Abstract
Agonism of insect odorant receptor (OR) cation channels may represent a new strategy for the manipulation of destructive insect olfactory-driven behaviors. We have explored the chemical space around VUAA1, the first in class agonist of the obligate OR co-receptor ion channel (Orco), and describe novel compound analogues with increased potency across insect taxa. Functional analyses reveal several of these VUAA1 structural analogues display significantly greater potency as compared to the activity of the previously described active compounds in mobility-based behavioral assays on mosquito larvae.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anopheles / drug effects*
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Behavior, Animal
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HEK293 Cells
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Humans
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Ion Channels / drug effects
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Larva / drug effects
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Motor Activity / drug effects
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RNA, Small Interfering / chemistry
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RNA, Small Interfering / pharmacology
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Receptors, Odorant / agonists*
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Structure-Activity Relationship
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Thioglycolates / chemical synthesis*
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Thioglycolates / pharmacology*
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Triazoles / chemical synthesis*
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Triazoles / pharmacology*
Substances
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Ion Channels
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N-(4-ethylphenyl)-2-((4-ethyl-5-(3-pyridinyl)-4H-1,2,4-triazol-3-yl)thio)acetamide
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RNA, Small Interfering
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Receptors, Odorant
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Thioglycolates
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Triazoles