5 replies to this topic

[Chris Malone]

http://www.ncbi.nlm....pubmed/24239329
http://en.wikipedia....iki/Tesofensine

Upregulates dopaminergic pathways, 90% bioavailability with a 220 hour half-life, metabolized by cytochrome P4503A4 (CYP3A4) for which there are plenty of natural inhibitors.
It sounds like it might do wonders for amphetamine/phenylethylamine tolerance. I can't find anything about it in the forums.. maybe because it's mainly known as an appetite suppressant?
I would be really interested in a group buy for this.

Edited by Chris Malone, 07 February 2014 - 07:32 AM.

[jadamgo]

Bump. I'm not personally interested - NRIs and I don't get along very well - but I'd be interested to hear others' experiences with this.

[mrd1]

Hmmm very interesting! So far I see

IC50 levels of (the lower the number the more its strength) for
1. norepinephrine 1.7 nm
2. seritonin 11 nm
3. dopamine 65 nm

as well as increase the expression of
1. bovine derived neurotrophic factor (bdnf)
2. Arc expression in ca1 of hippocampus

(Expression of brain derived neurotrophic factor, activity-regulated cytoskeleton protein mRNA, and enhancement of adult hippocampal neurogenesis in rats after sub-chronic and chronic treatment with the triple monoamine re-uptake inhibitor tesofensine)

And, that the increase in mRNA Arc expression could be from the increase bdnf I suppose? Given that bdnf seems to have the ability to activate arc. [ “The EJC factor eIF4AIII modulates synaptic strength and neuronal protein expression.” Cell. 130:179-191. ]

If arc does indeed play a role in learning and memory ( “The EJC factor eIF4AIII modulates synaptic strength and neuronal protein expression.” Cell. 130:179-191. ) And, BDNF, the norepinephrine, seritotonin, and dopamine reuptake inhibition all play a role in providing a antidepressant effect, this compound does seem very interesting.

However, given the easy availability of SSRIs NDRIs and compounds that increase BDNF, will this ever be cost effective? Perhaps it will be of best use to people who don't like swallowing a bunch of pills? I personally don't mind swallowing a SSRI NDRI and BDNF booster.

Edited by mrd1, 19 February 2014 - 08:48 AM.

[xks201]

I doubt I would touch any drug with a 220 hr half life.

[Doc Psychoillogical]

Emoxypine

(Emoxypine looks more promising, effective, and similar to Tesofensine)

Mechanism of action

Emoxypine's mechanism of action is believed to be its antioxidant and membrane-protective effects with the following key components:^{[3][6][medical citation needed]}

• Emoxypine effectively inhibits free radical oxidation of biomembrane lipids, reacts to peroxide radicals of lipids primary and hydroxyl radical of peptides
• Increases the activity of antioxidant enzymes, specifically that of superoxide dismutase, responsible for the formation and consumption of lipid peroxides and active oxygen forms
• Inhibits free radicals during the synthesis of prostaglandin catalyzed cyclooxygenase and lipoxygenase, increases the correlation prostacyclin/ thromboxane A2 and blocks the leukotriene formation
• Increases the content of polar fraction of lipids (phosphatidyl serine and phosphatidyl inositol) and reduces the cholesterol/phospholipids ratio which proves its lipid-regulatory properties; shifts structure transition into the low temperature zones, that is provokes the reduction of membrane viscosity and the increase of its fluidity, increases lipid-protein ration.
• Modulates the activity of membrane-bound enzymes: phosphodiesterase, cyclic nucleotides, adenylate cyclase, aldoreductase, acetylcholinesterase.
• Modulates the receptor complexes of the brain membranes, i.e. benzodiazepine, GABA, acetylcholine receptors by increasing their binding ability.
• Stabilizes biomembranes, i.e. membrane structures of blood cells - erythrocytes and thrombocytes during their haemolysis or mechanical injury accompanied by the formation of free radicals.
• Changes the monoamine level and increases the dopamine content in the brain.

 

 

Studies,Clinical trials, and research has shown:

Uses/Applications

 

+anxiolytic,

+anti-stress,

+anti-alcohol,

+anticonvulsant,

+nootropic/neuroprotective & anti-inflammatory actions

+improves cerebral blood circulation,

+inhibits thrombocyte aggregation,

+lowers cholesterol levels,

+ cardioprotective & antiatherosclerotic actions

[YimYam]

• I want to modulate my GABA receptors without taking Benzos and generally normalise my HPA as much as possible. Fluoxetine has been excellent for normalising my HPA (75% healed), but I feel GABA is the main culprit in getting me to 100% healed or close. 

 

Do you think this med sounds useful for my disorder?

 

 

You mention that its a serotonin-noradrenaline-dopamine reuptake inhibitor, but I see no mention of its effects on serotonin in your list. 

 

 

Pardon my lack of knowledge but is this the equivalent of an SSRI and Benzo being fusioned together? I presume if i wanted to try it I'd have to go off my ssri.

 

Thanks!