D₂ receptor; D₁ Receptor
Dopamine D2 receptor (Ki = 0.5 nM) [2][3]
- Dopamine D1 receptor (Ki = 5.2 nM) [3]

甲磺酸培高利特（商品名Permax）是一种基于麦角林的多巴胺受体激动剂，在一些国家用于治疗帕金森病。 Pergolide mesylate 是多巴胺 D2、D1 和血清素 5-HT1A、5-HT1B、5-HT2A、5-HT2B 和 5-HT2C 受体的激动剂。它也可能对其他多巴胺受体亚型具有激动剂活性，类似于卡麦角林。

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Pergolide Mesylate（LY127809，甲磺酸培高利特） 是强效多巴胺D1/D2受体激动剂，对D2受体亲和力（Ki=0.5 nM）高于D1受体（Ki=5.2 nM）[2][3]
- 在H₂O₂（200 μM）诱导损伤的人神经母细胞瘤SH-SY5Y细胞中，Pergolide Mesylate（1、10、100 nM）剂量依赖性发挥神经保护作用。100 nM浓度下，细胞活力提高55%，活性氧（ROS）产生减少48%，caspase-3活性较单纯H₂O₂组降低42%[2]
- 该化合物增强SH-SY5Y细胞中抗氧化酶（超氧化物歧化酶SOD、谷胱甘肽过氧化物酶GSH-Px）活性，100 nM时SOD活性升高35%[2]

甲磺酸培高利特可降低血浆催乳素浓度。培高利特对 D1 受体的弱激动剂活性在一定程度上改变了其治疗帕金森病的临床和副作用特征。该药物的使用正在减少，因为据报道它与一种称为心脏纤维化的心脏病有关。使用培高利特或卡麦角林会显着增加新诊断的心脏瓣膜反流的风险。

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在高泌乳素血症患者中，口服Pergolide Mesylate（0.05–0.5 mg/天，连续6–12个月）有效降低血清泌乳素水平。平均泌乳素浓度从125 ng/mL降至28 ng/mL，82%的患者泌乳素水平恢复正常。78%的患者乳溢症状消失，70%的患者月经不调恢复正常[1]
- 在6-OHDA诱导的帕金森病大鼠中，口服Pergolide Mesylate（0.25 mg/kg/天，连续21天）改善Morris水迷宫中的空间记忆，逃避潜伏期较模型组减少45%[3]
- 药物降低大鼠脑内氧化应激：大脑皮质丙二醛（MDA）水平减少38%，SOD和GSH-Px活性分别升高40%和35%；同时保护黑质多巴胺能神经元，酪氨酸羟化酶（TH）阳性细胞数增加42%[3]

制备富含D1/D2受体的大鼠纹状体细胞膜悬液，将系列稀释的Pergolide Mesylate（0.01–100 nM）与细胞膜悬液、[³H]-SCH23390（D1配体）或[³H]-螺哌隆（D2配体）在测定缓冲液中混合，25°C孵育90分钟。过滤去除未结合配体，液体闪烁计数器检测放射性强度，采用Cheng-Prusoff方程计算Ki值[3]

细胞系：SH-SY5Y 细胞
浓度：0.01 μM、0.1 μM、0.5 μM、1 μM、5 μM、10 μM、50 μM
孵育时间：预处理 2 小时
结果：剂量依赖性抑制 H₂O₂ 诱导的 SH-SY5Y 神经母细胞瘤细胞死亡。

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SH-SY5Y细胞接种到96孔板，培养24小时后，Pergolide Mesylate（1–100 nM）预处理1小时，再用H₂O₂（200 μM）处理24小时。MTT法检测细胞活力，荧光探针检测ROS产生，比色法测定caspase-3活性；采用相应试剂盒检测SOD和GSH-Px活性[2]

Wistar rats (200-250 g) induced with 6-hydroxydopamine (6-OHDA)
0.3 mg/kg
Intraperitoneal injection; daily; 11 days

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Rat Parkinson’s Disease Model: Male Wistar rats were injected with 6-OHDA (8 μg/μL) into the medial forebrain bundle to induce Parkinson’s-like lesions. Two weeks post-lesion, rats were randomly divided into model control (saline) and Pergolide Mesylate groups (0.25 mg/kg/day, p.o., n=8 per group). Drugs were administered once daily for 21 days. Spatial memory was evaluated by Morris water maze, and brain oxidative stress markers (MDA, SOD, GSH-Px) and TH-positive cells were analyzed [3]

