Azaphen (free base)

Azaphen free base (Azafen free base) is an orally active tricyclic antidepressant that inhibits the reuptake of serotonin and monoamines, regulates the 5-HT2c receptor, and exerts sedative, antidepressant and anxiolytic effects. Azaphen free base increases the bioavailability of serotonin in the synaptic cleft, does not block muscarinic receptors or affect monoamine oxidase activity, and binds to the human serotonin transporter via salt bridges, π-stacking, π-cation and hydrophobic interactions. Azaphen free base can be used in studies related to depression^[1][2][3]. In Vitro:Azaphen (5-20 mg/kg; p.o.; single dose) free base (Azafen free base) exhibits pronounced antidepressant activity in the Porsolt behavioral despair test, with significant reductions in immobility duration at oral doses of 5, 10, and 20 mg/kg^[2].
Azaphen free base exhibits pronounced antidepressant activity in the Normura forced swimming test with significant reductions in depressive state duration^[2]. In Vivo:Azaphen (Less than 1 mg; 0.5 s exposure per frame, 2° s^-1 rotation rate, 120° total rotation angle) free base (Azafen free base) has its first atomic solid-state structure solved by MicroED at 0.82 Å resolution, revealing two inversion-related conformers with minimal conformational flexibility that supports binding to its target protein^[3].
Azaphen free base binds preferentially to the allosteric (S2) site of hSERT with minimal conformational change from its solid-state structure, stabilized by multiple key interactions including a salt bridge, pi-stacking, and pi-cation interactions^[3].