UBP-282,544697-47-4

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UBP-282

CAS No. : 544697-47-4

MCE 国际站：UBP-282

产品活性：UBP-282 是一种有效的，选择性的和竞争性的 AMPA 和海藻酸酯 (kainate receptor) 受体拮抗剂。UBP-282 抑制 fDR-VRP 的 IC₅₀ 值为 10.3 μM，拮抗海藻酸酯对背根的去极化作用，pA₂ 值为 4.96。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：iGluR

In Vitro: UBP-282 (3-CBW) is selective for AMPA- and GluR5-containing kainate receptors vs NMDA, mGlu and kainate receptors expressed on motor neurones.
UBP-282 (3-CBW), at a concentration of 200 μM, blocks AMPA evoked depolarizations on motoneurones while responses to equi-effective doses of NMDA and DHPG were relatively unaffected. In the presence of 200 μM UBP-282, a concentration that completely abolishes AMPA-evoked depolarizations on motoneurones and kainate-evoked responses on dorsal root, there is still a noticeable depolarization evoked by kainate on motoneurones.

In Vivo: On neonatal rat motoneurones UBP-282 (3-CBW) (200 μM) almost completely abolished responses to AMPA while responses to NMDA, kainate and DHPG were 101.6%, 39.4% and 110.5% of control, respectively. UBP-282 can therefore be used to isolate kainate receptor responses from those mediated by AMPA receptors.

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