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Thursday, October 22, 2015

How to Manipulate the Serotonergic (Serotonin) System for Optimal/Best Sleep (Treating Severe Insomnia Naturally/Herbally)

Alright ladies and Gentlemen; we have another important , prized topic to Cover.

This here is the new 'bee's knees' of information collection regarding serotoninergic manipulation. Now, for those unfamiliar, Serotonin is a neurotransmitter that is 89-91% in the GUT - ONLY 10% is in the brain/CNS. Of course, the nerves in your intestines/gut can be considered a part of the nervous system; the 'enteric' nervous system...which is basically getting into the enterokinetic or enteroelectric activities that facilitate bowel movement etc.

Serotonin has SEVEN receptors. That's a lot! It is surpassed only by glutamate in terms of QUANTITY of structurally different receptors and amino acid sequences.

Serotonin is considered a 'monoamine' - but not a catecholamine (which includes dopamine and noradrenaline). Serotonin interacts with a wide array of neurotransmitters in the brain and body; actually practically every neurotransmitter in influenced by serotonin - so you can see why it's important to keep it in the right range!

Serotonin can be either stimulating or sedating; but the network of current medical evidence suggests  that serotonin is more likely to CAUSE anxiety than to relieve it. Serotonin in moderately elevated or excessive amounts leads to problems regulating body temperature, Diarrhea, nausea, fast or slow heart rate, blood pressure dysregulation, sexual dysfunctions, panic , anger/agitation, callousness, visual changes, delirium, neurosis, erotomania (fixation on famous characters or students/teachers that leads to obsession and delusions of unmutual love)....

Additionally, serotonin can suppress REMS sleep and delay onset of sleep; depending on what receptor it binds to. 



  • Generally speaking, serotonin can reduce both onset of sleep and reduce quality of sleep when activating the post-synaptic 5-HT(1)A receptors.
  • 5-HT1B activation promotes anxiety and aggravates obsessive-compulsive symptoms.
  • Activating 5-HT(2)A or 2C leads to Anxiety and sleeplessness as well as personality changes such as mania, hallucinations if a high degree of activation is present (such as with LSD or Ecstasy)
  • 5-HT3 receptor activation may lead to anxiety and memory problems as well as nausea.
  • 5-HT4 activation increases heart rate and nervous system stimulation as well as histamine release and excessive serotonin at this receptor is implicated in heart failure.
  • 5-HT5A receptor activation can lead to Insomnia, lack of curiosity, lack of pleasure, psychosis and a whole host of other symptoms such as low thyroid hormone and low metabolism. 
  • 5-HT7 activation promotes anxiety and aggression, in some instances.

Serotonin thus is largely stimulating - and though is often proclaimed to be a 'marvel anxiolytic' - the science doesn't quite hold up...anyway.


Your best bet to a tactical approach is to reduce net/total serotonin levels and / or antagonize specific receptors - the ones that seem to be the worst are the 5-HT4 receptors and 5-HT5A receptors - as well as the 5-HT1A receptors.


My recommendation is the below stack. 

  • Wild Jujube (Ziziphus Spinosa) antagonizes 5-HT1A and 5-HT1B receptors(1) (2).
  • L-Lysine antagonizes serotonin 5-HT(4) receptors and relieves anxiety and gut pathology/diarrhea predominant IBS. (3)
  • Valerian Extract and Valerinic Acid act as partial agonists to the human serotonin 5-HT5A receptor - which may improve sleep by reducing serotonin activity by the autoreceptors and also by reducing net sympathetic nervous system activity. The partial agonist effect essentially means that VRE keeps the 5-HT5A receptors intrinsic activity/value at a median and / or reduces the excessive activation but when under - active will normalize it to control rates. (4)
                                             

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