Description |
Lobeline (α-Lobeline; L-Lobeline), a lipophilic alkaloidal, is a nicotinic receptor agonist. Lobeline inhibits d-methamphetamine self-administration with no dopaminergic toxicity. Lobeline rescues d-amphetamine abuse induced addictive effect. Lobeline increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage[1][2][3].
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In Vitro |
Lobeline (0.1-100 μM) 诱导 [3H]DA 溢出呈非钙依赖性[1]。 Lobeline 抑制 [3H]DA 被突触小体 (IC50=80 μM) 和囊泡 (IC50=0.88 μM) 摄取[1]。 Lobeline (0.1-1μM; 1 h) 抑制 1 μM d-methamphetamine 诱导的纹状体切片释放多巴胺[2]。
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In Vivo |
Lobeline (0.3-3.0 mg/kg; 皮下注射; 单剂量) 降低模型大鼠 d-methamphetamine 的自我给药能力[3]。 Lobeline (3 mg/kg; 皮下注射; 7 个周期,共 7 次) 以非竞争性的方式特别降低大鼠对 d-methamphetamine 的反应,并增加耐受性发展[3]。 Animal Model: Sprague-Dawley rats (200-250 g)[3] Dosage: 0.3 mg/kg, 1.0 mg/kg, and 3.0 mg/kg for acute administration; 3 mg/kg for chronic administration Administration: Subcutaneous injection; 15 min prior to measurement, or every 15 min for 7 sessions; separated by 2 intervening maintenance days of d-methamphetamine (0.05 mg/kg/infusion) self-administration Result: Decreased d-methamphetamine Self-Administration.
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Density | 1.1±0.1 g/cm3 |
Boiling Point | 485.6±15.0 °C at 760 mmHg |
Flash Point | 247.5±20.4 °C |
Exact Mass | 337.204193 |
PSA | 40.54000 |
LogP | 3.61 |
Vapour Pressure | 0.0±1.3 mmHg at 25°C |