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The aim of the present study was to characterize functional responses to ropinirole, its major metabolites in man SKF 4- 3H indolone, SKF 4-carboxy 3H indolone and other dopamine receptor agonists at human dopamine D 2 long hD 2, D 3 hD 3 and D 4. All the receptor agonists tested ropinirole, SKF, SKF, bromocriptine, lisuride, pergolide, pramipexole, talipexole, dopamine increased extracellular acidification rate in Chinese hamster ovary clones expressing the human D 2, D 3 or D 4 receptor. Ropinirole is therefore at least 10 fold selective for the human dopamine D 3 receptor over the other D 2 receptor family members. At the hD 2 and hD 3 dopamine receptors all the compounds tested were full agonists as compared to quinpirole. Talipexole and the ropinirole metabolite, SKF, were partial agonists at the hD 4 receptor. Bromocriptine and lisuride had a slow onset of agonist action which precluded determination of EC 50 s.
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Ropinirole is used alone or with other medications to treat the symptoms of Parkinson's disease PD; a disorder of the nervous system that causes difficulties with movement, muscle control, and balance, including shaking of parts of the body, stiffness, slowed movements, and problems with balance. Ropinirole is also used to treat restless legs syndrome RLS or Ekbom syndrome; a condition that causes discomfort in the legs and a strong urge to move the legs, especially at night and when sitting or lying down.
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