Description

Ivermectin is a macrocyclic lactone derived from Streptomyces avermitilis with antiparasitic activity. Ivermectin exerts its anthelmintic effect via activating glutamate (https://pubchem.ncbi.nlm.nih.gov/compound/glutamate)-gated chloride (https://pubchem.ncbi.nlm.nih.gov/compound/chloride) channels expressed on nematode neurons and pharyngeal muscle cells. Distinct from the channel opening induced by endogenous glutamate (https://pubchem.ncbi.nlm.nih.gov/compound/glutamate) transmitter, ivermectin-activated channels open very slowly but essentially irreversibly. As a result, neurons or muscle cells remain at either hyperpolarisation or depolarization state, thereby resulting in paralysis and death of the parasites. Ivermectin does not readily pass the mammal blood-brain barrier to the central nervous system where glutamate (https://pubchem.ncbi.nlm.nih.gov/compound/glutamate)-gated chloride (https://pubchem.ncbi.nlm.nih.gov/compound/chloride) channels locate, hence the hosts are relatively resistant to the effects of this agent.