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Philanthotoxin 74 dihydrochloride

CAS No. : 1227301-51-0

MCE 站：Philanthotoxin 74 dihydrochloride

产品活性：Philanthotoxin 74 dihydrochloride (PhTx 74) 是 AMPAR 的拮抗剂; 抑制 GluR3 和 GluR1 的 IC₅₀ 值分别为263和296 nM。

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

作用靶点：iGluR

In Vitro: Philanthotoxin 74 in the micromolar concentration range displays selective inhibition between the two major subtypes of GluA2R-containing AMPARs, GluA1/A2R and GluA2R/A3, when these are coexpressed with γ-2 in oocytes. Philanthotoxin 74 is reported to fully inhibit GluA1/A2R receptors when applied at a concentration of 500 μM while producing 10% inhibition at GluA2R/A3 receptors. Philanthotoxin 74, when tested at concentrations of 100 and 500 μM, displays pronounced channel block (more than 80%) of GluA1/A2R but minimal block (less than 10%) of GluA2R/A3. Oocytes expressing GluA2R alone that homomeric GluA2R is virtually inert to philanthotoxin 74 in the 0.1-300 μM concentration range, displaying less than 5% inhibition at the maximum tested concentration of 300 μM. Philanthotoxin 74 inhibits these receptors nonselectively, with IC₅₀ values of about 30 μM, in both the presence and absence of γ-2.

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