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首页 / 抑制剂/激动剂 / 神经信号通路 /
DAT
AChR
/ Lobeline HCl

盐酸洛贝林 /Lobeline HCl {[allProObj[0].p_purity_real_show]}

货号：A561413 同义名： α-Lobeline hydrochloride;L-Lobeline hydrochloride Ambeed 开学季，买赠积分，赢豪礼

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.

Lobeline HCl 化学结构 CAS号：134-63-4
Lobeline HCl 化学结构
CAS号：134-63-4
Lobeline HCl 3D分子结构
CAS号：134-63-4
Lobeline HCl 化学结构 CAS号：134-63-4
Lobeline HCl 3D分子结构 CAS号：134-63-4
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Lobeline HCl 纯度/质量文件 产品仅供科研

货号：A561413 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 AChE ↓ AChR ↓ mAChR ↓ nAChR ↓ 其他靶点 纯度
Donepezil +++

hAChE, IC50: 11.6 nM

bAChE, IC50: 8.12 nM

 		{[allProObj[0].p_purity_real_show]}
Loganin ++

AChE, IC50: 3.95 μM

 		{[allProObj[0].p_purity_real_show]}
topride HCl ++

AChE, IC50: 2.04 μM

 		{[allProObj[0].p_purity_real_show]}
Dehydroevodiamine HCl ✔ {[allProObj[0].p_purity_real_show]}
Jatrorrhizine ++

AChE, IC50: 872 nM

 		{[allProObj[0].p_purity_real_show]}
Palmatine ++

AChE, IC50: 0.51 μM

 		{[allProObj[0].p_purity_real_show]}
(-)-Huperzine A ++++

AChE (G4 form), Ki: 7 nM

 		{[allProObj[0].p_purity_real_show]}
Galanthamine HBr ++

AChE, IC50: 0.35 μM

 		{[allProObj[0].p_purity_real_show]}
Trospium chloride ✔ {[allProObj[0].p_purity_real_show]}
Tiotropium Bromide Monohydrate ✔ {[allProObj[0].p_purity_real_show]}
Gallamine Triethiodide +

AChR, IC50: 68.0 μM

 		{[allProObj[0].p_purity_real_show]}
Hexamethonium Bromide ✔ {[allProObj[0].p_purity_real_show]}
Pancuronium dibromide ✔ {[allProObj[0].p_purity_real_show]}
Neostigmine bromide ✔ {[allProObj[0].p_purity_real_show]}
Orphenadrine citrate ✔ {[allProObj[0].p_purity_real_show]}
Oxybutynin ✔ {[allProObj[0].p_purity_real_show]}
Irsogladine ✔ PDE {[allProObj[0].p_purity_real_show]}
Pyridostigmine bromide ✔ {[allProObj[0].p_purity_real_show]}
Rivastigmine +

AChR, IC50: 5.5 μM

 		{[allProObj[0].p_purity_real_show]}
Paroxetine hydrochloride ✔ {[allProObj[0].p_purity_real_show]}
Rocuronium Bromide ✔ {[allProObj[0].p_purity_real_show]}
Tropicamide +++

M4 mAChR, IC50: 8 nM

 		{[allProObj[0].p_purity_real_show]}
Diphenmanil methylsulfate ✔ {[allProObj[0].p_purity_real_show]}
Umeclidinium bromide ✔ {[allProObj[0].p_purity_real_show]}
Otilonium bromide ✔ {[allProObj[0].p_purity_real_show]}
Flavoxate HCl +

mAChR, IC50: 12.2 μM

 		{[allProObj[0].p_purity_real_show]}
Ipratropium bromide ✔ {[allProObj[0].p_purity_real_show]}
Diphenidol HCl ✔ {[allProObj[0].p_purity_real_show]}
Darifenacin hydrobromide ++++

M3 mAChR, pKi: 8.9

 		{[allProObj[0].p_purity_real_show]}
Aclidinium Bromide ++++

M4 mAChR, Ki: 0.21 nM

M2 mAChR, Ki: 0.1 nM

 		{[allProObj[0].p_purity_real_show]}
Oxybutynin chloride ✔ {[allProObj[0].p_purity_real_show]}
Pentoxyverine citrate ✔ {[allProObj[0].p_purity_real_show]}
Solifenacin ✔ {[allProObj[0].p_purity_real_show]}
Catharanthine ✔ {[allProObj[0].p_purity_real_show]}
Benzethonium chloride +++

α4β2 nAChRs, IC50: 49 nM

α7 nAChRs, IC50: 122 nM

 		{[allProObj[0].p_purity_real_show]}
Vinblastine sulfate +

nAChR, IC50: 8.9 μM

 		{[allProObj[0].p_purity_real_show]}
PNU-120596 ++

α7 nAChR, EC50: 216 nM

 		{[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Lobeline HCl 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].

Lobeline HCl 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

Lobeline HCl 实验方案

计算器
存储液制备 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

Lobeline HCl 技术信息

CAS号134-63-4
分子式C22H28ClNO2
分子量 373.916
别名 α-Lobeline hydrochloride;L-Lobeline hydrochloride;VUF 10751;(–)-α-Lobeline;(–)-Lobelin (hydrochloride);Lobeline hydrochloride
运输蓝冰
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

Tags: Lobeline | 134-63-4 | α-Lobeline | L-Lobeline | Nicotinic Receptor Agonist | Membrane Transporter/Ion Channel | Neuronal Signaling | nAChR | Dopamine Transporter | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Lobeline HCl 纯度/质量文件 | Lobeline HCl 亚型比较 | Lobeline HCl 生物活性 | Lobeline HCl 参考文献 | Lobeline HCl 实验方案 | Lobeline HCl 技术信息

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