| 规格: | 98% |
| 分子量: | 328.7 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
Background:
JNJ-55511118 is a negative modulator of AMPA receptors containing transmembrane AMPA receptor regulatory protein γ8 (TARP-γ8).1 It inhibits glutamate-induced calcium flux in HEK293F cells co-transfected with TARP-γ8 and either GluA1o, GluA1i, GluA2i, GluA3o, or GluA4o (IC50s = 11.22, 12.3, 7.41, 38.02, and 15.85 nM, respectively). JNJ-55511118 is selective for GluA1o receptors containing TARP-γ8 over GluA1o receptors containing TARP-γ2, -γ3, -γ4, or -γ7 (IC50s = >10 μM for all). It reduces peak glutamate-induced currents in acutely dissociated murine hippocampal neurons to 60.7% of control cells when used at a concentration of 1 μM. JNJ-55511118 (1 μM) reduces field excitatory postsynaptic potentials (fEPSPs) in the hippocampal CA1 region from wild-type, but not TARP-γ8 knockout, mice. It also inhibits corneal kindling-induced seizures in mice (ED50 = 3.7 mg/kg).
|1. Maher, M.P., Wu, N., Ravula, S., et al. Discovery and characterization of AMPA receptor modulators selective for TARP-γ8. J. Pharmacol. Exp. Ther. 357(2), 394-414 (2016).
m.cnreagent.com