Dopamine receptor agonists in current clinical use: comparative dopamine receptor binding profiles defined in the human striatum.
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Gerlach M, Double K, Arzberger T, Leblhuber F, Tatschner T, Riederer P
Dopamine receptor agonists in current clinical use: comparative dopamine receptor binding profiles defined in the human striatum.
J Neural Transm (Vienna). 2003 Oct;110(10):1119-27. doi: 10.1007/s00702-003-0027-5.
- PubMed ID
- 14523624 [ View in PubMed]
- Abstract
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-dihydroergocryptine and lisuride displayed higher comparative affinities (Ki=35.4 and 56.7 nM, respectively) for D1 receptors, than the D1/D2 dopamine agonist pergolide (Ki=447 nM). The second generation non-ergot dopamine receptors agonists pramipexole and ropinirole demonstrated no affinity for D1 receptors at concentrations up to 10(-4) M. The ergoline dopamine agonists cabergoline and lisuride displayed the highest affinities for the D2 receptor (Ki=0.61 and 0.95 nM, respectively). Surprisingly, the second generation non-ergot dopamine receptors agonists pramipexole and ropinirole only weakly inhibited binding to D2 receptors (Ki=79.5 and 98.7 microM, respectively using [3H]spiperone). Interestingly we also found that the affinities of cabergoline (Ki=1.27 nM), lisuride (Ki=1.08 nM) and pergolide (Ki=0.86 nM) for the D3 receptor subtype were comparable to that of pramipexole (Ki=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.
DrugBank Data that Cites this Article
- Drugs
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Dihydro-alpha-ergocryptine D(1) dopamine receptor (Protein Group) Protein group Humans YesPartial agonistDetails Dihydro-alpha-ergocryptine Dopamine D2 receptor Protein Humans YesAgonistDetails Dihydro-alpha-ergocryptine Dopamine D3 receptor Protein Humans YesPartial agonistDetails