Dario Alessandro, Pisani Rossana, Sangiorgi Simone, Soragna Andrea, Reguzzoni Marcella, Protasoni Marina, Pessina Federico, Fesce Riccardo, Peres Antonio, Tomei Giustino
Neurosurgical Clinic, University of Insubria, Via L. Borri 57, 21100 Varese, Italy.
Eur J Pharmacol. 2006 Nov 21;550(1-3):33-8. doi: 10.1016/j.ejphar.2006.08.068. Epub 2006 Sep 8.
Up to now, baclofen (a GABA(B) receptor agonist) has been used for the treatment of severe spasticity unresponsive to oral antispasmodics. Although in humans it is usually administered at 2 mg/ml, the dosage to be used in the treatment of other diseases is unknown. For this reason, it is important to determine the safe maximum dosage and toxicity at the clinically used concentration. Primary cortical neurons represent a useful model to test the safety of baclofen. We performed a colorimetric assay (MTT test) as well as electron microscopy investigations, to determine neuronal survival after the treatment with baclofen at a concentration of 2 and 4 mg/ml. Our results demonstrated that, in our experimental model, neither concentration affected neuronal survival. Considering the above results, we can conclude that at the used concentrations, this drug is safe and its clinical use should be encouraged.
到目前为止，巴氯芬（一种γ-氨基丁酸（B）受体激动剂）已被用于治疗对口服抗痉挛药无反应的严重痉挛。尽管在人类中通常以2毫克/毫升的剂量给药，但用于治疗其他疾病的剂量尚不清楚。因此，确定临床使用浓度下的安全最大剂量和毒性很重要。原代皮层神经元是测试巴氯芬安全性的有用模型。我们进行了比色测定（MTT试验）以及电子显微镜研究，以确定在2毫克/毫升和4毫克/毫升浓度的巴氯芬治疗后神经元的存活情况。我们的结果表明，在我们的实验模型中，两种浓度均未影响神经元的存活。考虑到上述结果，我们可以得出结论，在所使用的浓度下，这种药物是安全的，应该鼓励其临床应用。
