Ligand A chemical which specifically binds to a receptor Agonist - Binds to a receptor and generates a receptor and causes a biological response Antagonist - Binds to a receptor and generates no response
Receptor A membrane protein which binds a drug Activation causes intracellular changes Drugs bind to specific receptors and saturate the binding We have receptors for hormones produced in the body (Ex: morphine receptors are present in the body because of endorphin hormone receptors) Possess structural and steric specificity Expressed in select tissues Saturable and finite (Limited number of binding sites) High affinity for the ligand o Ex: Adrenaline acts on the B1-adrenorecptor in the heart to increase the rate and force of cardiac contraction o Ex: Dopamine binds to dopamine receptors in the brain as a reward signal o Ex: Angiotensin will only act on angiotensin receptors on vascular NOT smooth tissue. Only on kidney epithelium but NOT intestinal epithelium. Tissue responses are generally directly proportional to the fraction of the receptors occupied with agonist Dose-response curve - Graph reaches a plateau where no more additional agonist has an effect on the response (No more receptors to bind to) EC50 = The 50% response of effective concentration between the baseline and max response (Compare drugs by looking at the dose that creates a 50% response)