Dibenzepine (hydrochloride)

Dibenzepine hydrochloride is a blood-brain barrier permeable ligand of the histamine H1 receptor (Histamine H1 Receptor), with a K_i value of 0.02 μM. Dibenzepine hydrochloride exhibits varying degrees of affinity for multiple serotonin receptors and dopamine receptors. Dibenzepine hydrochloride can be used in research related to depression, schizophrenia, dementia, and non-specific agitation^{[1][2][3][4][5][6][7][8][9][10]}. In Vitro:Dibenzepine (compound 5) exhibits high-affinity binding to the histamine H₁ receptor (K_i = 0.02 μM), shows moderate affinity for 5-HT₁A, 5-HT₂A, 5-HT₆, and 5-HT₇ receptors, weak affinity for SERT, and extremely low affinity for the D₂ receptor^[1].
Dibenzepine (1 μM-0.01 M; 1 h) inhibits hypotonic hemolysis of human erythrocytes and induces hemolysis at a concentration of 5 mM^[8]. In Vivo:Dibenzepine (3.5 mg/kg; administered daily for 28 consecutive days) increases the β-endorphin content in the brain of healthy albino Wistar rats to 906.63 pg/g^[10].