LDN-212320 functions as an activator for the glutamate transporter (GLT-1)/excitatory amino acid transporter 2 (EAAT2) at the translational level. It alleviates nociceptive pain through the upregulation of astroglial GLT-1 expression in the hippocampus and anterior cingulate cortex (ACC)[1][2].
LDN-212320 (10 or 20 mg/kg, i.p) significantly counteracts the impairment of hippocampal-dependent behavior induced by formalin. Moreover, LDN-212320 (10 or 20 mg/kg, i.p) enhances GLT-1 expression in the hippocampus and anterior cingulate cortex (ACC)[1].
LDN-212320 (20 mg/kg, i.p) significantly diminishes formalin-induced ERK phosphorylation, an indicator of nociception, in the hippocampus and anterior cingulate cortex (ACC)[1].
LDN-212320 动物实验
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Animal Model
Administration
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Description
References
C57BL/6NCrl mice
Photothrombotic focal ischemia model
Intraperitoneal injection
40-100 mg/kg
Single injection, 24 hours or 2 hours before inducing focal ischemia
To evaluate the effects of LDN on stroke-associated brain injury. Male mice treated with LDN showed upregulated GLT-1 protein levels, significantly smaller infarct size, and better sensorimotor performance compared to vehicle-treated males. In contrast, female mice treated with LDN did not show upregulated GLT-1 protein levels, and there was no difference in infarct size or sensorimotor performance between vehicle- and LDN-treated females.
Brain Sci. 2021 Jan 8;11(1):76
Male FVB/N mice
Healthy wild-type mice
Intraperitoneal injection
40 mg/kg
Single injection
LDN significantly increased total GLT-1 expression in the hippocampus, cortex, and striatum but had minimal impact on the clearance rate of extracellular glutamate following evoked synaptic release.
Front Cell Neurosci. 2021 Mar 26;15:661412
C57BL/6J mice
CFA-induced chronic inflammatory pain model
Intraperitoneal injection
20 mg/kg
Administered 24 h prior, duration of 7 days
LDN-212320 significantly attenuated CFA-induced tactile allodynia and thermal hyperalgesia by upregulating astroglial GLT-1 and CX43 expression and decreasing microglial activation in the hippocampus and ACC.
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