Fluralaner 是一种异恶唑啉杀外寄生虫剂。 它有效且选择性地抑制 GABA 受体通道阻滞剂 EBOB 与家蝇头膜的结合，IC50值为 455 pM。

Fluralaner is an isoxazoline ectoparasiticide. It potently and selectively inhibits binding of the GABA receptor channel blocker EBOB to housefly head membranes (IC50: 455 pM).

A1443 inhibits specific binding of the gamma-aminobutyric acid (GABA) receptor channel blocker EBOB to housefly-head membranes, with an IC(50) value of 455pM. In contrast, the IC(50) value in rat-brain membranes is>10muM. A1443 blocks GABA- and glutamate-induced chloride currents in Xenopus oocytes expressing MdGBCl or MdGluCl channels, with IC(50) values of 5.32 and 79.9 nM, respectively [1]. Fluralaner potently inhibited flea reproduction capacity in vitro. Oviposition ceased completely at concentrations as low as 25.0 ng/mL. While no ovicidal effect was observed, fluralaner exerted a larvicidal effect at exceptionally low concentrations (6.25 ng/mL) [2].

In the simulated flea-infested home environment, flea-control efficacy on fluralaner-treated dogs was >99% at every time point measured for 12 weeks. No adverse events were observed in fluralaner-treated dogs [2]. No adverse events were observed subsequent to fluralaner treatment of MDR1(-/-) Collies at three times the highest expected clinical dose [3].

864731-61-3

C22H17Cl2F6N3O3

556.29

氟雷拉纳;A1443;AH252723

H2O:Insoluble
DMSO:100 mg/mL (179.76 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years