Sigma-1 receptor antagonists: promising players in fighting neuropathic pain
Sigma-1 receptor antagonists: promising players in fighting neuropathic pain
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DOI：
10.4155/ppa-2020-0007
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发表时间：
2020-05-01
影响因子：
1.3
通讯作者：
Collina, Simona
中科院分区：
文献类型：
--
作者：
Linciano, Pasquale;Rossino, Giacomo;Collina, Simona
σ-1受体（S1 R）与神经性疼痛（NP）密切相关，因为它们的失活可以减少异常性疼痛或感觉迟钝，促进镇痛作用。在最近的专利景观中，具有纳摩尔S1 Rs亲和力的S1 R拮抗剂成为有效的抗伤害感受剂。到目前为止，已经提出了三种专利化合物来对抗NP。特别是分别由帕维亚大学（意大利）和Anavex公开的PV 752和AV 1066在临床前研究中显示出良好的镇痛活性。此外，Esteve（西班牙）开发的E 52862在临床前和II期临床试验中已被证明对NP的几种症状有效。这些专利确定S1 R拮抗剂作为潜在的药物，单独或与其他镇痛药物组合，用于管理人类NP。
Sigma-1 receptors (S1Rs) are strongly correlated to neuropathic pain (NP), since their inactivation may decrease allodynia or dysesthesia, promoting analgesic effects. In the recent patent landscape, S1R antagonists endowed with nanomolar S1Rs affinity emerged as potent antinociceptive agents. So far, three patented compounds have been proposed for counteracting NP. Particularly PV 752 and AV1066, disclosed by the University of Pavia (Italy) and Anavex, respectively, showed good analgesic activity in preclinical studies. Moreover, E 52862 developed by Esteve (Spain) has been proved to be effective, both in preclinical and Phase II clinical trials, against several symptoms of NP. These patents ascertain S1R antagonists as potential drugs, alone or in combination with other analgesic drugs, for managing NP in humans.