Small molecule sodium ion channel blockers with a pharmacophore of a-aminoamide have exhibited anti-allodynia effects on neuropathic pain. A library of new a-aminoamide derivatives containing a scaffold of substituted...Small molecule sodium ion channel blockers with a pharmacophore of a-aminoamide have exhibited anti-allodynia effects on neuropathic pain. A library of new a-aminoamide derivatives containing a scaffold of substituted benzene were designed and synthesized. These compounds were evaluated in mice formalin model and they exhibited significant analgesic activities. However, the anti-allodynia mechanism of these compounds remains unclear; some of the target compounds can only moderately inhibit the sodium ion channel, Navl.7, in a whole-cell patch clamp assay. These results suggest that introduction of the moiety of substituted benzene to a-aminoamide derivatives can improve their bioactivity and further study is warranted.展开更多
基金the Beijing Municipal Science and Technology Project(No.Z131100002713004)National Science and Technology Major Project of China(No.2012ZX09301003)
文摘Small molecule sodium ion channel blockers with a pharmacophore of a-aminoamide have exhibited anti-allodynia effects on neuropathic pain. A library of new a-aminoamide derivatives containing a scaffold of substituted benzene were designed and synthesized. These compounds were evaluated in mice formalin model and they exhibited significant analgesic activities. However, the anti-allodynia mechanism of these compounds remains unclear; some of the target compounds can only moderately inhibit the sodium ion channel, Navl.7, in a whole-cell patch clamp assay. These results suggest that introduction of the moiety of substituted benzene to a-aminoamide derivatives can improve their bioactivity and further study is warranted.
