Pergolide | CAS#66104-22-1 | MedKoo Biosciences

MedKoo Cat#: 315247 | Name: Pergolide

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Pergolide (Permax, Pergotoliderived) is an ergoline-based dopamine receptor agonist used in some countries for the treatment of Parkinson's disease. Parkinson's disease is associated with low levels of the neurotransmitter dopamine in the brain. Pergolide has some of the same effects as dopamine in the body. In 2007, pergolide was withdrawn from the U.S. market after several published studies revealed a link between the drug and increased rates of valvular dysfunction. (Source: http://en.wikipedia.org/wiki/Pergolide )

Chemical Structure

Pergolide

CAS#66104-22-1

Theoretical Analysis

MedKoo Cat#: 315247

Name: Pergolide

CAS#: 66104-22-1

Chemical Formula: C19H26N2S

Exact Mass: 314.1817

Molecular Weight: 314.49

Elemental Analysis: C, 72.56; H, 8.33; N, 8.91; S, 10.19

Price and Availability

Size	Price	Availability
50mg	USD 350.00	2 Weeks
100mg	USD 650.00	2 Weeks
200mg	USD 950.00	2 Weeks

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Related CAS #

423748-02-1 (mesylate salt) 66104-22-1 (free base)

Synonym

Pergolide; LY141B; LY-141B; LY 141B

IUPAC/Chemical Name

9-((methylthio)methyl)-7-propyl-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline

InChi Key

YEHCICAEULNIGD-UHFFFAOYSA-N

InChi Code

InChI=1S/C19H26N2S/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/h4-6,10,13,16,18,20H,3,7-9,11-12H2,1-2H3

SMILES Code

CCCN1CC(CSC)CC2C3=CC=CC4=C3C(CC12)=CN4

Appearance

Solid powder

Purity

>97% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO.

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Permax (Pergolide Mesylate) is an ergot derivative dopamine receptor agonist at both D1 and D2 receptor sites. Pergolide mesylate is chemically designated as 8B-[(Methylthio)methyl]-6-propylergoline monomethanesulfonate. The formula weight of the base is 314.5; 1 mg of base corresponds to 3.18 Âµmol. Permax is provided for oral administration in tablets containing 0.05 mg (0.159 Âµmol), 0.25 mg (0.795 Âµmol), or 1 mg (3.18 Âµmol) pergolide as the base. The tablets also contain croscarmel lose sodium, iron oxide, lactose, magnesium stearate, and povidone. The 0.05-mg tablet also contains methionine, and the 0.25mg tablet also contains FD&C Blue No.2. Pharmacodynamic Information: Pergolide mesylate is a potent dopamine receptor agonist. Pergolide is 10 to 1,000 times more potent than bromocriptine on a milligram per milligram basis in various in vitro and in vivo test systems. Pergolide mesylate inhibits the secretion of prolactin in humans; it causes a transient rise in serum concentrations of growth hormone and a decrease in serum concentrations of luteinizing hormone. In ParkinsonÂ†s disease, pergolide mesylate is believed to exert its therapeutic effect by directly stimulating postsynaptic dopamine receptors in the nigrostriatal system. Pharmacokinetic Information (Absorption, Distribution, Metabolism, and Elimination): Information on oral systemic bioavailability of pergolide mesylate is unavailable because of the lack of a sufficiently sensitive assay to detect the drug after the administration of a single dose. However, following oral administration of 14C radiolabeled pergolide mesylate, approximately 55% of the administered radioactivity can be recovered from the urine and 5% from expired CO2, suggesting that a significant fraction is absorbed. Nothing can be concluded about the extent of presystemic clearance, if any. At least 10 metabolites have been detected, including N-despropyl-pergolide, pergolide sulfoxide, and pergolide sulfone. Perolide sulfoxide and pergolide sulfone are dopamine agonists in animals. The other detected metabolites have not been identified and it is not known whether any other metabolites are active pharmacologically. The major route of excretion is the kidney. Pergolide is approximately 90% bound to plasma proteins. This extent of protein binding may be important to consider when pergolide mesylate is coadministered with other drugs known to affect protein binding.

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#T20C12I04

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

Pergolide (LY127809 (free base)) is an ergot-derived orally active dopamine receptor agonist.

In vitro activity:

This study examined levels of several neurotrophic factors associated with cornea nerve regeneration, including NGF, glial cell-derived neurotrophic factor, brain-derived neurotrophic factor, and vascular endothelial growth factor. RT-PCR demonstrated that only NGF was upregulated after the cornea was wounded. Further, upon treatment with liposomes loaded with pergolide, gene expression of NGF was significantly higher than in the vehicle control group (Fig. 2A). This was further confirmed by protein expression of NGF after treatment with different concentrations of pergolide as a clear aqueous solution with the Marinosolv formulation (10, 50, and 300 µg/ml) (Fig. 2B). Protein expression of NGF increased with pergolide treatment in a dose-dependent manner. Both liposomes and Marinosolv were effective as a vehicle for pergolide. Reference: Invest Ophthalmol Vis Sci. 2020 Jan 23;61(1):4. https://pubmed.ncbi.nlm.nih.gov/31999819/

In vivo activity:

