Receptors
Receptors are typically glycoproteins located in cell membranes that specifically recognize and bind to ligands. These are smaller molecules (including drugs) that are capable of 'ligating' themselves to the receptor protein. This binding initiates a conformational change in the receptor protein leading to a series of biochemical reactions inside the cell (‘signal transduction’), often involving the generation of ‘secondary messengers’ that is eventually translated into a biological response (e.g. muscle contraction, hormone secretion). Although the ligands of interest to prescribers are exogenous compounds (i.e. drugs), receptors in human tissues have evolved to bind endogenous ligands such as neurotransmitters, hormones, and growth factors. Formation of the drug-receptor complex is usually reversible and the proportion of receptors occupied (and thus the response) is directly related to the concentration of the drug. Reversibility enables biological responses to be modulated and means that similar ligands may compete for access to the receptor. The term 'receptor' is usually restricted to describing proteins whose only function is to bind a ligand, but it is sometimes used more widely in pharmacology to include other kinds of drug target such as voltage-sensitive ion channels, enzymes and transporter proteins.
This is a set of 20 slides suitable for beginners wishing to gain an understanding of the basic principles underlying receptor pharmacology. Provided by Prof. JA Peters, University of Dundee School of Medicine.