Drug Receptors Flashcards
Super Family: Ligand Gated Channels
Activated by:
Response time:
Found in:
Ligand
Milliseconds
Neurons
Superfamily: GPCRs Activated by: Response times: Found in: Additional uses:
Exocrine ligands binding to the outside of cell membrane
Seconds
Every cell
Hormonal uses
Superfamily: Kinase-Linked Activated by: Response time: Found in: Additional uses:
Cytokine or growth factor
Hours
differentiating cells
Complex cell functions
Nuclear Receptors
Activated by:
Response time:
Found in:
small lipid molecules (Hormones)
hours
cytosol
Nicotinic Acetylcholine Receptor (nAChR) is an example of what type of receptor
Ligand gated ion channel
B Adrenergic receptor is an example of what type of receptor
G protein coupled receptor
Epidermal Growth factor is an example of what receptor
Kinase linked receptor
Mineral cortoid receptors an example of what type of receptor
Nuclear receptor
Drug Binding: Define Lock and Key Design
Lock and key is defined by the receptor requiring an exact fit of a ligand in order for activation to occur
Drug Binding: Law of Mass action High and low infers what about the affinity
High: Low affinity
Low: High affinity
Due to kd = Reverse / Forward (rates)
Define Affinity
Affinity is the tendency to bind to a certain receptor
Define Efficacy
Efficacy is the tendency to activate bound receptors
Define Antagonist
A molecule that has affinity but no efficacy
Define Agonist
A molecule that has affinity and efficacy
EC50 means?
Amount of drug required to reach half maximal effect
