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• W1999463859 abstract "Glutamate-gated chloride channels (GluCls) are inhibitory neurotransmitter receptors that are present only in invertebrates such as nematodes and insects. These channels are important targets of insecticidal, acaricidal, and anthelmintic macrolides such as avermectins, ivermectin (IVM), and milbemycins. To identify the amino acid residues that interact with IVM in GluCls, three IVM B1a derivatives with different photoreactive substitutions at C-13 were synthesized in the present study. These derivatives displayed low- or subnanomolar affinity for parasitic nematode (Haemonchus contortus) and silkworm (Bombyx mori) GluCls expressed in COS-1 cells. The derivatives also activated homomeric H. contortus GluCls expressed in Xenopus oocytes. The results indicate that synthesized photoreactive IVM B1a derivatives have superior affinity and functionality for chemically labeling the macrolide-binding site in GluCls. ." @default.
• W1999463859 created "2016-06-24" @default.
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• W1999463859 date "2015-05-01" @default.
• W1999463859 modified "2023-09-25" @default.
• W1999463859 title "Synthesis of photoreactive ivermectin B 1a derivatives and their actions on Haemonchus and Bombyx glutamate-gated chloride channels" @default.
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• W1999463859 doi "https://doi.org/10.1016/j.pestbp.2014.10.017" @default.
• W1999463859 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/25987225" @default.
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