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Alomone Labs Ivermectin activates α7 nicotinic AChR heterologously expressed in Xenopus oocytes.Current traces of α7 nicotinic AChR at -80mV holding potential. Currents were elicited by applications 10 µM acetylcholine every 50 seconds. Increases of these induced currents were achieved upon perfusion of 10 µM Ivermectin (#I-110), as indicated by the horizontal bar.
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Neuronal nicotinic acetylcholine receptors (nAChRs) are members of the Cys-Loop ligand-gated ion channel superfamily, located both in the peripheral and central nervous systems (PNS and CNS, respectively)1 and are validated therapeutic targets for various CNS pathologies2. They can be divided into two main groups: those that contribute to receptors that are sensitive to the snake toxin α-Bungarotoxin (αBgt) and those that do not bind this toxin. Another important distinction is that the three αBgt-sensitive subunits (α7–9) can reconstitute functional homomeric receptors when expressed in a host system.
Positive allosteric modulators (PAMs) do not bind to the orthostetic binding sites but allosterically enhance the activity elicited by agonists by increasing the gating process (type I) and/or by decreasing desensitization (type II). Ivermectin is a positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor; its prolonged pre-application to the neuronal nicotinic acetylcholine receptor α7 from human and chick results in potentiation of the acetylcholine-elicited current3. It is also a positive allosteric modulator of the purinergic P2X4 receptor4.
Ivermectin modulates glutamate- and GABA-activated Cl- channels5 and probably binds to two sites on the GABAergic receptor resulting in activation of the receptor after binding to the high-affinity site and blocking it on further binding to the low-affinity site6. It also potentiates glycine-gated currents at low concentrations (30 nM)7.
Ivermectin was also found to positively modulate human P2X7 receptor while having no effect on the mouse receptor8.
Ivermectin (#I-110) is a highly pure, synthetic, and biologically active compound.