Sulfoxaflor

Sulfoxaflor is an orally active full agonist of insect nicotinic acetylcholine receptors (nAChRs), targeting the α-bungarotoxin-insensitive nAChR1 and nAChR2 subtypes. Sulfoxaflor binding to nACh is not inhibited by d-Tubocurarine (HY-125901), but is partially inhibited by Mecamylamine (HY-B1395A). Sulfoxaflor induces inward currents by activating nAChRs, leading to insect neurotoxicity. Sulfoxaflor can be used in the research of agricultural pest control, pesticide toxicology, insect neural receptor pharmacology, etc^[1][2]. In Vitro:Sulfoxaflor (1 mM; 300 ms) fully activates α-Bgt-insensitive nAChRs expressed on cockroach DUM neurons, evokes inward currents with an EC₅₀=153.7±10.2 μM^[1].
5 μM Mecamylamine (HY-B1395A) inhibits the current by 60%, while 20 μM d-Tubocurarine (HY-125901) has no blocking effect^[1]. In Vivo:Sulfoxaflor (5 μg·dm-3; dissolved in sucrose solution; daily free access; 2 weeks) causes bumblebee (Bombus terrestris) colonies reared from wild queens to produce significantly fewer worker bees during the early growth stages and fewer reproductive offspring than unexposed controls^[2].