Dihydropteridine reductase from human liver and rat striatal synaptosomes is noncompetitively inhibited by apomorphine and its analogs. The Ki or I50 values are in the range of 0.6 to 2.9 microM for R-(-)-apomorphine, R-(-)-and S-(+)-2, 10, 11-trihydroxyaporphine, R-(-)-norapomorphine, R-(-)-N-hydroxyethylnorapomorphine, R-(-)-2,10,11-trihydroxy-N-n-propylnoraporphine, R-(-)- and S-(+)-N-n-prop...

BACKGROUND Dopaminergic and opioidergic drugs have been found to be effective in patients with restless legs syndrome (RLS). OBJECTIVES To test the effect of apomorphine--a combined opioidergic and dopaminergic agonist--and subsequent selective antagonism by naloxone and metoclopramide on subjective and objective symptoms in patients with idiopathic RLS. METHODS Nine patients with RLS were ...

The metabolism of apomorphine is quite complex due to interactions with proteins and other tissue components that affect its pharmacokinetic profile. The electrochemical oxidation mechanism of apomorphine and of some synthesised apomorphine derivatives was studied. It was found to be related to the reaction of o-diphenol and tertiary amine groups and strongly dependent on pH.

BACKGROUND In patients with motor fluctuations complicating Parkinson's disease (PD), delays in time-to-ON with levodopa are common. This open-label study aimed to assess the effect of apomorphine on time-to-ON in PD patients with morning akinesia. METHODS The safety population included 127 enrolled patients, and the full analysis set (FAS) included 88 patients. Patients completed a 7-day lev...

Artificially roughened gold surfaces with controlled nanostructure produced by pulsed laser deposition have been investigated as sensors for apomorphine detection aiming at clinical application. The use of such gold surfaces has been optimized using aqueous solutions of apomorphine in the concentration range between 3.3 × 10(-4) M and 3.3 × 10(-7) M. The experimental parameters have been invest...

The MCH and dopamine receptor systems have been shown to modulate a number of behaviors related to reward processing, addiction, and neuropsychiatric conditions such as schizophrenia and depression. In addition, MCH and dopamine receptors can interact in a positive manner, for example in the expression of cocaine self-administration. A recent report (Chung et al., 2011a) showed that the DA1/DA2...

Apomorphine is a potent dopamine agonist at both D1 and D2 receptors and has been used successfully for treating the 'on/off' phenomenon in Parkinson's disease. We report our experience with apomorphine in treating the 'on/off' phenomenon in L-dopa responsive idiopathic Parkinson's disease. Thirteen such patients were commenced on apomorphine infusions. Their mean age was 69 (range 53-80) years...

Previous data have established that postsynaptic stimulation of central dopaminergic receptors was mainly involved in the protective action of apomorphine against the comportmental consequences of hypobaric hypoxia in rats: disturbances in a conditioned avoidance response. We confirm this notion showing that domperidone (a peripheral dopaminergic blocking agent) does not antagonize the protecti...

objective: curcumin is a major constituent of turmeric and influences many functions of the brain. in the present study, we investigated the effect of curcumin on yawning induced by apomorphine in rats. materials and methods: curcumin administered orallyfor 10 consecutive days. yawning was induced by subcutaneous (s.c.) injection of apomorphine (a dopamine receptor agonist) and the number of ya...

BACKGROUND As Parkinson's disease (PD) progresses,despite optimized pharmacotherapy, patients experience more frequent fluctuations between symptomatic improvement ("on" times) and the return of motor features ("off" times). Apomorphine, the first injectable dopamine agonist available in the United States, is indicated for the acute treatment of "off" episodes (eg, end-of-dose wearing-off episo...