Galanthamine hydrobromide
目录号 : GC36103
Galanthamine氢溴酸盐是长效的中心活性的乙酰胆碱酯酶（AChE）抑制剂，IC50为410 nM，同时是神经元烟碱乙酰胆碱受体的变构增强剂。
Cas No.:1953-04-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Galanthamine hydrobromide is a long-acting, centrally active acetylcholinesterase(AChE) inhibitor (IC50 = 410 nM) and allosteric potentiator at neuronal nicotinic ACh receptors. IC50 Value: 410 nM Target: AChEGalanthamine hydrobromide prevents β-amyloid-induced apoptosis in SH-SY5Y and bovine chromaffin cells. Long-term administration reduces amyloid precursor protein deposition and neurodegeneration in a mouse model of Alzheimer's disease.
[1]. Kita Y, Ago Y, Takano E, Fukada A, Takuma K, Matsuda T.Galantamine increases hippocampal insulin-like growth factor 2 expression via α7 nicotinic acetylcholine receptors in mice.Psychopharmacology (Berl). 2012 Aug 30. [2]. Berkov S, Viladomat F, Codina C, SuÁrez S, Ravelo A, Bastida J.GC-MS of amaryllidaceous galanthamine-type alkaloids.J Mass Spectrom. 2012 Aug;47(8):1065-73. [3]. Park CW, Son DD, Kim JY, Oh TO, Ha JM, Rhee YS, Park ES.Investigation of formulation factors affecting in vitro and in vivo characteristics of a galantamine transdermal system.Int J Pharm. 2012 Oct 15;436(1-2):32-40. Epub 2012 Jul 5. [4]. Park YS, Kim SH, Kim SY, Kim YH, Lee MH, Yang SC, Shaw LM, Kang JS.Quantification of Galantamine in Human Plasma by Validated Liquid Chromatography-Tandem Mass Spectrometry using Glimepride as an Internal Standard: Application to Bioavailability Studies in 32 Healthy Korean Subjects.J Chromatogr Sci. 2012 Jun 28. [5]. Arias et al Galantamine prevents apoptosis induced by b-amyloid and thapsigargin: involvement of nicotinic acetycholine receptors. Neuropharmacology (2004) 46 103.
| Cas No. | 1953-04-4 | SDF | |
| Canonical SMILES | O[C@@H]1C[C@@H]2OC3=C4C(CN(C)CC[C@]42C=C1)=CC=C3OC.Br | ||
| 分子式 | C17H22BrNO3 | 分子量 | 368.27 |
| 溶解度 | Water: 25 mg/mL (67.88 mM); DMSO: ≥ 3.7 mg/mL (10.05 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7154 mL | 13.577 mL | 27.154 mL |
| 5 mM | 0.5431 mL | 2.7154 mL | 5.4308 mL |
| 10 mM | 0.2715 mL | 1.3577 mL | 2.7154 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
In vitro metabolism of Galanthamine hydrobromide (Nivalin) by rat and rabbit liver homogenate
Eur J Drug Metab Pharmacokinet 1987 Jan-Mar;12(1):25-30.PMID:3609070DOI:10.1007/BF03189858.
The metabolism of Galanthamine hydrobromide (Nivalin) was investigated in rat and rabbit liver homogenates. Experiments were carried out varying several parameters of incubation: substrate (Galanthamine hydrobromide, galanthamine, galanthaminone and epigalanthamine), cofactor enrichment (NADPH, NADP/G-6-P, NAD), pH (7.4 and 9.3), time of incubation. Substrates and metabolites were identified and quantitatively determined by GC/MS. In vitro metabolism in rat liver homogenate was negligible. The experiments with rabbit liver homogenate indicated, that galanthamine was actively metabolised the major metabolites being the oxidised product - galanthaminone, and the isomer of galanthamine - epigalantamine. The experimental results show that the metabolism of galanthamine is substrate and product stereoselective.
Pharmacokinetics of Galanthamine hydrobromide after single subcutaneous and oral dosage in humans
Pharmacology 1989;39(1):50-8.PMID:2587617DOI:10.1159/000138571.
Galanthamine hydrobromide (Nivalin, dose 10 mg) was given subcutaneously and orally to 8 volunteers. Galanthamine and its metabolites were quantified in plasma and urine by reversed-phase HPLC. An unusual two-stage absorption and biexponential drug decline were observed. Galanthamine plasma peaks (1.24 micrograms/ml after subcutaneous and 1.15 micrograms/ml after oral doses) were reached 2 h following administration, the t1/2(beta) values being 5.70 and 5.26 h, respectively. Minor epigalanthamine and galanthaminone plasma levels were detected. An almost complete urinary recovery of galanthamine and its metabolites was obtained within 72 h. The plasma AUC, Cmax, tmax and ka suggest that the subcutaneous and oral Nivalin formulations are bioequivalent.
Influence of the cholinesterase inhibitor Galanthamine hydrobromide on normal sleep
Psychiatry Res 1994 Mar;51(3):253-67.PMID:8208872DOI:10.1016/0165-1781(94)90013-2.
Evidence from animal experiments has suggested that the triggering and maintenance of rapid eye movement (REM) sleep is mainly under the control of cholinergic neurons in the brain stem. Correspondingly, studies in humans have demonstrated that the application of cholinergic agonists or cholinesterase inhibitors provokes an earlier onset of REM sleep. The present study investigated the influence of Galanthamine hydrobromide, a reversible cholinesterase inhibitor, on REM sleep regulation in 18 healthy volunteers. After an adaptation night, the subjects were given two doses of galanthamine (10 mg and 15 mg) or placebo at 10 p.m. in a randomized double-blind design. Both doses of galanthamine shortened REM latency (with statistical significance depending on the definition of REM latency used), increased REM density, and reduced slow wave sleep mainly in the first non-REM cycle. Higher doses of galanthamine (15 mg) seem to be accompanied by unwanted side effects that warrant the application of a peripheral antidote. These results are comparable to those for other cholinomimetics and stress the usefulness of galanthamine for pharmacological challenge studies in healthy subjects and depressed patients.
Pharmacokinetics of Galanthamine hydrobromide (Nivalin) following single intravenous and oral administration in rats
Pharmacology 1986;32(6):301-6.PMID:3725886DOI:10.1159/000138184.
A study on Galanthamine hydrobromide (Nivalin) pharmacokinetics was carried out on male Wistar rats following single intravenous and oral administration. Plasma samples were collected after decapitation of the animals. The drug concentrations were determined spectrophotofluorometrically. A two-compartment open model was found to describe best the experimental data. Galanthamine has an elimination half-life of 40-50 min, a volume of distribution over 2 liters/kg, a plasma clearance of about 2 liters/h X kg and an oral bioavailability of about 65%.
The effect of Galanthamine hydrobromide on plasma ACTH in patients undergoing anaesthesia and surgery
Acta Anaesthesiol Scand 1980 Jun;24(3):166-8.PMID:6255718DOI:10.1111/j.1399-6576.1980.tb01527.x.
The effects of two anticholinesterases, galanthamine and neostigmine, on ACTH and, in some cases, cortisol were compared in 16 patients undergoing relaxant anaesthesia and surgery for varicose veins. The procedures produced increases both in ACTH and cortisol. Following administration of the study drugs to reverse the non-depolarising neuromuscular block, a statistically significant elevation of ACTH occurred in those patients who received galanthamine. It was concluded, therefore, that the rise in plasma cortisol is ACTH-dependent and not due to a peripheral cholinergic mechanism.