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Pergolide is a long-acting dopamine agonist that is uncommonly used for the management of Parkinson's disease, due to the risk for cardiac valvulopathy.
Pergolide is a long-acting dopamine agonist that is uncommonly used for the management of Parkinson's disease, due to the risk for cardiac valvulopathy.
The dopamine D receptor is a 7-transmembrane G-protein coupled receptor associated with G proteins. In lactotrophs, stimulation of dopamine D receptor causes inhibition of adenylyl cyclase, which decreases intracellular cAMP concentrations and blocks IP3-dependent release of Ca from intracellular stores. Decreases in intracellular calcium levels may also be brought about via inhibition of calcium influx through voltage-gated calcium channels, rather than via inhibition of adenylyl cyclase. Additionally, receptor activation blocks phosphorylation of p42/p44 MAPK and decreases MAPK/ERK kinase phosphorylation. Inhibition of MAPK appears to be mediated by c-Raf and B-Raf-dependent inhibition of MAPK/ERK kinase. Dopamine-stimulated growth hormone release from the pituitary gland is mediated by a decrease in intracellular calcium influx through voltage-gated calcium channels rather than via adenylyl cyclase inhibition. Stimulation of dopamine D receptors in the nigrostriatal pathway leads to improvements in coordinated muscle activity in those with movement disorders.
Indicated as adjunctive treatment to levodopa/carbidopa in the management of the signs and symptoms of Parkinson's disease. It was withdrawn from the US and Canadian markets in 2007 due to an increased risk of cardiac valvulopathy.
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One entry per invention. Patent families filed in the US, EP, WO and CN offices.
