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Antagonist拮抗药 Competitive antagonist 竞争性拮抗药 Ligand (L) Inhibitor(I) [RT] = [R] + [LR] + [IR] [LR]/[RT] = [L]/KD + [L] [LR]/[RT] = [L]/[L] + KD(1 + [I]/KI) Competitive Antagonist 药物的作用取决于 [I]/KI， [I]浓度愈高或KI愈小,激动药的效应低， 拮抗作用强。 如果[LR]/[RT]→100%, 激动药的量效 反应曲线可以被竞争性拮抗药平行右移。 如果增加竞争性激动药浓度，仍可达到 Emax. Competitive Antagonist(A) 激动药的量效反应曲线被竞争性拮抗药平行右移, 如果增加竞争性激动药浓度，仍可达到Emax。 Competitive Antagonist(A) 激动药的量效反应曲线被竞争性拮抗药平行右移, 如果增加竞争性激动药浓度，仍可达到Emax。 Competitive Antagonist pA2 is the antagonism parameter pA2 = -log[I] = -logKI pA2 Express the extent of antagonism of a given antagonist, when the agonist and antagonist are used in same preparation, two times concentration (X2) of agonist(A2) only produce ordinary concentration of that agonist effect, in that time the negative log concentration of antagonist is