Cell lines

SH-SY5Y neuroblastoma cell

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10 nM to 50 μM

Applications

Pergolide dose-dependently protected neuroblastoma cells from H2O2-induced neurotoxicity with IC50 values of pergolide of about 40 and 60 nM. Incubation of the cells with 1 μM pergolide for 26 h did not affect cell viability. Preincubation of the cells with 100 nM pergolide for 2 h before the cytotoxic agent did not affect the neurotoxic effect of either doxorubicin or cis-platinum.

Animal models

Female rats

Dosage form

Intraperitoneal injection, 0.5 mg/kg/day, 7 days

Application

In spayed female rats, pergolide mesylate significantly suppressed food intake and body weight. Inhibition of food intake by a constant dose of pergolide progressively diminished with repeated administrations. Pergolide suppressed body weight with no indications of tolerance. In rats treated with pergolide mesylate (7 days 0.5 mg/kg/day, i.p.), the average amount of 2,3-DHBA associated with 6-OHDA striatal infusion was significantly smaller than that in controls. Pergolide treatment led to an increased ability of striatal tissue to quench hydroxyl radical formation in vivo.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

Pergolide mesylate is an antiparkinsonian agent which functions as a dopaminergic agonist.Target: Dopamine ReceptorPergolide 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 [1, 2]. Pergolide mesylate decreases plasma prolactin concentrations [3]. 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 [4].

References:
[1]. Lemberger, L. and R.E. Crabtree, Pharmacologic effects in man of a potent, long-acting dopamine receptor agonist. Science, 1979. 205(4411): p. 1151-3.
[2]. Koller, W.C., et al., The pharmacological evaluation of pergolide mesylate as a potential anti-parkinson agent. Neuropharmacology, 1980. 19(9): p. 831-7.
[3]. Franks, S., et al., Effectiveness of pergolide mesylate in long term treatment of hyperprolactinaemia. British medical journal (Clinical research ed.), 1983. 286(6372): p. 1177.
[4]. Schade, R., et al., Dopamine agonists and the risk of cardiac-valve regurgitation. N Engl J Med, 2007. 356(1): p. 29-38.