第二章药效学 3.pptVIP

Occupation theory A + R AR E K1 K2 When receptors are occupied, the pharmacological effects will occur. The effects of drug are directly proportional to the numbers of receptors occupied. * Development of occupation theory 令 KD = K2 / K1； A + R AR E K1 K2 Clark（1926） * Development of occupation theory 整理后得：[AR](KD+[A])=[A] [RT] 因为: [RT]=[R]+[AR]，[R]=[RT]-[AR]； 代入R得： * Development of occupation theory When [AR]/[RT]=0, E=0. When [A]＞＞KD, [AR]/[RT]=1, [AR]=[RT] , E=Emax. When [AR]/[RT]=1/2, E=50%Emax, KD = [A]. * Interaction between drug and receptor