SYM 2081

SYM 2081 is a kainate receptor agonist. SYM 2081 is a substrate of EAAT1 (K_m of 54 μM). SYM 2081 inhibits EAAT2-mediated glutamate transport (K_b is 3.4 μM in Xenopus oocytes), modulates Apoptotic signaling pathways (increases Bcl-2 and decreases Bax/caspase-3 expression). SYM 2081 exhibits neuroprotective activity. SYM 2081 can be used in the study of hypoxic-ischemic brain damage and inflammatory or neuropathic pain^[1][2][3][4]. IC50 & Target:IC50: 35 nM (kainate receptors)^[1] In Vitro:SYM 2081 is transported by EAAT1 expressed in Xenopus laevis oocytes with a K_m of 54 μM, while it potently blocks glutamate transport by EAAT2 with a K_b of 3.4 μM^[2].
SYM 2081 (10 μg/mL; 16 h) increases Bcl-2 expression and decreases Bax/caspase-3 expression and Bax/Bcl-2 ratio in cultured embryonic cortical neuronal cells under hypoxia^[4]. In Vivo:SYM 2081 (10-100 mg/kg; i.p.; before Capsaicin) attenuates Capsaicin (HY-10448)-evoked mechanical and heat hyperalgesia in rats^[3].
SYM 2081 (10 mg/kg; i.p.; 30 min before the hypoxic exposure) reduces apoptosis in the hypoxic-ischemic brain of neonatal rats by increasing Bcl-2 expression and decreasing Bax/caspase-3 expression and Bax/Bcl-2 ratio^[4].