Trazodone

Trazodone (AF-1161 free base) is a triazolopyridine derivative that belongs to the class of serotonin receptor antagonists and reuptake inhibitors (SARIs). Trazodone has anti-depressant and anti-insomnious activity. Trazodone exerts antagonistic properties against a1- and a2-adrenergic receptors and histamine H1 receptors, with minimal anticholinergic effects^[1]. In Vitro:Trazodone binds to 5-HT_1A receptor with a K_i of 23.6 nM^[3].
Trazodone (1 nM–10 μM, 24 h or 72 h) reduces the expression of neuroinflammatory markers by inhibiting key signaling pathways such as NF-κB, p38 MAPK, and JNK, exhibiting neuroprotective effects^[5].
In Vivo:Trazodone (1.5 mg/kg, i.p., single dose) reduces spontaneous motor activity in cats and dogs^[2].
Trazodone (100 mg/kg, i.p., single dose) reduces hyperactivity, prostration and clonic convulsions in cats and dogs^[2].
Trazodone (12.5-25 mg/kg, i.p., single dose) inhibits nicotine- and Oxotremorine (HY-170032)-induced tremor^[2].
Trazodone (5-20 mg/kg/day, s.c., 2-14 d) significantly decreases the spontaneous firing rate of DR 5-HT neurons by 40% and 37% with 10 and 20 mg/kg dose in SD rats^[4].