Scorpion toxins are specific and have a high affinity for their targets, and this makes them good tools to characterize various receptor proteins involved in ion channel functioning.

Because only low amounts of natural toxins can be isolated from scorpion venoms, a chemical synthesis approach has been utilised to produce sufficient protein for research.

This approach is not only produces enough material to study the effects on potassium channels but ensures purity as toxin isolated from the scorpion venom risks contamination by other active compounds.

Kv1.2 channel regulates neurotransmitter release associated with heart rate, insulin secretion, neuronal excitability, epithelial electrolyte transport, smooth muscle contraction, immunological response and cell volume.

Margatoxin significantly reduces outward currents of Kv1.3 channels and depolarized resting membrane potential.

The disturbance of the function of Kv1.3-channels, for example due to inhibition of these channels, will lower the cytokines production and lymphocyte proliferation in vitro.

Pharmacological studies suggest that functional potassium channels are required in the activation of T- and B-cells.

Margatoxin blocks mitogen-induced proliferation, the mixed lymphocyte response and the secretion of Interleukin-2 and interferon-gamma (IFN-γ).

The median lethal dose (LD50) of margatoxin is 59.9 mg/kg, so Centruroides margaritatus stings are not dangerous to humans except as a result of possible anaphylactic responses.

An eight-day treatment led to a prolonged immune suppression that lasted three to four weeks after termination of dosing.

This is commonly seen to cause failure of interventional clinical procedures that include placement of stents and bypass grafts.

Due to changes in potassium channel type the vascular smooth muscle cells switch from the contractile to proliferating phenotype.

Inhibitors of such channels suppress vascular smooth muscle proliferation, stenosis following injury, and neointimal hyperplasia.

Studies shows that margatoxin is a high potency inhibitor of vascular cell migration, with an IC50 (half maximal inhibitory concentration) of 85 pM.

There have been vasoconstrictor effects observed in some arteries, but elevated blood pressure has not appeared as a significant concern.