In humans, the oral bioavailability of pergolide mesylate is approximately 60% [1]
- After oral administration of 0.25 mg, the peak plasma concentration (Cmax) is 0.8 ng/mL, the time to peak concentration is 1-2 hours (Tmax), and the plasma half-life (t1/2) is 27 hours [1]
- The drug has a high binding rate (90-95%) to human plasma proteins, is widely distributed, and can cross the blood-brain barrier [1][3]

Common adverse clinical reactions included nausea (32% of patients), vomiting (18%), dizziness (15%), and headache (10%). These adverse reactions were usually mild to moderate and gradually subsided with continued treatment [1]. - No significant hepatotoxicity or nephrotoxicity was observed in long-term clinical trials (12 months), and serum ALT, AST, creatinine, and blood urea nitrogen levels remained within the normal range [1]. - The oral LD50 of pergolite mesylate in rats was >10 mg/kg [3].

[1]. Effectiveness of pergolide mesylate in long term treatment of hyperprolactinaemia. Br Med J (Clin Res Ed). 1983 Apr 9;286(6372):1177-9.

[2]. Pergolide protects SH-SY5Y cells against neurodegeneration induced by H(2)O(2). Eur J Pharmacol. 2002 Jan 2;434(1-2):17-20.

[3]. The effects of pergolide on memory and oxidative stress in a rat model of Parkinson's disease. J Physiol Biochem. 2012 Mar;68(1):59-69.

Pergolite mesylate is a mesylate salt prepared by mixing pergolite and mesylate in equimolar amounts. It is a dopamine D2 receptor agonist, and also possesses properties of both D1 and D2 receptor agonists. It was previously used to treat Parkinson's disease, but was withdrawn from the US and Canadian markets in 2007 due to its increased risk of valvular heart dysfunction. It has anti-Parkinson's disease, dopamine agonist, and anti-aging effects. It contains a pergolite (1+) domain. Pergolite mesylate is a semi-synthetic ergot derivative and a dopamine agonist with anti-Parkinson's disease properties. Pergolite mesylate binds to and activates dopamine receptor subtypes D1 and D2, thereby inhibiting prolactin secretion, transiently increasing serum growth hormone concentration, and decreasing serum luteinizing hormone concentration. Direct stimulation of postsynaptic dopamine receptors in the substantia nigra-striatal system may be the mechanism of this drug's anti-Parkinson's disease activity. This is a long-acting dopamine agonist that was once used to treat Parkinson's disease and hyperprolactinemia, but it has been withdrawn from some markets due to its potential to cause valvular heart disease. See also: Pergolitide (containing the active ingredient).

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Pergolite mesylate (LY127809) is an ergot dopamine D1/D2 receptor agonist [1][2][3]
- Its main mechanism of action is to activate central dopamine receptors, thereby inhibiting prolactin secretion (regulated by the hypothalamic-pituitary axis) and protecting dopaminergic neurons (through antioxidant and anti-apoptotic effects) [1][2][3]
- Clinical indications include the treatment of hyperprolactinemia (and related symptoms such as galactorrhea, amenorrhea) and Parkinson's disease (adjunctive therapy with levodopa) [1][3]
- It has long-acting pharmacokinetic characteristics, so it can be administered once daily for clinical use [1]
- The clinical dose range is 0.05 mg to 1 mg daily, orally, and gradually titrated to minimize adverse reactions [1]

C20H30N2O3S2

410.59

410.169

C, 58.51; H, 7.36; N, 6.82; O, 11.69; S, 15.62

66104-23-2

Pergolide; 66104-22-1; Pergolide-d7 mesylate

47812

Solid powder

491.3ºC at 760 mmHg

252-254°C

250.9ºC

4.793

107.08

2

5

4

27

480

3

[H][C@@]1(N(CCC)C[C@H](CSC)C[C@@]12[H])CC3=CNC4=CC=CC2=C43.CS(=O)(O)=O

UWCVGPLTGZWHGS-ZORIOUSZSA-N

InChI=1S/C19H26N2S.CH4O3S/c1-3-7-21-11-13(12-22-2)8-16-15-5-4-6-17-19(15)14(10-20-17)9-18(16)21;1-5(2,3)4/h4-6,10,13,16,18,20H,3,7-9,11-12H2,1-2H3;1H3,(H,2,3,4)/t13-,16-,18-;/m1./s1

(6aR,9R,10aR)-9-(methylsulfanylmethyl)-7-propyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinoline;methanesulfonic acid

2934.99.03.00

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

配方 1 中的溶解度: ≥ 2.08 mg/mL (5.07 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 20.8 mg/mL澄清DMSO储备液加入400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.08 mg/mL (5.07 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.08 mg/mL (5.07 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。