SAR studies of derivatives of diclofenac and meclofenamic acid.
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COX inhibition was measured by the production of PGE2 in cultured mouse colon adenocarcinoma (CT26) and mouse Lewis lung carcinoma cells (D122) cells. IC50 values in µM represent the average values from two experiments, each performed in triplicate. The impact of the compounds on M-channel activity was measured by the heterologous coexpression of Kv7.2 and Kv7.3 subunits in CHO cells. EC50 values in µM represent the average values of opener potency as determined by the concentration-dependent left-shift in the half-activation potential ΔV50 (mV) and fitted by a sigmoidal function (n = 3–5).
创建时间:
2007-12-26



