Current preclinical evidence supports the modulatory role of the sigma-1 receptor (σ1R) in nociception, mainly based on the pain-attenuated phenotype of σ1R knockout mice and on the antinociceptive effect exerted by σ1R antagonists on pain of different etiology, very consistently in ...
:The sigma 1 receptor (S1R) is a molecular chaperone protein located in the endoplasmic reticulum and plasma membranes and has been shown to play important roles in various pathological disorders including pain and, as recently discovered, COVID-19. Employing structure- and QSAR-based drug design...
The sigma-1 receptor (σ1R), an endoplasmic reticulum chaperone protein, is widely distributed and regulates numerous intracellular processes in neurons. Nerve injury alters the structure and function of axotomized dorsal root ganglion (DRG) neurons, contributing to the development of pain. The σ1...
30, we also investigated phosphorylation in the spinal cord of the glutamateN-methyl-D-aspartate (NMDA) receptor and the extracellular signal-regulated kinase (ERK1/2); both of which are reportedly involved in central sensitization19and hypersensitivity in neuropathic pain conditions31,32...
Role of Sigma-1 Receptor/p38 MAPK Inhibition in Acupoint Catgut Embedding–Mediated Analgesic Effects in Complete Freund’s Adjuvant-Induced Inflammatory Pain 背景与目的 内质网伴侣蛋白Sigma-1受体(Sig-1R)和丝裂原活化蛋白激酶(MAPKs)参与疼痛的致病机制。穴位刺激在炎性疼痛中发挥抗痛觉过敏作用。然而,Sig-...
Sigma-1 Receptor and Pain There is a critical need for new analgesics acting through new mechanisms of action, which could increase the efficacy respect to existing therapies and/or... M Merlos,L Romero,D Zamanillo,... 被引量: 6发表: 2017年 Antinociception by Sigma-1 Receptor Antagonists ...
11. M. C. Ruiz-Cantero, R. González-Cano, M. Tejada, M. Santos-Caballero, G. Perazzoli, F. R. Nieto, E. J. Cobos, Sigma-1 receptor: A drug target for the modulation of neuroimmune and neuroglial interacti...
11. M. C. Ruiz-Cantero, R. González-Cano, M. Tejada, M. Santos-Caballero, G. Perazzoli, F. R. Nieto, E. J. Cobos, Sigma-1 receptor: A drug target for the modulation of neuroimmune and neuroglial interactions during chronic pain.Pharmacological research163, 105339 (2021). ...
英文名称 Sigma-1 receptor antagonist 3 生化机理 Sigma-1 受体拮抗剂 3(化合物 135)是一种强效且具有选择性的 Sigma-1 (σ1) 受体拮抗剂,其 K i 为 1.14 nM。Sigma-1 受体拮抗剂 3 可抑制人乙醚-a-go-相关基因(hERG),IC 50 为 1.54 μM。Sigma-1 受体拮抗剂 储存温度 -80℃储存 运输条件...
Sigma-1 receptor (σ1R), an endoplasmic reticulum-chaperone protein, can modulate painful response after peripheral nerve injury. We have demonstrated that voltage-gated calcium current is inhibited in axotomized sensory neurons. We examined whether σ1R contributes to the sensory dysfunction of voltag...