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σ受体调节剂是对抗多发性硬化症的武器吗?

Are sigma receptor modulators a weapon against multiple sclerosis disease?

作者信息

Collina Simona, Rui Marta, Stotani Silvia, Bignardi Emanuele, Rossi Daniela, Curti Daniela, Giordanetto Fabrizio, Malacrida Alessio, Scuteri Arianna, Cavaletti Guido

机构信息

Department of Drug Sciences, Medicinal Chemistry & Pharmaceutical Technology Section, Centre for Health Technologies (CHT), University of Pavia, Viale Taramelli 12, Pavia 27100, Italy.

Medicinal Chemistry, Taros Chemicals GmbH & Co. KG, Emil-Figge-Str. 76a, Dortmund 44227, Germany.

出版信息

Future Med Chem. 2017 Nov;9(17):2029-2051. doi: 10.4155/fmc-2017-0122. Epub 2017 Oct 27.

Abstract

Effective therapies for multiple sclerosis (MS) are still missing. This neurological disease affects more than 2.5 million people worldwide. To date, biological immunomodulatory drugs are effective and safe during short-term treatment, but they are suitable only for parenteral administration and they are expensive. Accordingly, academic and industrial environments are still focusing their efforts toward the development of new MS drugs. Considering that neurodegeneration is a contributory factor in the onset of MS, herein we will focus on the crucial role played by sigma 1 receptors (S1Rs) in MS. A pilot study was performed, evaluating the effect of the S1R agonist (R)-RC33 on rat dorsal root ganglia experimental model. The encouraging results support the potential of S1R agonists for MS treatment.

摘要

目前仍缺乏针对多发性硬化症(MS)的有效疗法。这种神经系统疾病在全球影响着超过250万人。迄今为止,生物免疫调节药物在短期治疗中有效且安全,但仅适用于肠胃外给药且价格昂贵。因此,学术界和产业界仍在致力于开发新的MS药物。鉴于神经退行性变是MS发病的一个促成因素,在此我们将聚焦于σ1受体(S1Rs)在MS中所起的关键作用。我们进行了一项初步研究,评估S1R激动剂(R)-RC33对大鼠背根神经节实验模型的作用。这些令人鼓舞的结果支持了S1R激动剂用于治疗MS的潜力。

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