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Wednesday, May 13, 2015

How to Prevent/Reverse Dopamine Receptor Downregulation from Dopamine Agonists, Stimulants and other Causes

While it is certainly notable that many neurodegenerative diseases can cause malfunction in dopamine neurons (Parkinson's, MS, Infections, FMNP, CFS) - that doesn't mean that dopamine issues can not occur without their involvement...and organic and / or idiopathic (of unknown cause) dopamine deficiency is not the only form of imbalance nor does it always affect receptor expression and / or internalization.

There's also drug-induced downregulation - a problem encountered often in scientific study and sometimes in mental patients taking specific Psychiatric medications. Some antibiotics may influence receptor expression as well.

ADHD sufferer's who take Ritalin should be made aware that their medication may decrease in effectiveness over time - in part due to downregulation of dopamine receptors as well as increase in dopamine transporter activity...

Parkinson's patients on dopamine agonist drugs may experience a lessening in effects/benefits after the period of 3-6 months - an effect that can also be prevented and / or reversed by the below methods.

My only main recommendation to both prevent and reverse downregulation is one backed up by clear scientific study

A stack consisting of ...
(NOTE: You only have to use 2 or 3 out of these but you CAN use all five if you wish, it might be a bit overkill though.)

1.) Phenyl Piracetam 
 This is a racetam derivative / analogue that has the unique ability to increase dopamine D1, D2, D3 expression and to protect dopaminergic neurons(1) (2). It has nootropic effects , thus improving cognitive/brain function and can be bought over the counter.

HOW TO TAKE IT: Take 100mg 2-3 times a day, dose the latest dose at evening time no later than 6 PM. Take for at least 3-6 months during or post-treatment.

Can be purchased here -->

2.) Tianeptine
Use with caution and start with low doses, tianeptine is a serotonin modulating and dopamine enhancing anti-depressant/nootropic with a strong safety record and low remission rate (3). Tianeptine can improve anxiety and depression while boosting dopamine receptor concentration(4).

HOW TO TAKE IT : Take it at dosage of 12 mg THREE TIMES A DAY. Do this for 3-6 months, ideally..although as with phenyl piracetam, you will notice benefits within the first weeks - peak effects and such occur later. 

It can be purchased at Ceretropic over the counter --> 


Usage of lavender has been shown to also increase dopamine receptor concentration (5) and to help alleviate stress - it is one of the most powerful natural anti-anxiety remedies also has benefits in those with OCD; Obsessive-Compulsive-Disorder(6).

I recommend the 'Young Living' Lavender essential oil. {CLICK HERE}

4.) Inositol 
Inositol is shown to increase STRIATAL dopamine D(2) receptor concentration specifically. 
Must be used continuously(7)
I recommend Solgar brand. {CLICK HERE}


Forskolin raises HUMAN DOPAMINE D(2)L receptors and also promotes nitric oxide activity. THIS ONE is especially good for increasing libido / arousal and for enhancing the WORK OUT PUMP! (8) (9)
Forskolin is studied in potential erectile dysfunction treatments. (10)

I recommend Analyzed Supplements 'Forskolin-95'
Click the word or the image below to go to the Product Page.

click here now


  1. Wow, cool post. I’d like to write like this too – taking time and real hard work to make a great article… but I put things off too much and never seem to get started. Thanks though.
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  2. You might want to change the dosing on the Tianeptine recommendation to a once a day with a 40mg dose; you linked the sulfate version but provided the tianeptine sodium dosing schedule.

  3. What about Memantine? What do you think of that, if dosed at small amounts ?