4) (15), and D(1) (83) Significant affinities were also demonstr

4) (15), and D(1) (83). Significant affinities were also demonstrated at alpha-adrenergic (alpha(2B), SNX-5422 K (i) = 27 nM) and serotonin receptors (5-HT(1A) K (i) = 30 nM). In newly developed reporter-gene assays

for determination of functional activity, rotigotine behaved as a full agonist at dopamine receptors (rank order: D(3) > D(2L) > D(1) = D(5) > D(4.4)) with potencies 2,600 and 53 times higher than dopamine at dopamine D(3) and D(2L) receptors, respectively. At alpha-adrenergic sites, rotigotine acted as an antagonist on alpha(2B) receptors. At serotonergic sites, rotigotine had a weak but significant agonistic activity at 5-HT(1A) receptors and a minor or nonexistent activity at other serotonin receptors. Thus, in respect to PD, rotigotine can be characterized as a

specific dopamine receptor CP-868596 supplier agonist with a preference for the D(3) receptor over D(2) and D(1) receptors. In addition, it exhibits interaction with D(4) and D(5) receptors, the role of which in relation to PD is not clear yet. Among non-dopaminergic sites, rotigotine shows relevant affinity to only 5-HT(1A) and alpha(2B) receptors. Further studies are necessary to investigate the contribution of the different receptor subtypes to the efficacy of rotigotine in Parkinson’s disease and possible other indications such as restless legs syndrome.”
“Dietary strategies to improve early cardiovascular markers in overweight children are needed. We investigated the effect of dietary protein and glycemic index (GI) on cardiovascular markers and:metabolic syndrome (MetS) scores in 5- to 18-y-old children of overweight/obese parents from 8 European centers. Families were randomized to 1 of 5 diets consumed ad libitum: high protein

(HP) or low protein (LP) combined with. high GI (HGI) or low GI (LGI), or a control diet. At 6 centers, families received dietary instruction (instruction centers); at 2 centers, free foods were also provided (supermarket centers). Diet, anthropometry, blood pressure, and serum cardiovascular markers (lipid profile, glucose regulation, and inflammation) were measured in 253 children GW786034 order at baseline, 1 mo, and/or 6 mo. Protein intake was higher in the HP groups (19.9 +/- 1.3% energy) than in the LP groups at 6 mo (16.8 +/- 1.2% energy) (P = 0.001). The GI was 4.0 points lower (95% CI: 2.1, 6.1) in the LGI compared with the HGI groups (P < 0.001). In the supermarket centers, the HP and LP groups differed more in protein intake than did the groups in the instruction centers (P = 0.009), indicating better compliance. The HP diets evoked a 2.7-cm (95% CI: 0.9, 5.1) smaller waist circumference and a 0.25-mmol/L (95% CI: 0.09, 0.41) lower serum LDL cholesterol compared with the LP diets at 6 mo (P < 0.007). In a separate supermarket center analysis, the HP compared with LP diets reduced waist circumference (P = 0.004), blood pressure. (P < 0.01), serum insulin (P = 0.013), and homeostasis model of assessment-insulin resistance (P = 0.016).

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