Pergolide mesylate
(Synonyms: 甲磺酸培高利特; Pergolide methanesulfonate; LY127809) 目录号 : GC16615
A dopamine D1 and D2 receptor agonist
Cas No.:66104-23-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
SH-SY5Y neuroblastoma cell |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
10 nM to 50 μM |
|
Applications |
Pergolide dose-dependently protected neuroblastoma cells from H2O2-induced neurotoxicity with IC50 values of pergolide of about 40 and 60 nM. Incubation of the cells with 1 μM pergolide for 26 h did not affect cell viability. Preincubation of the cells with 100 nM pergolide for 2 h before the cytotoxic agent did not affect the neurotoxic effect of either doxorubicin or cis-platinum. |
| Animal experiment [2,3]: | |
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Animal models |
Female rats |
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Dosage form |
Intraperitoneal injection, 0.5 mg/kg/day, 7 days |
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Application |
In spayed female rats, pergolide mesylate significantly suppressed food intake and body weight. Inhibition of food intake by a constant dose of pergolide progressively diminished with repeated administrations. Pergolide suppressed body weight with no indications of tolerance. In rats treated with pergolide mesylate (7 days 0.5 mg/kg/day, i.p.), the average amount of 2,3-DHBA associated with 6-OHDA striatal infusion was significantly smaller than that in controls. Pergolide treatment led to an increased ability of striatal tissue to quench hydroxyl radical formation in vivo. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Uberti D, Piccioni L, Colzi A, et al. Pergolide protects SH-SY5Y cells against neurodegeneration induced by H 2 O 2[J]. European journal of pharmacology, 2002, 434(1): 17-20. [2]. Greene S B, Mathews D, Hollingsworth E M, et al. Behavioral effects of pergolide mesylate on food intake and body weight[J]. Pharmacology Biochemistry and Behavior, 1985, 23(2): 161-167. [3]. Opacka-Juffry J, Wilson A W, Blunt S B. Effects of pergolide treatment on in vivo hydroxyl free radical formation during infusion of 6-hydroxydopamine in rat striatum[J]. Brain research, 1998, 810(1): 27-33. | |
Pergolide mesylate is an antiparkinsonian agent which functions as a dopaminergic agonist.Target: Dopamine ReceptorPergolide mesylate (trade name Permax) is an ergoline-based dopamine receptor agonist used in some countries for the treatment of Parkinson's disease. Pergolide mesylate functions as an agonist at the dopamine D2, D1 and serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors. It may possess agonist activity at other dopamine receptor subtypes as well, similar to cabergoline [1, 2]. Pergolide mesylate decreases plasma prolactin concentrations [3]. The weak agonist activity of pergolide at D1 receptors somewhat alters its clinical and side effect profile in the treatment of Parkinson's disease. The drug is in decreasing use, as it is reported to be associated with a form of heart disease called cardiac fibrosis. The use of pergolide or cabergoline is associated with a significantly increased risk of newly diagnosed cardiac-valve regurgitation [4].
References:
[1]. Lemberger, L. and R.E. Crabtree, Pharmacologic effects in man of a potent, long-acting dopamine receptor agonist. Science, 1979. 205(4411): p. 1151-3.
[2]. Koller, W.C., et al., The pharmacological evaluation of pergolide mesylate as a potential anti-parkinson agent. Neuropharmacology, 1980. 19(9): p. 831-7.
[3]. Franks, S., et al., Effectiveness of pergolide mesylate in long term treatment of hyperprolactinaemia. British medical journal (Clinical research ed.), 1983. 286(6372): p. 1177.
[4]. Schade, R., et al., Dopamine agonists and the risk of cardiac-valve regurgitation. N Engl J Med, 2007. 356(1): p. 29-38.
| Cas No. | 66104-23-2 | SDF | |
| 别名 | 甲磺酸培高利特; Pergolide methanesulfonate; LY127809 | ||
| 化学名 | (6aR,9R,10aR)-9-(methylsulfanylmethyl)-7-propyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinoline;methanesulfonic acid | ||
| Canonical SMILES | CCCN1CC(CC2C1CC3=CNC4=CC=CC2=C34)CSC.CS(=O)(=O)O | ||
| 分子式 | C19H26N2S.CH4O3S | 分子量 | 410.59 |
| 溶解度 | ≥ 6.8mg/mL in DMSO | 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 | 2.4355 mL | 12.1776 mL | 24.3552 mL |
| 5 mM | 0.4871 mL | 2.4355 mL | 4.871 mL |
| 10 mM | 0.2436 mL | 1.2178 mL | 2.4355 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。