Description
A sigma receptor ligand; binds to σ1 and σ2 receptors in guinea pig brain membrane preparations (IC50s = 7 and 56 nM, respectively); selective for σ1 and σ2 over histamine H2, dopamine D1, α1- and α2-adrenergic, and muscarinic M1 receptors (IC50s = 4,300, 900, 200, 6,100, and 3,300 nM, respectively) and has no effect on 5-HT or norepinephrine uptake (IC50s = >10,000 nM for both); binds histamine H1 and dopamine D2 receptors (IC50s = 12 and 120 nM, respectively) and 5-HT2 (IC50 = 120 nM); ex vivo, binds to brain σ1 and σ2 receptors in mice (ED50s = 1 and 8 mg/kg, respectively); increases social interaction time in a social exploration test in rats at 0.01 mg/kg; decreases immobility time in the forced swim test in rats at 10 mg/kg
Formal name: 4-[3-(5H-dibenz[b,f]azepin-5-yl)propyl]-1-piperazineethanol
Synonyms: G-33040|GR-33040|NSC 169867
Molecular weight: 363.5
CAS: 315-72-0
Purity: ≥98%
Formulation: A crystalline solid
