Hey
What are the three a subunits
as, ai, aq
What bond makes an irreversible drug binding
Covalent
What is important about full agonists
Has greater affinity for active receptors and it can activate receptors at 100% efficacy
What is the Law of mass action
States that the rate of a chemical reaction is proportional to the concentration (mass) of the reactants
What is an example of an Inverse agonist
Loratadine
Adenylate Cyclase and cAMP
What are the two types of drug receptor interactions
Orthosteric and Allosteric
What is important to note about inverse agonists
Has greater affinity for inactive receptors and has (-) efficacy. Thus, if it binds to an active receptor an inverse agonist can inhibit the receptor
What is the dissociation constant
The ratio of the rate of offset of ligand away from a receptor divided by the rate of onset of the ligand approaching the receptor
What are the general rules of MOAs
1. Drug must reach the site of action
2. Drug must bind to an interact with a receptor
3. Drug do not create anything, but change the ongoing phys. system
What is ai effector and 2nd messenger
Adenylate Cyclase and cAMP
What are second messengers
Small molecules that have been created, degraded or moved by an enzyme, ion channel, or transport protein (effector)
What is important to note about reversible and irreversible antagonists
Neutral; equal affinity for receptors in the active and inactive state with no efficacy and irreversible has the highest affinity
What happens to affinity when the Kd value is low
It increases
What are some Transducers that
Gai and Gas
Phospholipase C and IP3
What are the two basic concepts in Pharmacodynamics
Affinity and Efficacy
What is important to know about allosteric sites
It binds at a different binding site in the receptor and can increase/decrease the affinity and/or efficacy of another drug
If a drug has a low ED50 it has what
high affinity/potency
What are examples of effectors
Adenylate Cyclase and Phospholipase C
RTK is what type of receptor protein
1-transmembrane proteins
What is important partial agonists
Has greater affinity for active receptors, but lower (+) Efficacy than the full agonist (1-99%)
What is important about indirect antagonists
Increase physiological function, binds to components upstream/downstream from the receptor (inhibit the generation of a biological response) and can be reversible or irreversible
What is smaller uM or nM
What are the 5 steps in the RTKs activation
1. Inactive receptor is in a monomeric state
2. Ligand binding to extracellular domain induces Dimerization causing the activation of the receptors
3. Cross-phosphorylation of the kinase domain
4. Phosphorylation forms docking sites and signaling complexes
5. Tyrosine Phosphatase