The evolution of the receptor concept is traced from the turn of the century where the receptor was an organizational concept to the present day where seven transmembrane (7TM) receptors are considered to be complex control units for cellular function. Drug receptor effect can be quantified without knowledge of molecular mechanism through the operational model of drug action. Alternatively, biochemical knowledge of the receptor as an independent protein unit recognizing both external chemicals and cytosolic protein independently can be used to understand ligand-specific receptor effects and how these might be exploited therapeutically.

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