Receptors Flashcards
Ligands
chemical substances that bind to a specific receptor
agonists
binds to a receptor and stimulates the function that receptor serves
antagonists
binds to a receptor and blocks the function that receptor serves
competitive binding
reversible binding with the receptor - it’ll wear off/terminate
noncompetitive
irreversible binding - in order for bond to be broken receptor or cell would have to be destroyed
ED50
effective dose in 50% of the population
TD50
toxic dose in 50% of the population
LD50
lethal dose in 50% of the population
LD50/ED50
Therapeutic index - the higher, the safer the drug is
TD50/ED50
therapeutic window - estimation of drug dosage which can treat disease effectively while staying within the safety range
receptor
macromolecular complex which acts as the site of action for a drug. They are usually proteins involved in a production of normal cellular function. They may include membrane proteins, enzymes, carrier molecules, ion channels, nucleic acids.
Bond strength of the chemical bonds
Covalent > Ionic > Hydrogen > Hydrophobic > van der Waals
“Can I have higher valuables?”
Down regulation
continued stimulation of cells with agonists generally results in a state of desensitization - cells decrease the number of receptors for a given drug in response to chronic stimulation (insulin/glucose relationship in DM)
Up regulation
process by which a cell increases the number of receptors to a given drug (chronic blockage with BBs)
Interaction
alteration in the therapeutic action of a drug by concurrent administration of other exogenous chemicals
