A sigma receptor ligand; binds to σ1 and σ2 receptors in guinea pig brain membrane preparations (IC50s = 7 and 56 nM

Opipramol – 25 mg

Brand:
Cayman
CAS:
315-72-0
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Opipramol is a sigma-1 (σ1) and σ2 receptor ligand.{46600} It binds to σ1 and σ2 receptors in guinea pig brain membrane preparations (IC50s = 7 and 56 nM, respectively). It is 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 serotonin (5-HT) or norepinephrine uptake (IC50s = >10,000 nM for both), but does bind to histamine H1 and dopamine D2 receptors (IC50s = 12 and 120 nM, respectively), as well as the 5-HT receptor subtype 5-HT2 (IC50 = 120 nM). Opipramol (0.01 mg/kg) increases social interaction time in a social exploration test in rats, indicating anxiolytic-like activity. It also decreases immobility time in the forced swim test in rats, indicating antidepressant-like activity, when administered at a dose of 10 mg/kg.  

 

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SKU: 29471 - 25 mg Category:

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

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