Why is dopamine important?
As we age, our dopaminergic neurons – the main source of dopamine in the mammalian central nervous system – either gets damaged or dies. Although dopaminergic neurons correspond to less than 1% of the total number of brain neurons, they play a crucial role in controlling several aspects of the basic brain functions such as motor behavior, motivation, and working memory (Chinta & Andersen., 2004).
A study was done on the characteristics of dopamine neuron responses to primary rewards and reward-predicting stimuli in monkeys. The results showed an increased firing of the dopamine neurons when the monkeys were given an unpredicted reward, while the absence of an expected reward has inhibitory effects. This has led to the proposal that dopamine neurons function as detectors of reward prediction errors (Schultz, 2002). Likewise, dopamine also regulates our brain’s emotional and movement responses, and pleasure.
On the other hand, a deficiency of dopamine causes several disease conditions such as Parkinson’s disease and drug addiction. Therefore, regulation of dopamine plays an important role in both the mental and physical health.
Addiction & Tolerance
In the brain, pleasure is tied with dopamine release in the nucleus accumbens – a cluster of nerve cells lying underneath the cerebral cortex. It is the speed with which dopamine is released, the intensity of that release, and the reliability of that release that is linked with addiction. All drugs can cause this powerful surge of dopamine and depend on the method of administration which can greatly influence the likelihood that will lead to addiction. For example, injecting the drug intravenously commonly produces a faster, stronger dopamine signal than swallowing it as a pill.
Addictive drugs also provide a shortcut for dopamine and other neurotransmitters to flood the brain in a quick and reliable way. The unnatural rush of dopamine makes it difficult for the brain receptors to withstand because the brain is naturally conditioned to receive rewards with time and effort. This leads to the brain producing less dopamine or eliminating dopamine receptors. As a result, dopamine has less impact on the brain’s reward center making the desired drug becomes less pleasurable, an effect known as tolerance. The only options in order to feel the same effects are to increase the dosage or cycle off.
Smart Drugs that involve dopamine
Currently, there is no information stating that smart drugs will make the brain healthier. It has little to no concern about the long-term side effects making it quite dangerous if taken for a duration of time. Other than that, two smart drugs that involve dopamine are Modafinil and Sulbutiamine.
Modafinil is an ingredient found in various smart drugs and it has the ability to increase the user’s alertness and energy levels. It works by restraining the actions of the dopamine transporter, leading to the increase in extracellular and synaptic concentrations of dopamine. This promotes a natural sense of wakefulness in the user by raising the hypothalamic histamine levels (Ishizuka et al., 2003). Additionally, Modafinil restrains the GABAergic neurotransmission and activates the glutamatergic circuits in the brain (Gerrard & Malcolm, 2007). As a result, the user is able to concentrate, learn and perform various mental tasks at ease. The short-term side effects of Modafinil include a headache, anxiety, and a decrease in appetite, nausea, and insomnia.
Sulbutiamine is a synthetic vitamin derivative of Vitamin B1/Thiamine that has stimulating properties. The mechanism of action is not entirely understood, but dopamine and the cholinergic system is involved. Once Sulbutiamine is in the brain, thiamine phosphate levels increase. Thiamine is then used to produce both GABA and acetylcholine which increases the levels of D1 and D2 receptors. This elevates the feeling of pleasure and the ability to focus on a task. On the other hand, it is listed to be potentially addictive and a buildup of tolerance can occur.
Nootropics that involve dopamine
If it gets you high, wired, sedate or altered it is a smart drug and not a Nootropic. This is because Nootropic does not seem to have adverse body side effects, impaired brain function, neurotransmitter depletion, or tolerance/habit-forming potential. Nootropic is/should be sustainable and focuses on mild metabolic and nutritive for long term gains and protection. Some Nootropics ingredients that involve dopamine are CDP Choline, Gingko Biloba, Hordenine, L-Phenylalanine, L-Tyrosine, Mucuna Pruriens.
CDP-choline (citicholine) converts choline and cytidine into uridine in the body. Uridine can produce positive health effects on humans which include improving brain function and aid in treating mental disorders, reduce pain, and protect the heart (Robinson et al., 2017). It also has been suggested that it augments dopaminergic signaling by both increasing levels of the dopamine transporter and by increasing the amount of dopamine released from a stimulated neuron (“CDP-choline”, n.d.).
Ginkgo Biloba is leaves from the Ginkgo Biloba tree and it acts as an antioxidant and improves circulation of blood flow to the brain. Many people take it to ward off dementia, stay mentally sharp, and improve memory. It is an inhibitor of the platelet activating factor (PAF) receptor which may underlie some neuroprotective effects. Additionally, oral ingestion of Ginkgo Biloba subchronically appears to increase dopamine concentrations in the prefrontal cortex, which seems to be related to the flavonoids rather than terpenoids (“Ginkgo biloba”, n.d.). However, even though Ginkgo Biloba can boost cognition, its effect is not very reliable.
L-phenylalanine is a bio-available amino acid that the body converts into L-tyrosine by an enzyme in the liver called phenylalanine hydroxylase. The L-tyrosine is later converted into L-3,4-dihydroxyphenylalanine, known as L-DOPA. The decarboxylation of L-DOPA results in the synthesis of the neurotransmitter dopamine. The remaining dopamine that is not used by the brain is available to produce norepinephrine (noradrenaline) and epinephrine (adrenaline) which helps with concentration, organize thoughts and emotions, sleeping, dreaming, and learning.
L-tyrosine is an indirect precursor to L-DOPA which is then converted into dopamine by the enzyme AADC. Just like L-phenylalanine, after dopamine is used up, the remaining is used to produce norepinephrine (noradrenaline) and epinephrine (adrenaline).
Macuna Pruriens comes from the velvet bean and contains high amounts of L-DOPA. Again, L-DOPA is a natural precursor to dopamine, so the benefits include enhance motivation/reward messaging system
CDP-choline – Scientific Review on Usage, Dosage, Side Effects. (n.d.). Retrieved March 29, 2017, from https://examine.com/supplements/cdp-choline/
Chinta, S. J., & Andersen, J. K. (2004, December 2). Dopaminergic neurons. Retrieved March 29, 2017, from http://www.sciencedirect.com/science/article/pii/S1357272504003711
Gerrard, P., & Malcolm, R. (2007, June). Mechanisms of modafinil: A review of current research. Retrieved March 29, 2017, from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2654794/
Ginkgo biloba – Scientific Review on Usage, Dosage, Side Effects. (n.d.). Retrieved March 29, 2017, from https://examine.com/supplements/ginkgo-biloba
Ishizuka, T., Sakamoto, Y., Sakurai, T., & Yamatodani, A. (2003, March 20). Modafinil increases histamine release in the anterior hypothalamus of rats. Retrieved March 29, 2017, from https://www.ncbi.nlm.nih.gov/pubmed/12614915
Robinson, L., Segal, J., & Smith, M. (2017, January). The Mental Health Benefits of Exercise. Retrieved March 29, 2017, from https://www.helpguide.org/articles/exercise-fitness/emotional-benefits-of-exercise.htm
Schultz, W. (2002, February 11). Dopamine neurons and their role in reward mechanisms. Retrieved March 29, 2017, from http://www.sciencedirect.com/science/article/pii/S0959438897800074
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