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CAS No.: 134-63-4

Lobeline HCl/盐酸洛贝林 Catalog No. CSN19428

Synonyms: α-Lobeline hydrochloride;L-Lobeline hydrochloride;α-Lobeline HCl

Lobeline HCl is a mixed agonist–antagonist of nAchR agonist and has multiple function such as VMAT2 ligand, inhibiting the reuptake of dopamine and serotonin, antagonist at μ-opioid receptors and P-glycoprotein inhibitor.

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技术信息

生物活性

描述Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes. The pKa of (-)-lobeline HCl at 25 degrees C is 8.6 (approx), indicating that (-)-lobeline is at least 90% in the protonated form at physiological pH (7.6) ^[3]. Intravenous injections of lobeline HCl into twenty-six normal young male human volunteers produced sensations of choking, pressure or fumes in the throat and upper chest at a mean threshold dose of 12 micrograms kg-1^[4]. Sodium cyanide, lobeline HCl, and doxapram HCl in the doses of 2-400 mug/kg injected into the external carotid artery stimulated respiration significantly. Injections of the drugs into the ascending aorta produced less effects which were abolished after section of the carotid sinus nerves. The drugs produced a significant increase in the carotid sinus nerve activity but failed to do so in the aortic depressor or recurrent laryngeal nerves^[5]. Stimulation of carotid body chemoreceptors by i.a. injections of lobeline, doxapram or 0.015 N HCl in saline also briefly reinstates phrenic nerve discharges after inhibition by clonidine. Inhibition is also overcome during electrical stimulation of the carotid sinus nerve^[6].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00664703	Attention Deficit Disorder Wit... more >>h Hyperactivity Collapse <<	Phase 2	Completed	-	United States, Kentucky ... more >> General Clinical Research Center, University of Kentucky Lexington, Kentucky, United States, 40506 Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6744 mL
- 13.3720 mL
- 26.7440 mL
- 5 mM
- 0.5349 mL
- 2.6744 mL
- 5.3488 mL
- 10 mM
- 0.2674 mL
- 1.3372 mL
- 2.6744 mL

技术信息

CAS号

134-63-4

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H28ClNO2

运输

蓝冰

分子量

373.92

别名

α-Lobeline hydrochloride;L-Lobeline hydrochloride;α-Lobeline HCl;L-Lobeline HCl;(-)-Lobeline HCl;(–)-Lobelin (hydrochloride);(–)-α-Lobeline;VUF 10751;盐酸洛贝林

溶解度

DMSO	230.0 mg/mL (615.1 mM)
Water	insoluble

动物实验配方

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