Rotigotine is a potent agonist at dopamine D1 receptors as well as at dopamine D2 and D3 receptors

摘要: Background and Purpose Rotigotine acts as a dopamine receptor agonist with high affinity for the D2, D3, D4 D5 receptors but low D1 receptor. We have investigated this further in radioligand binding functional studies compared profile of rotigotine that other drugs used treatment Parkinson's disease (PD). Experimental Approach The to human D1, was determined using [3H]rotigotine standard antagonist radioligands. Functional interactions also determined. Key Results [3H]rotigotine can be an label all subtypes important derive estimates. Rotigotine maintains at especially D2 D3 and, lesser extent, receptors. Rotigotine, like apomorphine unlike ropinirole pramipexole, potent receptors. Conclusions Implications Rotigotine is high-potency lower potency These differentiate from conventional agonists, PD, such pramipexole which lack activity receptors, resembles has greater efficacy PD than agonists suboptimal pharmacokinetic properties.