Sceletium is a monoamine releasing agent, rather than only a selective serotonin reuptake inhibitor.

[Alchemica]

High-mesembrine Sceletium extract (Trimesemine™) is a monoamine releasing agent, rather than only a selective serotonin reuptake inhibitor.

ETHNOPHARMACOLOGICAL RELEVANCE:

Extracts from and alkaloids contained in plants in the genus Sceletium have been reported to inhibit ligand binding to serotonin transporter. From this, the conclusion was made that Sceletium products act as selective serotonin-reuptake inhibitors. However, other mechanisms which may similarly result in the anxiolytic or anti-depressant effect ascribed to Sceletium, such as monoamine release, have not been investigated.

AIMS OF THE STUDY:

The current study investigated simultaneously and at two consecutive time points, the effect of high-mesembrine Sceletium extract on both monoamine release and serotonin reuptake into both human astrocytes and mouse hippocampal neurons, as well as potential inhibitory effects on relevant enzyme activities.

MATERIALS AND METHODS:

Human astrocytes and mouse hippocampal cells were treated with citalopram or Sceletium extract for 15 and 30 minutes, after which protein expression levels of serotonin transporter (SERT) and vesicular monoamine transporter-2 (VAMT-2) was assessed using fluorescent immunocytochemistry and digital image analysis. Efficacy of inhibition of acetylcholinesterase (AChE) and monoamine oxidate -A (MAO-A) activity were assessed using the Ellman and Olsen methods (and appropriate controls) respectively.

RESULTS:

We report the first investigation of mechanism of action of Sceletium extract in the context of serotonin transport, release and reuptake in a cellular model. Cell viability was not affected by Sceletium treatment. High-mesembrine Sceletium extract down-regulated SERT expression similarly to citalopram. In addition, VMAT-2 was upregulated significantly in response to Sceletium treatment. The extract showed only relatively mild inhibition of AChE and MAO-A.

CONCLUSIONS:

We conclude that the serotonin reuptake inhibition activity ascribed to the Sceletium plant, is a secondary function to the monoamine-releasing activity of high-mesembrine Sceletium extract (Trimesemine^TM).

Edited December 3, 2015 by Alchemica

[Alchemica]

Trying to learn how to edit wikipedia but that's proving a challenge for me - everyone else just seems to be referencing with <ref name="pmid26615766"/> type things but when I try that, it doesn't work. Can't spot a simple answer in the help.

If anyone wants to correct it, that would be appreciated https://en.wikipedia.org/w/index.php?title=Sceletium_tortuosum&action=edit&section=4

[gtarman]

I have no idea what any of that means in practical terms, but it sounds really interesting haha

[Alchemica]

See: https://en.wikipedia.org/wiki/Monoamine_releasing_agent

It gives some evidence to there being potential empathogenic/entactogenic ^[1] effects from Sceletium rather than actions of simple serotonin reuptake inhibition which generally doesn't discriminate as such. That said, I used to find acute doses of sertraline or paroxetine in particular somewhat empathogenic but maybe I'm just weird

So who's got a good source of mesembrine-rich extract?

Edited December 5, 2015 by Alchemica

[Psylocke]

You mean like this?