IVERMECTIN

[A macrocyclic lactone derived from Streptomyces avermitilis with antiparasitic activity. Ivermectin exerts its anthelmintic effect via activating glutamate-gated chloride channels expressed on nematode neurons and pharyngeal muscle cells. Distinct from the channel opening induced by endogenous 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 results in paralysis and death of the parasites. Ivermectin does not readily pass mammal blood-brain barrier to central nervous system where glutamate-gated chloride channels locate, hence the hosts are relatively resistant to the effects of this agent. ( NCI )]

UMLS (NCI) C0022322