6-Acetyl-5-hydroxy-4,7-dimethylcoumarin derivatives : design, synthesis, modeling studies, 5-HT1A, 5-HT2A and D2 receptors affinity

Molecular docking studies using appropriate 5-HT$_{1A}$, 5-HT$_{2A}$ and D$_{2}$ receptors models were used to design sixteen new 5-hydroxycoumarin derivatives with piperazine moiety (3–18). The microwave radiation have been used to synthesize them and their structures have been confirmed using mass spectrometry, $^{1}$H and $^{13}$C NMR. All newly prepared derivatives were evaluated for their 5-HT$_{1A}$, 5-HT$_{2A}$ and D$_{2}$ receptor affinity. Seven of the synthesized derivatives showed very high affinities to 5-HT$_{1A}$ receptor (3–4.0 nM, 6–4.0 nM, 7–1.0 nM, 9–6.0 nM, 15–4.3 nM, 16–1.0 nM, 18–3.0 nM) and one of them showed high affinities to 5-HT$_{2A}$ receptor (16–8.0 nM). In the case of the D$_{2}$ receptor none of the tested derivatives showed high affinity. Compounds 7 and 16 were identified as potent antagonists of the 5-HT$_{1A}$ receptor as shown by the [35S]GTPcS binding assay but they didn’t show any antidepressant effect at the single dose tested (10 mg/kg) in the tail suspension tests

Evaluation of the Effect of SPIDER System Therapy on Weight Shifting Symmetry in Chronic Stroke Patients—A Randomized Controlled Trial

(1) Background: The Strengthening Program for Intensive Developmental Exercises and Activities for Reaching Health Capability (SPIDER) system is dedicated to patients with motor deficits resulting from damage to the peripheral or central nervous system (including post-stroke patients). It enables the conduct of forced-weight-bearing therapy to the lower limb affected by the paresis. In this study, the TYMO® measuring platform was used to quantify the impact of therapy using the SPIDER system and therapy that did not use this system. The TYMO® device is a portable posturography platform that monitors the tilting of the body’s center of mass and reports the results of the rehabilitation process. (2) Objective: To evaluate the effect of therapy based on neurophysiological methods (proprioceptive neuromuscular facilitation (PNF), neurodevelopmental treatment according to the Bobath concept (NDT-Bobath)) and the SPIDER system on body weight transfer shifting, in post-stroke patients in the chronic phase, compared to therapy based on neurophysiological methods (PNF, NDT-Bobath), without the use of the SPIDER system. (3) Methods: This is a randomized controlled trial in which patients (n = 120; adults, post-ischemic stroke—first stroke episode, in chronic phase—up to 5 years after the stroke incident) were assigned to one of two groups: study, n = 60 (with therapy using PNF, NDT-Bobath methods and the SPIDER system); and control, n = 60 (with therapy using PNF and NDT-Bobath methods, without the SPIDER system). In patients in both groups, before and after the training (2 weeks of therapy), body weight distribution was measured on the TYMO® platform. (4) Results and Conclusions: The results of the statistical analysis demonstrated a greater reduction in the tilt of the body’s center of mass in therapy using the SPIDER system, compared to therapy in which the system was not used