Nemifitide (diTFA)

Nemifitide diTFA (INN 00835 diTFA) is a 5-HT2A receptor ligand that crosses the blood-brain barrier. Nemifitide diTFA is used in research related to major depressive disorder^[1][2][3]. In Vitro:Nemifitide diTFA (INN 00835 diTFA) and its active metabolite (M1) bind to 5-HT2A, 5-HT2C, melanocortin MC4, MC5, and bombesin receptors at micromolar concentrations in cell-free biochemical assays^[1].
Nemifitide diTFA binds to 5-HT₂A, 5-HT₂C, NPY1, MC4, MC5, and bombesin receptors in cell-free biochemical assays^[2].
Nemifitide diTFA undergoes extensive metabolism in rat and human intestinal and liver enzyme preparations in vitro^[3]. In Vivo:Nemifitide (0.0125-15 mg/kg; i.p.; daily; 14 days) diTFA (INN 00835 diTFA) produces antidepressant-like effects in male FSL rats via a U-shaped dose-response curve, with significant increases in forced swim test swimming time observed at doses from 0.025 mg/kg to 0.3 mg/kg and 3.0 mg/kg to 15.0 mg/kg after 14 days of daily intraperitoneal administration^[2].
Nemifitide (0.3 mg/kg; i.p.; daily; 5 days) diTFA produces a rapid-onset antidepressant-like effect in male FSL rats, significantly increasing forced swim test swimming time after just 5 days of daily intraperitoneal administration of 0.3 mg/kg^[2].
Nemifitide (0.3 mg/kg; i.p.; daily; 14 days) diTFA produces prolonged antidepressant-like effects in male FSL rats, with significantly increased forced swim test swimming time persisting for at least 5 days after cessation of 14 days of daily intraperitoneal administration of 0.3 mg/kg^[2].
Nemifitide (0.3 mg/kg; i.p.; daily; 14 days) diTFA does not produce antidepressant-like effects in male FRL control rats, as 14 days of daily intraperitoneal administration of 0.3 mg/kg does not significantly increase forced swim test swimming time^[2].
Nemifitide (0.3 mg/kg; i.p.; daily; 14 days) diTFA produces antidepressant-like effects in male HDS and LDS rats, significantly increasing forced swim test swimming time after 14 days of daily intraperitoneal administration of 0.3 mg/kg^[2].
Nemifitide (0.3 mg/kg; i.p.; daily; 14 days) diTFA produces antidepressant-like effects in female FSL rats, significantly increasing forced swim test swimming time after 14 days of daily intraperitoneal administration of 0.3 mg/kg^[2].