Phosalone

Phosalone is an orally active, blood-brain barrier penetrant Insecticide and acaricide. Phosalone inhibits the activity of Acetylcholinesterase. Phosalone acts as a substrate for detoxifying esterases. Phosalone induces symptoms of cholinergic hyperactivity, toxic reactions, mortality, oxidative stress, and changes in pro-inflammatory protein levels, and exerts toxic effects on colonic tissues and cells. Phosalone controls pistachio psyllids. Phosalone can be used in studies related to colitis^[1][2][3]. In Vitro:Phosalone (Five or six distinct concentrations; 24 h) exhibits variable toxicity to 5th instar nymphs of nine Agonoscena pistaciae populations, with the Rafsanjan (RF) population showing the highest resistance (11.3-fold) and the Bam (BA) population being the most susceptible (LC₅₀ = 55 mg/L)^[3].
Phosalone (Various concentrations; 8 h) is 15.65-fold more toxic to susceptible (BA) adult Agonoscena pistaciae (LC₅₀ = 1.14 mg/L) than to resistant (RF) adults, with TPP (synergist ratio 3.14) and DEM (synergist ratio 1.41) enhancing phosalone toxicity in RF adults, while PBO acts antagonistically (synergist ratio 0.45)^[3]. In Vivo:Phosalone (4-130 mg/kg; p.o.; single dose) has an acute oral LD₅₀ of 120 mg/kg in combined male and female CD (COBS) rats, with minimal lethal doses ranging from 67 to 100 mg/kg depending on sex^[1].
Phosalone (4-36 mg/kg; p.o.; single dose) inhibits erythrocyte, plasma, and brain cholinesterase in female CD (COBS) rats after single oral administration, with peak erythrocyte cholinesterase inhibition (ID₅₀ = 10.5 mg/kg) occurring 5 hours post-dose^[1].
Phosalone (6-40 mg/kg; gavage; daily; 30 days) induces dose-dependent colon inflammation and oxidative stress in male Wistar rats, with the highest tested dose (40 mg/kg, 1/3 LD₅₀) causing the most severe reductions in AChE activity, total thiols, and antioxidant power, plus the greatest elevations in inflammatory markers, myeloperoxidase activity, and lipid peroxidation^[2].