RESUMO
Two novel 8-azabicyclo[3.2.1]octan-3-ol derivatives, 11a and 11b, with high affinity for sigma-2 receptors and a very good sigma-1/sigma-2 selectivity ratio were synthesized. In comparison with several well established sigma-2 selective ligands, 11 b showed a very low sigma-1 receptor affinity. Functional assays demonstrated that 11b acts as an agonist and in A-375 human melanoma cell line is able to lower levels of procaspase-3, thus confirming a potential major role for sigma-2 pure agonists in the treatment of rapid proliferating melanoma cells.
Assuntos
Caspase 3/metabolismo , Melanoma Experimental/enzimologia , Receptores sigma/efeitos dos fármacos , Animais , Caspase 3/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Ativação Enzimática/efeitos dos fármacos , Cobaias , Humanos , Íleo/efeitos dos fármacos , Técnicas In Vitro , Melanoma Experimental/tratamento farmacológico , Contração Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Especificidade por Substrato , Receptor Sigma-1RESUMO
AIM: The Back School is a widely accepted and effective method for treating low back pain, whereas no scientific evidence exists about the effects of the Pilates CovaTech method. With this study we wanted to evaluate the efficacy of this new method in patients with low back pain. METHODS: Fifty-three patients with at least 3 months of nonspecific low back pain were entered into a Pilates therapy or a Back School treatment group, 43 of which completed the study. Small exercise groups of 7 patients each followed a daily kinesitherapy protocol for 10 days. Evaluations were performed at the start of the study and then at 1, 3 and 6 months after the beginning of treatment. We used the Oswestry Low Back Pain Disability Scale (OLBPDQ) to assess disability and the visual analog scale (VAS) to evaluate pain. RESULTS: Demographic and baseline clinical characteristics were similar for both groups. A significant reduction in pain intensity and disability was observed across the entire sample. The Pilates method group showed better compliance and subjective response to treatment. CONCLUSIONS: The results obtained with the Pilates method were comparable to those achieved with the Back School method, suggesting its use as an alternative approach to the treatment of non specific low back pain.
