Journal
JOURNAL OF NEURAL TRANSMISSION
Volume 110, Issue 10, Pages 1119-1127Publisher
SPRINGER WIEN
DOI: 10.1007/s00702-003-0027-5
Keywords
dopamine receptor agonists; dopamine D-1-agonist; dopamine D(2)agonist; dopamine D-3-agonist; Parkinson therapy; dopamine receptors; receptor binding
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The aim of this study was to compare dopamine receptor binding affinities of all currently approved dopamine receptor agonist treatments for Parkinson's disease (PD) in human brain tissue. alpha-Dihydroergoeryptine and lisuride displayed higher comparative affinities (K-i = 35.4 and 56.7 nM, respectively) for D-1 receptors, than the D-1/D-2 dopamine agonist pergolide (Ki = 447 nM). The second generation non-ergot dopamine receptors agonists pramipexole and ropinirole demonstrated no affinity for D, receptors at concentrations up to 10(-4) M. The ergoline dopamine agonists cabergoline and lisuride displayed the highest affinities for the D-2 receptor (K-i = 0.61 and 0.95 nM, respectively). Surprisingly, the second generation non-ergot doparnine receptors agonists pramipexole and ropinirole only weakly inhibited binding to D2 receptors (K-i = 79.5 and 98.7 muM, respectively using [H-3]raclopride). Interestingly we also found that the affinities of cabergoline (K-i = 1.27 nM), lisuride (K-i = 1.08 nM) and pergolide (K-i = 0.86 nM) for the D-3 receptor subtype were comparable to that of pramipexole (K-i = 0.97 nM). The present results thus support the hypothesis that the antiparkinsonian effect of dopamine receptor agonists is mediated by a more complex interactions with dopamine receptor subtypes than currently believed.
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