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Pergolide Mesylate 66104-23-2

Product Description

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Pergolide mesylate (trade name Permax) is an ergoline-based dopamine
receptor agonist used in some countries for the treatment of Parkinson's
disease. Pergolide mesylate functions as an agonist at the dopamine D2,
D1 and serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors. It may possess agonist activity at other dopamine receptor subtypes as well, similar to cabergoline.




Pergolide mesylate decreases plasma prolactin concentrations. The weak agonist activity of pergolide at D1 receptors somewhat alters
its clinical and side effect profile in the treatment of Parkinson's
disease. The drug is in decreasing use, as it is reported to be
associated with a form of heart disease called cardiac fibrosis. The
use of pergolide or cabergoline is associated with a significantly
increased risk of newly diagnosed cardiac-valve regurgitation.





Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species Baboon Dog Monkey Rabbit Guinea pig Rat Hamster Mouse
Weight (kg) 12 10 3 1.8 0.4 0.15 0.08 0.02
Body Surface Area (m2) 0.6 0.5 0.24 0.15 0.05 0.025 0.02 0.007
Km factor 20 20 12 12 8 6 5 3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by Animal B Km
Animal A Km



For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × mouse Km(3) = 11.2 mg/kg
rat Km(6)







Chemical Information




Molecular Weight (MW) 410.59
Formula

C19H26N2S.CH4O3S

CAS No. 66104-23-2

Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms LY127809



Solubility (25°C) * In vitro DMSO 10 mg/mL (24.35 mM)
Water 82 mg/mL (199.71 mM)
Ethanol <1 mg/mL (
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.




Chemical Name Ergoline, 8-[(methylthio)methyl]-6-propyl-, (8β)-, monomethanesulfonate (9CI)







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