Portal de Periódicos da CAPES

Schild regressions as indicators of non-equilibrium steady-states and heterogeneous receptor populations

1985; Elsevier BV; Volume: 6; Linguagem: Inglês

10.1016/0165-6147(85)90030-6

1873-3735

Terry Kenakin,

Pharmacological Effects and Assays

Schild regression analyses are based on the antagonist-induced shift in concentration-response curves and are a useful tool in determining classification of drugs and their receptors. However their validity depends on true experimental equilibrium conditions, which it is not always possible to achieve. Terry Kenakin demonstrates the usefulness of Schild regression in recognizing 'veiled' non-equilibrium steady states in isolated tissues (which may occur for example when uptake inhibitors also have receptor-blocking properties), and in detecting temporal inequilibrium. He also describes alternate interpretations of regression analyses of data derived from experiments studying effects of a single antagonist on heterogeneous receptor-binding of several agonists. Postulation of different receptor subtypes to account for different curve shifts may not be valid in all cases.