Rocastine fumarate

Rocastine (0.08-6.07 mg/kg; oral gavage; various pretreatment times prior to histamine challenge) fumarate is a potent, rapid-acting antihistamine, with oral PD₅₀ values as low as 0.08 mg/kg^[1].
Rocastine (0.46-26.10 mg/kg; oral gavage; 1, 3, or 6 hours prior to histamine challenge) fumarate potently protects guinea pigs from histamine-induced prostration, with an oral PD₅₀ of 0.46 mg/kg at 1-hour pretreatment and 2.34 mg/kg at 3-hour pretreatment, demonstrating greater potency than pyrilamine at these time points^[1].
Rocastine (0.316-3.16 mg/kg; oral gavage; 1 hour prior to antigen challenge) fumarate potently protects actively sensitized guinea pigs from antigen-induced anaphylactic collapse, with an oral PD₅₀ of 1.00 mg/kg at 1-hour pretreatment^[1].
Rocastine fumarate blocks histamine-induced hypotension in cats at intravenous doses starting at 1 mg/kg, and does not induce EEG changes indicative of sedation even at a total cumulative dose of 39.9 mg/kg^[1].
Rocastine fumarate does not potentiate yohimbine-induced toxicity in female ICR mice at oral doses of 31.6 mg/kg and 66.0 mg/kg, indicating a lack of CNS depressant activity at these doses^[1].