Opipramol

A σ receptor ligand

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库存: 现货

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5mg

￥712.00

570.00

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10mg

￥1175.00

940.00

- +
25mg

￥2712.00

2170.00

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货号: ajcx20382
CAS: 315-72-0
别名: 奥匹哌醇; Ensidon; G-33040
分子式: C23H29N3O
分子量: 363.5
纯度: >98%
溶解度: Acetonitrile: slightly soluble,Chloroform: slightly soluble,Methanol: slightly soluble
储存: Store at -20°C
库存: 现货

Background

Opipramol is a sigma-1 (σ1) and σ2 receptor ligand.1 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.

|1. Müller, W.E., Siebert, B., Holoubek, G., et al. Neuropharmacology of the anxiolytic drug opipramol, a sigma site ligand. Pharmacopsychiatry 37(Suppl 3), S189-S197 (2004).