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Autism Coach

BH4- Biopterin-Pteridin


BH4- Biopterin-Pteridin

0.25 LBS

Product Description

1-29-20 - Backorder Status Update

About a week ago we spoke with the manufacturer and they assured us it would be back in stock by the end of January.  Today we called to double-check that it would be shipping and were told it now has an estimated arrival time of mid-Feburary.  Because of this, we have stopped taking advance orders until it has been shipped.   Our apologies.  If anyone would like a refund at this time, please email and we will refund your money. 

Now TENTATIVELY on backorder until February 15, 2020

 Tetrahydrobiopterin (also known as BH4 or Biopterin) may be a critical nutrient for individuals within the autism spectrum.  BH4 is a molecule that is naturally produced by the body.  It has been shown to be 42% lower in the cerebro spinal fluid of children diagnosed with autism.* 

Biopterin is depleted by the man-made chemical, glyphosate, the active ingredient in the the weed killer, Roundup, that contaminates most of the U.S. food supply.  Millions of tons of Roundup have been sprayed on agricultural fields since genetically modified (GMO) crops were introduced in 2000.  Virtually every person in the United States is contaminated with glyphosate in their body.  The increase in the incidence of autism directly correlates to the introduction and increase of glyphosate into the food supply. (5)  Glyphosate actually increases levels of ammonia in the body and BH4 is one of the primary molecules used by the body to break down and excrete ammonia.

What is BH4 and what does it do?  It is a molecule that activates (initiates a chemical reaction) for important metabolic processes in the body:

  • converts the amino acid phenylalanine into the amino acid tyrosoine - too much phenyalanine can cause a form of brain damage called phenylketonuria; phenyalanine levels tend to be high in autism
  • converts the amino tryptophan into the active form 5-hydroxytryptophan (5-HTP), a molecule that is used to produce the neurotransmitters serotonin (for alertness and good mood) and melatonin (promotes sleep)
  • converts tyrosine to the neurotransmitter L-DOPA, L-DOPA is needed to make the neurotransmitters norepinephrine and epinephrine
  • converts the amino acid arginine to nitric oxide (NO); nitric oxide helps to dialate blood vessesls allowing oxygen and nutrients to reach cells more efficiently; not enough nitric oxide can cause neurovascular disease, including contributing to circulation diseases like diabetes
  • helps to remove excess levels of ammonia in the body

Metabolic Pathways Disrupted by Low Levels of BH4

BH4 is not only is involved in the formation of neurotransmitters, but also involved in heart, and endothelial dysfunction, the immune response, and pain sensitivity, forming lipids (membranes), and recycling and making folate, methylfolate, and SAMe, all critical for neurological function and detoxificationThe figure below shows processes in which BH4 is critical.  BH4 is is used to make several neurotransmitters but is also used to detoxify toxins such as ammonia.  Chronic and excessive levels of inflammation due to factors such as a vaccine reaction use up BH4 so there is not enough to make neurotransmitters.  BH4 is very sensitive to toxins that produce oxidative stress driven by chronic inflammation, which causes it to irreversibly degrade into dihydroxyanthopterin (XPH2).  

In animal and human studies, when BH4 is decreased the following metabolic disruptions occur:

  • the ratio of phenylalanine to tyrosine increases, leading to increased fatigue severity
  • was also increased and this correlated with fatigue severity, as well as with reductions in
  • reduced levels of of dopamine and HVA in the cerebral spinal fluid
  • a decrease in bioavailability of monoamine neurotransmitters, including tyrosine and tryptophan, and the development of symptoms related to decreased levels of neurotransmitters


The figure below shows how BH4 is made in the BH4/BH2 Metablic cycle and how it is frequently used up by the Urea Cycle instead of being used to make Neurotransmitters and in the Folate Cycle is critical for methylation processes that turn genes on and off. 

disrupted-pathways-1-2-24-18.jpgAn initial study done with autism by Dr. Frye indicated it helped some individuals with autism. (1)

The importance of BH4 was not lost on a Swiss pharmaceutical company, who somehow manged to obtain a monopoly on it and an affordable product incredibly expensive and difficult to obtain.  Because of this, this product is expensive to make and frequently out of stock (the last time it was out of stock for over a year).  If you do order it, store it in the freezer to extend the shelf life.  It is very expensive for us to obtain it but we offer $15 off the suggested retail price.

Lack of BH4 bioavailability can lead to the development of impaired NO-mediated microvascular function in a wide variety of conditions, including diabetes, hypertension, hypercholesterolemia, atherosclerosis, and aging.  Nitric oxide synthases (NOS) needs BH4 for the production of nitric oxide. When there is low BH4 concentration, NOS generates superoxide instead of NO, which increases oxidative stress and causes endothelial dysfunction.  Oxidative stress  can contribute to many complications, such as heart disease, high cholesterol, diabetes, high blood pressure, and stroke. Supplementation with BH4 may restore BH4 concentrations and prevent these diseases.  Infusion of BH4 could restore the heart conditions in patients with high cholesterol, type II diabetes, congestive heart failure and heart disease.

Depression is associated with an inflammatory response as well as activation of the anti-inflammatory reflex system. It is also accompanied by oxidative and nitrosative stress (2).

Elevated levels of inflammation and oxidative damage can subsequently lead to a depletion of tetrahydrobiopterin levels (2, 3).

The depletion of BH4 reduces the synthesis of neurotransmitters that compounds are essential for controlling daily body functions including mood, sleep cycle, memory, and appetite (2).  Loss of BH4 might explain some of the symptoms of depression. If BH4 levels increased, then it can be an effective treatment for depression (2).

Diabetes is characterized by glucose intolerance and insulin resistance, which can be caused by endothelial nitric oxide synthase (eNOS) dysfunction. Diabetes can also cause gastroparesis, and its symptoms include pain, nausea, and vomiting (2,3).  BH4 helps regulate eNOS activity and prevents it from dysfunction. Administration of BH4 in mice lead to less glucose intolerance and insulin resistance; it has potential to help alleviate symptoms of diabetes (2, 3).

There are various genes that when mutated can cause lower BH4.  These include:

  • Defects in the MTHFR gene
  • Defects in the DHFR gene
  • Defects in the GCH1 gene
  • Defects in the SPR gene

In addition to taking BH4 directly  the following supplements can help to increase levels of BH4 in the body:

Exercise can also increase levels of BH4

Supplement Facts

Serving Size:  1 capsule


Vitamin C (as ascorbic acid) 10 mg,

Tetrahydrobiopterin (a stable form of the physiologic agent, biopterin) 2.5 mg.

Other ingredients: Sucrose, Gelatin, L-Leucine.


1.  RE Frey et al., Neurotherapeutics.  2010 July; 7(3):  241-249





* The statements made in this description have not been evaluated by the Food and Drug Administration.  This product is not intended to diagnose, treat, cure or prevent any disease.

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