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编 号：F514347
分子式：C22H27NO2
分子量：337.46
分子式：C22H27NO2
分子量：337.46
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CAS No: 90-69-7
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生物活性：
Lobeline (α-Lobeline) is a brain-penetrant nicotinic receptor agonist. Lobeline increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline is effective in smoking cessation.
体内研究：
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。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。Animal Model:Sprague-Dawley rats (200-250 g)
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.
体外研究：
Lobeline (0.1-100 μM) 诱导 [3H]DA 溢出呈非钙依赖性。Lobeline 抑制 [3H]DA 被突触小体 (IC50=80 μM) 和囊泡 (IC50=0.88 μM) 摄取。
Lobeline (α-Lobeline) is a brain-penetrant nicotinic receptor agonist. Lobeline increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline is effective in smoking cessation.
体内研究：
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。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。Animal Model:Sprague-Dawley rats (200-250 g)
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.
体外研究：
Lobeline (0.1-100 μM) 诱导 [3H]DA 溢出呈非钙依赖性。Lobeline 抑制 [3H]DA 被突触小体 (IC50=80 μM) 和囊泡 (IC50=0.88 μM) 摄取。
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