Hordenine
Neurotransmitter Booster
Hordenine is a phytochemical that occurs in a number of different plants. It’s a natural neural
stimulant and nootropic that can enhance your cognitive functions, stimulate higher energy levels and
improve your mood. Hordenine is a biogenic amine that
regulates neurotransmitters. Hordenine is a mild, short acting
nerve stimulant in man that causes a release of norepinephrine.
It’s also a highly selective substrate of MAO-B and acts as a
temporary reversible MAO-B inhibitor. Because Hordenine
crosses the blood brain barrier it is able to inhibit MAO-B
enzymes in both the body and brain.
Hordenine is an alkaloid of the phenylethylamine class and a biogenic amine. Hordenine gained
attention after it appeared in the serum or horses fed sprouted barley that contains Hordenine
and indirectly acted as an adrenal gland stimulant. Hordenine is one of the many biogenic
amines found in bitter orange, a popular dietary supplement.
REGULATES NEUROTRANSMITTERS
Hordenine binds to special trace amine receptors that regulate neurotransmitters. Trace amines occur
in low levels in our brain. They’re structurally similar to neurotransmitters like dopamine, epinephrine
and serotonin. Important trace amines found in your body include β-phenethylamine and tryptamine.
Studies conducted in the last five years, have shown the importance of trace amines as
neuromodulators in the brain. They alter monoamine neurotransmitters transporter function by
binding with paired Trace Amine-Associated Receptors (TAAR). And they keep neurotransmitter
levels within their normal range of activity. Of significant importance, Hordneine’s binding of TAAR1
was found almost identical in potency to the same concentration of β-phenethylamine in binding
TARR1.
,
An expanding base of research show that trace amine and TARR dysfunctions play an important role
in causing a in a diverse array of human disorders. Furthermore, trace amines may be used
therapeutically for treating many behavioral and cognition disorders The lists includes attention
deficit disorders, drug dependence, addiction, depression, overeating, stress, and anxiety disorders.
ADRENAL-LIKE ACTIONS
Hordenine exerts both stimulant and neuromodulating effects. Researchers found that Hordenine is a
reuptake inhibitor of norepinephrine. It blocks the transporter-mediated reuptake of the
neurotransmitter norepinephrine, into the neuron from the synapse, (the space between adjoining
neurons). As a result, Hordenine can increase the level of the brains natural energizer
norepinephrine. In high animal dosages Hordenine has produced adrenalin-like stimulation.
NATURAL MAO-B INHIBITION
The research of Dr C. J. Barwell found it work as an selective and reversible MAO-B inhibitor.
Monoamine Oxidase (MAO) is an enzyme that breaks down the neurotransmitters dopamine,
phenylethylamine and others. By inhibiting the effects of MAO enzyme in preventing neurotransmitter
Copyright NanoSphere Health Sciences, LLC 2014. breakdown from occurring, neurotransmitter levels and activity increase. Because Hordenine crosses
the blood brain barrier it may able to inhibit MAO-B enzymes in both the body and brain.
MAO-B inhibitors are safe to take and a lot different that the MAOI inhibitors. MAOI inhibitors prevent
breaking down excess levels of tyramine that can cause blood pressure to skyrocket and result in a
hypertensive crisis. Remarkably, studies found that MAO-B inhibits the negative effects of tyramine.
AGING INCREASES MAO-B AND NATURAL DECLINE
Numerous papers have demonstrated that MAO-B activity progressively increases in the aging brain
and this increase plays a role in initiating aging. According to the research of Dr. Edward Knoll,
higher function neuron and cell loss is a general feature of the aging brain. The accompanying
selective increase of MAO-B activity with increasing age severely depresses necessary levels of
monoamine neurotransmitters. This leads to a major catecholamine and trace-amine deficiency. This
mechanism is responsible for the age-related decline in sexual and learning performances, and
ultimately leads to natural death.
To counteract this mechanism, Knoll recommends the daily dose of an enhancer substance to keep
the engine of their brain on a higher activity level in adulthood. According to Knoll It will improve the
quality of life in the latter decades, increase the chances for a longer life, and decrease the danger of
precipitating age-related depression and neurodegenerative diseases
β-phenethylamine (PEA) is the brains natural enhancer substance but suffers the fate of being rapidly
broken down by MAO-B. Knoll believes this contributes to neuronal loss and accelerated aging
decline. By contrast, the synthetic enhancer substance deprenyl derived from PEA is a potent,
selective MAO-B inhibitor that effectively prevents higher levels of neuron loss, protects the brain and
fights aging.
