Dopamine Receptors: Antiparkinsonian Activity and Molecular Mechanisms
Ergot derivatives such as bromocriptine, lergotrile, pergolide, and mesulergine relieve tremor and elicit abnormal involuntary movements in monkeys with ventromedial tegmental lesions. These ergots are of therapeutic value in patients with advanced Parkinson’s disease, especially in those whose condition is complicated by diurnal oscillations in performance and/or who no longer respond to treatment with levodopa alone. Some nonergot dopamine agonists (e.g., LY 141865, EMD 23–448, AY 27–110) stimulate, at low doses, presynaptic, as well as supersensitive postsynaptic, dopamine receptors. Results obtained from studies in animal models suggest that these compounds might be effective antiparkinsonian agents.
In separate study, we have investigated the properties of solubilized striatal D-2 dopamine receptors. Evidence has been obtained that the D-2 dopamine receptor is a glycoprotein, and that the ganglioside, GM-1, interacts with the lectin, WGA, at a similar site as the dopamine receptor.
KeywordsDopamine Receptor Ergot Alkaloid Sialic Acid Residue Ergot Derivative Diurnal Oscillation
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