Binding affinities for selected pharmacophore hit compounds at the α1-adrenoceptors (ARs).
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n represents the number of experiments, each performed in triplicate.Ø represents no binding at concentrations up to 100 µM.apKi (−Log Ki).bKi (inhibition constants) are the antilog of mean pKi.Ki values were calculated according to the equation of Cheng and Prusoff . Ki = IC50/1 + ([L]/KD) when [L] is the radioligand concentration and KD its dissociation constant.Aindicates significant differences from the α1A –AR (pBindicates significant differences from the α1B –AR (pDindicates significant differences from the α1D –AR (p
n代表实验总次数,每组实验均进行三次平行重复。符号Ø表示当浓度最高达100 μM时未发生结合。apKi即负对数Ki值(−Log Ki)。bKi(抑制常数,inhibition constants)为平均pKi的反对数。Ki值按照程-普雷索夫(Cheng-Prusoff)公式计算:当[L]为放射性配体(radioligand)浓度、KD为其解离常数(dissociation constant)时,Ki = IC₅₀ / (1 + [L]/K_D)。A表示与α₁A-肾上腺素能受体(α₁A–AR)存在显著性差异,B表示与α₁B-肾上腺素能受体(α₁B–AR)存在显著性差异,D表示与α₁D-肾上腺素能受体(α₁D–AR)存在显著性差异(原文此处p值未完整标注)。




