Eprinomectin B1a is a semi-synthetic analogue of avermectin B1a prepared by oxidation of the 4''-hydroxy moiety and reductive amination followed by acetylation. Eprinomectin B1a is the major component (>90%) of the commercial product for endo- and exo-parasite control, eprinomectin. The avermectins and milbemycins are also potent insecticides and acaricides.
Eprinomectin B1a is soluble in ethanol, methanol, DMF or DMSO. Poor water solubility.
Eprinomectin B1a is soluble in ethanol, methanol, DMF or DMSO. Poor water solubility.
Mechanism of Action | Members of the avermectin/milbemycin class exert their anthelmintic effects by binding to glutamate-gated chloride channels expressed on nematode neurones and pharyngeal muscle cells. |
References | 4-Keto- and 4-amino-4-deoxy avermectin compounds and substituted amino derivatives thereof. Mrozik H.H. et al. 1984 US Patent 4,427,663. Synthesis of 4"-epi-amino-4"-deoxyavermectins B1. Cvetovich R.J. et al. J. Org. Chem. 1994, 59, 7704. Efficacy in sheep and pharmacokinetics in cattle that led to the selection of eprinomectin as a topical endectocide for cattle. Shoop W.L. et al. Int. J. Parasitol. 1996, 26, 1227. |