Deprenyl was developed in Hungary more than 30 years ago by Dr Knoll. It’s the only selective MAOB inhibitor in medical use and became the standard treatment for Parkinson’s disease during the
1990′s. Four series of rat experiments, and experiment with dogs, have shown that deprenyl can
extend lifespan significantly, even beyond the “technical lifespan” of a species. This adds
experimental proof to Dr Knoll’s research of enhancer regulation and aging decline.
CAN HORDENINE FIGHT AGING?
Deprenyl works in part because it inhibits MAO-B and is self-protected from quickly breaking down.
This helps allow it to activate neurons and increase levels of dopamine, PEA and other
neurotransmitters that maintain the brain in a high level of activity throughout your lifespan. Likewise
Hordenine is an MAO-B inhibitor and could be taken in conjunction with PEA. Hordenine would help
prevent PEA breakdown, and enable PEA function in a similar manner as an enhancer substance
throughout life that protects neurons from aging, fights aging decline, improves cognition, protects the
brain, and boosts performance.
References
1. Barwell C.J. Iinhibition of guinea pig liver monoamine oxidase-b by Hordenine (njn-dimethyl tyramine.) Br Journal
Pharmacol 2012
2. Barwell CJ, Basma AN, et al. Deamination of hordenine by monoamine oxidase and its action on vasa deferentia
of the rat; School of Pharmacy, Portsmouth Polytechnic, Hampshire, UK; J Pharm Pharmacol. 1989
Jun;41(6):421-3;
Copyright NanoSphere Health Sciences, LLC 2014. 3. Berry, M.D., The Potential of Trace Amines and Their Receptors for Treating Neurological and Psychiatric
Diseases. Reviews on Recent Clinical Trials, 2007, 2, 3-19
4. Branchek TA, Blackburn TP. Trace amine receptors as targets for novel therapeutics: legend, myth and fact. Curr
Opin Pharmacol 2003; 3: 90-97.
5. Burzow R, Sonders MS. et al Amphetamine, 3,4-methylenedioxymethamphetamine, lysergic acid diethylamide,
and metabolites of the catecholamine neurotransmitters are agonists of a rat trace amine receptor. Mol.
Pharmacol. 2001 601181-1188
6. Duke,JA. Jo M. et al. Duke's Handbook of Medicinal Herbs of Latin America; CRC Press, 2009;416
7. Finberg JP, Gillman K. Selective inhibitors of monoamine oxidase type B and the "cheese effect". Int Rev
Neurobiol. (2011)
8. Frank M, et al. Hordenine: pharmacology, pharmacokinetics and behavioural effects in the horse. Equine Vet J.
(1990)
9. Hapke HJ, Strathmann W. Pharmacological effects of hordenine. Dtsch Tierarztl Wochenschr. (1995)
10. Knoll J Deprenyl (selegiline).The history of its development andpharmacological action. Acta Neurol Scand Suppl
1983 95:57-80
11. Knoll J Pharmacological basis of the therapeutic effect of (-)deprenyl inage-related neurological diseases. Med
2es Rev 199312:505-524
12. Knoll, J. The Brain and Its Self: A Neurochemical Concept of Innate and Acquired Drives. 2005 Springer Verlag
13. Knoll, J. The mechanism of the anti-aging effect of Depreny.l Anti-aging Bulletin Winter 2003 International
Antiaging Systems Ltd
14. Magyar, K. et al. “The pharmacology of B-type selective monoamine oxidase inhibitors; milestones in deprenyl
research” J Neural Transm (Suppl) 1996 48, 29-43.
15. Sander LC, et al. Certification of standard reference materials containing bitter orange. Anal Bioanal Chem.
(2008)
16. Youdim, M. Finberg, J. “Pharmacological actions of L-deprenyl (selegeline) and other selective monoamine
oxidase B inhibitors” Clin Pharmacol Ther 1994 56, 725-33.
These statements have not been evaluated by the Food and Drug Administration.
This product is not intended to diagnose, treat, cure, or prevent any disease
Copyright NanoSphere Health Sciences, LLC 2014.