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Sunday, February 8, 2015

Natural NOREPINEPHRINE Only Reuptake INHIBITORS (Natural NET Inhibitors)

In my quest to find natural norepinephrine transporter inhibitors - AKA NorAdrenaline reuptake inhibitors AKA natural NET Inhibitors - I have come across three easily obtainable "remedies" that also have a fair amount of LEGIT, unquestionable science behind them.

But real quickly , why would one want a norepinephrine inhibitor, and not a dopamine reuptake inhibitor, or serotonin reuptake inhibitor?

  • Norepinephrine is a form of adrenaline, thus if you have low blood pressure - it may be one part of one means to increase it.
  • NorAdrenaline can be made more efficient by increasing it's activity; and thus can be a side-kick to a formidable natural anti-depressant.
  • Norepinephrine (NORadrenaline) is involved in attentiveness to detail, in particular lights, smells and colors. 
  • Low levels of norepinephrine often result in  "depressive like symptoms" with sensory deficiency and low enthusiasm / quality of life. 
  • Rasing the activity of norepinephrine may improve energy levels and treat SOME** ADD symptoms and may help to counter the lethargy associated with many anti-psychotic/mood stabilizing drugs.
  • It may help in increments to restore normal visual processing capacity, naturally!

The first natural norepinephrine reuptake inhibitor would be ginkgo biloba extract; however, it is not purely so - it also antagonizes GABA-A and affects receptor expression across the board. Mainly influencing the 5-HT1A receptors (preventing loss of) and increasing muscarinic receptors if they are decreased by age.

 2009 Jul;60(1):68-73. doi: 10.1016/j.phrs.2009.02.012. Epub 2009 Mar 21.

Ginkgo biloba extract (EGb761) influences monoaminergic neurotransmission via inhibition of NE uptake, but not MAO activity after chronic treatment.


In order to explain cognition-enhancing effects of standardized Ginkgo biloba extract (EGb761), an increase of central monoaminergic neurotransmission has been suggested, but the underlying mechanisms have not yet been elucidated. Here, we confirm that the norepinephrine (NET), the serotonin (SERT), the dopamine (DAT) uptake transporters and MAO activity are inhibited by EGb761 in vitro, although rather high concentrations are required for inhibition of MAO-A and MAO-B activity. However, after 14 days of daily oral treatment with 100mg/kg EGb761 only NE uptake is significantly decreased in NMRI mice, while 5-HT uptake and MAO activity are not affected. As synaptic dopamine clearance in the frontal cortex is mediated by NET, not DAT, these findings may give an explanation for the enhancement of dopaminergic neurotransmission by EGb761 seen in animal models, presumably linked to its positive effects on cognition and attention.
[PubMed - indexed for MEDLINE]



"This one is a real gem, with additional dopamine reuptake inhibiting properties and listed as an MAO-Inhibiting herb."

It's mentioned on a discussion forum called "DR.BOB" and reiterated as the new "god-tier herb" and future phenomenon on longecity!

 2009 May;66(9):1617-29. doi: 10.1007/s00018-009-9030-9.

In vitro dopaminergic neuroprotective and in vivo antiparkinsonian-like effects of Delta 3,2-hydroxybakuchiol isolated from Psoralea corylifolia (L.).


Cocktail recipes containing Psoralea corylifolia seeds (PCS) are used to empirically treat Parkinson disease. A PCS isolate Delta(3),2-hydroxybakuchiol (BU) can inhibit dopamine uptake in dopamine transporter (DAT) transfected Chinese hamster ovary (CHO) cells, and dopamine reuptake blockade may provide an alternative approach for ameliorating parkinsonism. Here, we assessed the potential dopaminergic neuroprotective, and antiparkinsonian-like activity of BU. BU sample size was increased by using a scale-up extraction paradigm. Pharmacologically, BU significantly protected SK-N-SH cells from 1-methyl-4-phenylpyridinium (MPP(+)) insult, produced striking inhibitory actions on dopamine/norepinephrine uptake and WIN35,428 binding in synaptosomes on in vivo administration, and significantly preventing poor performance on rotarod and dopaminergic loss in substantia nigra in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) mice. BU acts by protecting dopaminergic neurons from MPP(+) injury and preventing against MPTP-induced behavioral and histological lesions in the Parkinson's disease (PD) model, possibly by inhibiting monoamine transporters. These findings suggest that BU could be meaningful in PD treatment.

Antidepressant-like effects of psoralen isolated from the seeds of Psoralea corylifolia in the mouse forced swimming test.

Bakuchiol analogs inhibit monoamine transporters and regulate monoaminergic functions.

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