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 ergot derivative classified as a potent dopamine receptor agonist, widely recognized for its ability to interact with both D1 and D2 dopamine receptor subtypes. As a small-molecule compound, it holds significant importance in neuropharmacological research due to its structural similarity to endogenous neurotransmitters and its well-characterized receptor binding profile. The mesylate salt form enhances its solubility and stability, making it a preferred choice for in vitro and in vivo studies examining dopaminergic pathways. Its ability to modulate neurotransmitter systems has made it a valuable tool in the elucidation of dopaminergic function, receptor pharmacology, and neurochemical signaling processes.
Neuropharmacology research: Pergolide Mesylate Salt is routinely utilized in studies investigating the pharmacodynamics and pharmacokinetics of dopaminergic agents. Its high affinity for dopamine receptors allows researchers to dissect the functional roles of D1 and D2 receptor subtypes in neural signaling. By serving as a reference agonist, it enables the assessment of novel compounds' efficacy and selectivity, supporting the development of new agents targeting the central nervous system. Its use in receptor binding assays and intracellular signaling studies provides critical insights into dopaminergic modulation at the molecular and cellular levels.
Parkinsonism modeling: The compound is frequently employed in preclinical models to simulate dopaminergic stimulation, aiding in the study of Parkinson's disease mechanisms and motor control. By activating dopaminergic receptors, pergolide mesylate can mimic or counteract dopaminergic deficits in animal models, facilitating the exploration of neuronal degeneration, compensatory mechanisms, and synaptic plasticity. This application is vital for understanding disease progression and for evaluating the neuroprotective potential of experimental interventions in a controlled research environment.
Endocrine regulation studies: Owing to its dopaminergic agonist properties, pergolide mesylate is instrumental in research on neuroendocrine regulation, particularly within the hypothalamic-pituitary axis. It is used to modulate prolactin secretion in pituitary cell cultures and animal models, enabling detailed investigations into the feedback mechanisms governing hormone release. Such studies are essential for mapping the neurochemical pathways that control endocrine homeostasis and for identifying molecular targets for further research into hormone-related disorders.
Behavioral neuroscience: Researchers utilize pergolide mesylate to probe the behavioral consequences of altered dopaminergic activity, including locomotor function, reward processing, and cognitive performance. Its administration in animal models helps delineate the contribution of dopamine signaling to complex behaviors and neuropsychiatric phenomena. By systematically varying dose and administration protocols, investigators can assess the compound's impact on behavior, supporting the development of experimental paradigms for neurobehavioral analysis.
Drug interaction and toxicity assessment: Pergolide mesylate serves as a benchmark compound in the evaluation of drug-drug interactions and toxicity profiles within dopaminergic systems. Its well-characterized mechanism of action and predictable pharmacological effects make it suitable for use in screening studies that assess the safety, compatibility, and potential adverse effects of new chemical entities. These investigations are crucial for early-stage compound profiling, risk assessment, and the refinement of pharmacological strategies in neurochemical research.
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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