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Lobeline HCl

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Chemical Structure| 134-63-4 同义名 : α-Lobeline hydrochloride;L-Lobeline hydrochloride;VUF 10751;(–)-α-Lobeline;(–)-Lobelin (hydrochloride);Lobeline hydrochloride
CAS号 : 134-63-4
货号 : A561413
分子式 : C22H28ClNO2
纯度 : 98%
分子量 : 373.916
MDL号 : MFCD00082455
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

H2O: 6 mg/mL(16.05 mM),配合低频超声助溶

动物实验配方:
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.67mL

0.53mL

0.27mL

13.37mL

2.67mL

1.34mL

26.74mL

5.35mL

2.67mL

参考文献

[1]Yalcindağ ON. [Stability of injectable lobeline hydrochloride to sterilization with steam and lobeline hydrochloride assay in solutions] . Turk Hij Tecr Biyol Derg. 1966;26(1):93-8. Turkish.

[2]DONZELOT E, MILOVANOVICH JB. [Effects of lobeline hydrochloride on the heart of the frog in situ] . C R Seances Soc Biol Fil. 1954 Jul;148(13-14):1167-70. French.

[3]Barlow RB, Johnson O. Relations between structure and nicotine-like activity: X-ray crystal structure analysis of (-)-cytisine and (-)-lobeline hydrochloride and a comparison with (-)-nicotine and other nicotine-like compounds. Br J Pharmacol. 1989;98(3):799-808

[4]Raj H, Singh VK, Anand A, Paintal AS. Sensory origin of lobeline-induced sensations: a correlative study in man and cat. J Physiol. 1995;482 ( Pt 1)(Pt 1):235-246

[5]Sapru HN, Krieger AJ. Carotid and aortic chemoreceptor function in the rat. J Appl Physiol Respir Environ Exerc Physiol. 1977;42(3):344-348

[6]McCrimmon DR, Lalley PM. Inhibition of respiratory neural discharges by clonidine and 5-hydroxytryptophan. J Pharmacol Exp Ther. 1982;222(3):771-777