In this way, the aim of the present study was to examine the effects of low-dose pergolide on memory deficits and brain oxidative stress in a 6-OHDA (6-hydroxydopamine)-induced rat model of PD (Parkinson’s disease). A reduced number of working/reference memory errors was observed in 6-OHDA + pergolide group, compared to sham-operated rats. Additionally, post hoc analysis showed significant differences between 6-OHDA and 6-OHDA + pergolide groups in both Y-maze and radial-arm-maze tasks. This study also noted a significant decrease of MDA level in the 6-OHDA + pergolide group, compared to sham-operated rats. Significant correlations were also found between behavioral parameters and MDA levels. These data suggest that pergolide facilitates spatial memory and improves brain oxidative balance, after a 6-OHDA-induced model of PD. Reference: J Physiol Biochem. 2012 Mar;68(1):59-69. https://pubmed.ncbi.nlm.nih.gov/22006204/

Preparing Stock Solutions

The following data is based on the product molecular weight 314.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Zhang X, Muddana S, Kumar SR, Burton JN, Labroo P, Shea J, Stocking P, Siegl C, Archer B, Agarwal J, Ambati BK. Topical Pergolide Enhance Corneal Nerve Regrowth Following Induced Corneal Abrasion. Invest Ophthalmol Vis Sci. 2020 Jan 23;61(1):4. doi: 10.1167/iovs.61.1.4. PMID: 31999819; PMCID: PMC7205105. 2. Jeong I, Choi BH, Hahn SJ. Pergolide block of the cloned Kv1.5 potassium channels. Naunyn Schmiedebergs Arch Pharmacol. 2013 Feb;386(2):125-33. doi: 10.1007/s00210-012-0776-5. Epub 2012 Jul 5. PMID: 22763615. 3. Ciobica A, Olteanu Z, Padurariu M, Hritcu L. 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. doi: 10.1007/s13105-011-0119-x. Epub 2011 Oct 18. PMID: 22006204. 4. Ono S, Hirai K, Tokuda E. Effects of pergolide mesilate on metallothionein mRNAs expression in a mouse model for Parkinson disease. Biol Pharm Bull. 2009 Oct;32(10):1813-7. doi: 10.1248/bpb.32.1813. PMID: 19801850.

In vitro protocol:

In vivo protocol:

1. Ciobica A, Olteanu Z, Padurariu M, Hritcu L. 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. doi: 10.1007/s13105-011-0119-x. Epub 2011 Oct 18. PMID: 22006204. 2. Ono S, Hirai K, Tokuda E. Effects of pergolide mesilate on metallothionein mRNAs expression in a mouse model for Parkinson disease. Biol Pharm Bull. 2009 Oct;32(10):1813-7. doi: 10.1248/bpb.32.1813. PMID: 19801850.

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PMID: 38396558; PMCID: PMC10885905. 5: Rouaud A, Calder AE, Hasler G. Microdosing psychedelics and the risk of cardiac fibrosis and valvulopathy: Comparison to known cardiotoxins. J Psychopharmacol. 2024 Mar;38(3):217-224. doi: 10.1177/02698811231225609. Epub 2024 Jan 12. PMID: 38214279; PMCID: PMC10944580. 6: Drozdzewska K, Winter J, Barton AK, Merle R, Gehlen H. Influence of feeding and other factors on adrenocorticotropin concentration and thyrotropin-releasing hormone stimulation test in horses and ponies. Equine Vet J. 2024 Mar;56(2):342-351. doi: 10.1111/evj.14030. Epub 2023 Nov 27. PMID: 38010866. 7: Blau N, Pearson TS, Kurian MA, Elsea SH. Aromatic L-Amino Acid Decarboxylase Deficiency. 2023 Oct 12. In: Adam MP, Feldman J, Mirzaa GM, Pagon RA, Wallace SE, Bean LJH, Gripp KW, Amemiya A, editors. GeneReviews® [Internet]. Seattle (WA): University of Washington, Seattle; 1993–2024. 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PMID: 37385577. 11: Ralta A, Prakash A, Kumar M P, Kumar R, Sarma P, Bhatia A, Medhi B, Chakrabarti A. Neuroprotective Effect of Celastrus Paniculatus Seed Extract on Epilepsy and Epilepsy-associated Cognitive Deficits. Basic Clin Neurosci. 2023 Jan-Feb;14(1):155-166. doi: 10.32598/bcn.2021.3154.1. Epub 2023 Jan 1. PMID: 37346867; PMCID: PMC10279989. 12: Aoyagi H, Tsujinaga S, Takahashi Y, Naito S, Sato T, Otsuka T, Tamaki Y, Motoi K, Ishizaka S, Chiba Y, Kamiya K, Iwano H, Nagai T, Wakasa S, Anzai T. Multimodal Imaging of Constrictive Pericarditis Induced by Long-term Pergolide Treatment for Parkinson's Disease. Intern Med. 2023 Dec 15;62(24):3637-3641. doi: 10.2169/internalmedicine.1381-22. Epub 2023 Mar 31. PMID: 37005266; PMCID: PMC10781551. 13: Tng EL, Teo AE, Aung AT. Macroprolactinoma with secondary resistance to dopamine agonists: a case report and review of the literature. J Med Case Rep. 2023 Mar 17;17(1):96. doi: 10.1186/s13256-023-03820-5. 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