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Purity: ≥98%
Pergolide Mesylate (Permax; Pergotoliderived; LY127809; LY-127809), the mesylate salt of Pergolide, is a novel and potent antiparkinsonian agent which acts as a dopaminergic agonist. It is used to treat Parkinson's disease in certain nations. The dopamine D2, D1, and serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors are all agonist-activated by pergolide mesylate. It might also, like cabergoline, have agonist activity at other dopamine receptor subtypes.
| Targets |
D2 receptor; D1 Receptor
Dopamine D2 receptor (Ki = 0.5 nM) [2][3] - Dopamine D1 receptor (Ki = 5.2 nM) [3] |
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| ln Vitro |
In vitro activity: Pergolide treatment dose-dependently blocks H2O2-induced cell death in SH-SY5Y neuroblastoma cells. Pergolide, which acts at very low concentrations (nanomolar range) and in the very early stages of the neurotoxic intracellular process, protects SH-SY5Y neuroblastoma cells from cell death that is specifically induced by H2O2(2).
Pergolide Mesylate (LY127809) acts as a potent agonist of dopamine D1 and D2 receptors, with higher affinity for D2 receptors (Ki=0.5 nM) than D1 receptors (Ki=5.2 nM) [2][3] - In SH-SY5Y human neuroblastoma cells exposed to H₂O₂ (200 μM), Pergolide Mesylate (1, 10, 100 nM) dose-dependently protected against neurodegeneration. At 100 nM, cell viability increased by 55%, reactive oxygen species (ROS) production decreased by 48%, and caspase-3 activity was reduced by 42% compared to the H₂O₂-only group [2] - The compound enhanced the activity of antioxidant enzymes (superoxide dismutase, SOD; glutathione peroxidase, GSH-Px) in SH-SY5Y cells, with SOD activity increased by 35% at 100 nM [2] |
| ln Vivo |
Pergolide (0.3 mg/kg; intraperitoneal injection; daily; 11 days) treatment lowers the amount of working/reference memory errors in a rat model of Parkinson's disease induced by 6-OHDA. Pergolide enhances the oxidative balance of the brain and helps with spatial memory[3].
In patients with hyperprolactinaemia, oral administration of Pergolide Mesylate (0.05–0.5 mg daily for 6–12 months) effectively reduced serum prolactin levels. The mean prolactin concentration decreased from 125 ng/mL to 28 ng/mL, with 82% of patients achieving normal prolactin levels. Galactorrhoea resolved in 78% of cases, and menstrual irregularities normalized in 70% [1] - In 6-OHDA-induced Parkinson’s disease rats, oral Pergolide Mesylate (0.25 mg/kg/day for 21 days) improved spatial memory in the Morris water maze test, reducing escape latency by 45% compared to the model group [3] - The drug reduced oxidative stress in the rat brain: cerebral cortex malondialdehyde (MDA) levels decreased by 38%, while SOD and GSH-Px activities increased by 40% and 35% respectively. It also protected dopaminergic neurons in the substantia nigra, increasing tyrosine hydroxylase (TH)-positive cell count by 42% [3] |
| Enzyme Assay |
Membrane preparations were isolated from rat striatum (enriched in D1/D2 receptors). Serial dilutions of Pergolide Mesylate (0.01–100 nM) were mixed with membrane suspensions and [³H]-SCH23390 (D1 ligand) or [³H]-spiperone (D2 ligand) in assay buffer. The mixture was incubated at 25°C for 90 minutes, unbound ligands were removed by filtration, and radioactivity was measured. Ki values were calculated using the Cheng-Prusoff equation [3]
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| Cell Assay |
Cell Line: SH-SY5Y cells
Concentration: 0.01 μM, 0.1 μM, 0.5 μM, 1 μM, 5 μM, 10 μM, 50 μM Incubation Time: Pretreated for 2 hours Result: Dose-dependently inhibited H2O2-induced cell death in SH-SY5Y neuroblastoma cells. SH-SY5Y cells were seeded in 96-well plates and cultured for 24 hours. Cells were pretreated with Pergolide Mesylate (1–100 nM) for 1 hour, then exposed to H₂O₂ (200 μM) for 24 hours. Cell viability was measured by MTT assay, ROS production was detected using a fluorescent probe, and caspase-3 activity was quantified by colorimetric assay. SOD and GSH-Px activities were measured using respective assay kits [2] |
| Animal Protocol |
Wistar rats (200-250 g) induced with 6-hydroxydopamine (6-OHDA)
0.3 mg/kg Intraperitoneal injection; daily; 11 days 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] |
| ADME/Pharmacokinetics |
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] |
| Toxicity/Toxicokinetics |
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].
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| References |
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| Additional Infomation |
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).
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] |
| Molecular Formula |
C20H30N2O3S2
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| Molecular Weight |
410.59
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| Exact Mass |
410.169
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| Elemental Analysis |
C, 58.51; H, 7.36; N, 6.82; O, 11.69; S, 15.62
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| CAS # |
66104-23-2
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| Related CAS # |
Pergolide; 66104-22-1; Pergolide-d7 mesylate
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| PubChem CID |
47812
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| Appearance |
Solid powder
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| Boiling Point |
491.3ºC at 760 mmHg
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| Melting Point |
252-254°C
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| Flash Point |
250.9ºC
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| LogP |
4.793
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
480
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| Defined Atom Stereocenter Count |
3
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| SMILES |
[H][C@@]1(N(CCC)C[C@H](CSC)C[C@@]12[H])CC3=CNC4=CC=CC2=C43.CS(=O)(O)=O
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| InChi Key |
UWCVGPLTGZWHGS-ZORIOUSZSA-N
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| InChi Code |
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
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| Chemical Name |
(6aR,9R,10aR)-9-(methylsulfanylmethyl)-7-propyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinoline;methanesulfonic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.07 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 | 4.8710 mL | |
| 10 mM | 0.2436 mL | 1.2178 mL | 2.4355 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01066403 | Completed | Drug: Pergolide | Schizophrenia | Heidelberg University | October 2003 | Not Applicable |
| NCT00000248 | Completed | Drug: Pergolide | Cocaine-Related Disorders | Medical University of South Carolina |
February 1996 | Phase 3 |
| NCT00004433 | Completed | Drug: pergolide | Tourette Syndrome | Children's Hospital Medical Center, Cincinnati |
December 1994 | Not Applicable |
| NCT00000215 | Completed | Drug: Pergolide | Cocaine-Related Disorders | National Institute on Drug Abuse (NIDA) |
December 2001 | Phase 2 |
| NCT00000269 | Completed | Drug: Pergolide | Cocaine-Related Disorders Substance-Related Disorders |
National Institute on Drug Abuse (NIDA) |
October 1995 | Phase 2 |
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