Pergolide mesylate salt is a methanesulfonate salt obtained from pergolide by mixing eqimolar amount of pergolide and methanesulfonic acid. A dopamine D2 receptor agonist which also has D1 and D2 agonist properties, it is used in the management of Parkinson's disease and hyperprolactinemia.
CAT No: 10-101-119
CAS No:66104-23-2
Synonyms/Alias:Pergolide Mesilate; LY 127809; (8β)-8-[(Methylthio)methyl]-6-propylergoline monomethanesulfonate; 8-Methylsulfanylmethyl-6-propyl-ergoline methanesulfonate
Pergolide Mesylate Salt is a synthetic ergoline derivative widely recognized for its dopaminergic agonist properties, making it a valuable compound in neuropharmacological research and biochemical studies. Characterized by its potent interaction with dopamine receptors, this salt form of pergolide offers enhanced solubility and stability, facilitating its integration into various experimental protocols. Researchers frequently select Pergolide Mesylate Salt for its well-documented receptor specificity and ability to modulate neurotransmitter pathways, which supports a range of investigative pursuits in both in vitro and in vivo systems. Its chemical profile allows for reliable and reproducible results, making it a preferred choice for laboratories focused on the mechanisms of neurodegeneration, neurotransmitter regulation, and receptor pharmacology.
Neuroscience Research: In the field of neuroscience, Pergolide Mesylate Salt serves as a critical tool for elucidating the functional roles of dopamine receptors, particularly the D1 and D2 subtypes. Researchers use this compound to probe dopaminergic signaling pathways, assess receptor-ligand interactions, and model the effects of dopamine agonism in cellular and animal models. Its application extends to studies investigating the pathophysiology of movement disorders, where the compound helps delineate the consequences of altered dopamine transmission on motor function and neuronal circuitry. By selectively activating dopaminergic pathways, it enables the dissection of complex neurobiological processes underlying both normal and pathological states.
Receptor Binding Assays: Pergolide, in its mesylate salt form, is frequently employed in receptor binding assays to quantify the affinity and selectivity of dopaminergic ligands. Its high receptor specificity makes it an ideal reference compound in competitive binding experiments, where it helps define the pharmacological profile of novel drug candidates. These assays are instrumental in characterizing the interaction dynamics between potential therapeutics and dopamine receptors, thus advancing the rational design of new neuroactive agents. The compound's consistent performance in these assays underpins its widespread adoption in pharmacological research.
Behavioral Pharmacology: In behavioral pharmacology, Pergolide Mesylate Salt is utilized to investigate the influence of dopaminergic modulation on animal behavior. Experimental paradigms often involve administering the compound to model reward-related behaviors, assess locomotor activity, or explore the neurochemical basis of motivation and reinforcement. Its capacity to mimic endogenous dopamine activity allows researchers to simulate and manipulate dopaminergic states, providing insights into the neural substrates of behavior. Such studies contribute to a deeper understanding of the neurochemical mechanisms underlying psychiatric and neurodegenerative conditions.
Endocrine Studies: The dopaminergic properties of Pergolide Mesylate Salt also render it valuable in endocrine research, particularly for examining the regulation of hormone secretion. By acting on dopamine receptors in the pituitary gland, the compound is used to modulate the release of prolactin and other pituitary hormones in experimental models. This application aids in unraveling the complex feedback mechanisms that govern endocrine function and supports the development of new approaches for investigating hypothalamic-pituitary axis dynamics. Its role in these studies underscores the versatility of dopaminergic agents in diverse biological contexts.
Signal Transduction Pathway Analysis: Scientists leverage Pergolide Mesylate Salt to study intracellular signaling cascades triggered by dopamine receptor activation. By applying the compound to cultured cells or tissue preparations, researchers can monitor downstream effects such as changes in cyclic AMP levels, protein phosphorylation, and gene expression profiles. These analyses provide mechanistic insights into how dopamine agonists modulate cellular responses, offering a foundation for understanding the molecular basis of dopaminergic signaling. The ability to precisely manipulate these pathways with Pergolide Mesylate Salt makes it an indispensable reagent for dissecting the complexities of cell signaling in neurobiology and beyond.
Pergolide mesylate (proprietary name Permax) is used to treat equine Cushing's syndrome. Since pergolide mesylate has been removed from the market, the tablets are no longer available. Therefore, pergolide mesylate preparations have to be compounded for veterinary use. Compounded oral liquid formulations have been given arbitrary beyond-use dates of 14 days (aqueous) to 90 days (oil based). The goal of this study was to determine the stability of a 0.2 mg/mL pergolide oral liquid prepared according to a previousy published formulation and stored at room temperature. The sample preparation and the high-performance liquid chromatographic assay described in the United States Pharmacopeia-National Formulary were modified to treat the oral liquid as a suspension. The assay was evaluated prior to its use. A linear relationship was found between peak area and concentration with Rsquared values ranging for 0.989 to 0.999 for three of the sample calibration plots. The daily reproducibility and day-to-day variability of single injections of the assay were found to have relative standard deviations of 1.26% and 3.52%, respectively. Analysis of the oral liquid and a blank oral liquid (without pergolide mesylate) exposed to acid and heat demonstrated that the excipients and degradation species did not interfere with the drug peak. Samples, in replicates of five, were stored at room temperature, then pulled at specific intervals (1, 2, 4, 8, 12, and 16 weeks) and stored at -80 deg C for assay at a later date. After 16 weeks at room temperature, the drug degraded to 71% of its original concentration. The time to reach 90% potency (t90) of pergolide mesylate was calculated to be 6.5 weeks (45 days). Degradation studies at 35 deg C, 45 deg C, and 60 deg C are in progress.
Shank, B. R., & Ofner III, C. M. (2009). Stability of Pergolide Mesylate Oral Liquid at Room Temperature. International journal of pharmaceutical compounding, 13(3), 254.
Results indicated that pergolide mesylate was unstable after compounding in an aqueous vehicle and that storage conditions had an effect on stability of the compounded formulation. Compounded pergolide formulations in aqueous vehicles should be stored in a dark container, protected from light, and refrigerated and should not be used >30 days after produced. Formulations that have undergone a color change should be considered unstable and discarded.
Davis, J. L., Kirk, L. M., Davidson, G. S., & Papich, M. G. (2009). Effects of compounding and storage conditions on stability of pergolide mesylate. Journal of the American Veterinary Medical Association, 234(3), 385-389.
In the past 15 years, clinical data of over 1,500 patients treated with pergolide mesylate have been published. Pergolide is a dopamine agonist with a potent stimulating effect on D2 and also on D1 receptors. This pharmacodynamic characteristic seems the most effective in increasing the motility in Parkinson's disease. Pergolide has been used almost exclusively as an adjunct to levodopa treatment. Its positive effects seems to be related to its long plasma half life, about 27 hours, and 5-6 hours of clinical activity; it has shown to be effective on all parkinsonian symptoms except for the reduction of postural reflexes, it reduces off periods and compared to bromocriptine, it considerably improves the activities of daily living. Adverse reactions are, for the most part, mild and reversible, they mostly include nausea and gastroenteric disturbances.
Pezzoli, G., Canesi, M., Pesenti, A., & Mariani, C. B. (1995). Pergolide mesylate in Parkinson's disease treatment. Journal of neural transmission. Supplementum, 45, 203-212.
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