Table 1.
Experimental Settings for Studying the Effects of Ivermectin on Ion Channels, FXR, NHR-8, Viruses, Malaria, Cancer, and Asthma
| Target | Experimental preparation | Concentration: ng/ml (nM) | Refs and comment |
|---|---|---|---|
| AVR-15b Haemonchus contortus channel opening | HEK293 expressed | EC50 19 (22 nM) | [28] |
| Abamectin on GluCls of Ascaris suum pharynx inhibition | Dissected whole worm pharynx | EC50 350 (400 nM) | [37] |
| Brugia malayi mf protein release, ES inhibition by Bma-AVR-14A GluCl | Whole Brugia and microfilaria | <88 (<100 nM) | [31] |
| Downregulation of B. malayi meiosis genes | Whole Brugia | <88 (<100 nM) | [8] |
| A. suum GABA ion-channel inhibition | Dissected preparation | <175 (<200 nM) | [27] |
| Histamine-gated Cl channel activation | Expressed channel from Drosophila melanogaster | 875 (1000 nM) used | [33] |
| pH-gated Cl channel activation | Sarcoptes scabiei oocyte expressed receptor | Single conc 10 000 (11 429 nM) | [34] |
| Nematode nAChRs | Expressed channels and A. suum preparation | EC50 368 (420 nM) | [35,37] |
| FXR activation and transcription | FXR and ivermectin Crystal structure and mice, serum glucose and cholesterol decrease | 1300 μg/kg per day for 14 days | [69–72] Repurpose or find more potent analog |
| NHR-8 transcription factor | NHR-8 of Caenorhabditis elegans and H. contortus | Knockout in C. elegansreduced ∼2 LDA (from 1.63 to 0.96 nM) | [104] Low level of resistance |
| Dengue; West Nile virus; Venezuelan equine encephalitis virus inhibition | Tissue culture inhibition transport into by nuclear importin α/β1 | IC50s 875–3500 (1000–4000 nM) | [55–61] More potent analog required to be effective |
| SARS-Covid-2 inhibition | Tissue culture | 4375 (5000 nM), ∼ 100× | [107] |
| Plasmodium inhibition | Culture: inhibition of Plasmodium in liver inhibits nuclear import of signal recognition particles of P. falciparum | IC50 ∼438 (∼500 nM) | [65–67] More potent analog required to be effective. Ivermectin has effects on mosquitoes |
| Cancer | Tissue culture and mice experiments by different mechanisms | <8000 nM | [76,77,79–83,105] High concentrations required for effects |
| Asthma | Mice: reduction of cellular and humoral responses to antigen in asthma model | 2000 μg/kg | [89] High μg/kg dose |