (20).
4. Eating FISH (Mackerel, Tuna, Herring, Sprat, Tilapia, Salmon) can increase histamine and the enzyme that helps the body produce it (HDC) (21) (22) (23) (24)
5. Tadalafil (Cialis) : Is known to improve memory/cognitive function/s and improve the Glutamate:GABA Ratio in the Brain (25).