drug and receptor
the interaction between what two things is ultimately responsible for pharmaceutical effect- pharmacodynamics ?
receptor
-protein-molecule that recognizes and responds to endogenous chemical signals
low
The driving force or drug-receptor complex is at what energy state?
Kd
-measures the affinity of a receptor to a drug
-represents concentration of the drug that gives 50% drug-receptor complex
larger concentration of drug-receptor complex; greater affinity for the drug
A smaller Kd tells us what about the receptor?
Ionic (electrostatic) interaction
-when a full charge interacts with another full charge
histamine, lysine, arginine
Basic groups involves with ionic interactions? (gives us a positive charge)
aspartic acid, glutamine
Acidic groups that give us a negative charge?
ionic
What type of interaction is occuring?
ion-dipole
What type of reaction is this?
dipole-dipole
What type of reaction is this?
hydrogen bonding
What type of reaction is this?
intermolecular
hydrogen bonding that occurs between two molecules
intramolecular
hydrogen bonding that occurs within the same molecule
decreases free energy; stabilizing
Increase in entropy of H2O molecules _______. Leads to _________ the complex
pi stacking
What type of hydrophobic interaction is this?
Van der Waals forces
-as molecules approach, temporary dipoles in one atom induce opposite dipoles in another; therefore, producing an intermolecular attraction
full agonist
What is this a representation of ?
partial agonist
What is this a representation of?
agonist
To effect a certain response of a receptor, design a(n) ____
antagonist
To block a particular response of a natural ligand of a receptor, design a(n)
inverse agonist
To produce the opposite affect of the natural ligand, design a(n)
agonist
Which shows structural similarity to natural ligand; agonist or antagonist?
agonist
What type of drug is this?
antagonist
What type of drug is this?
enantiomer
What type of drug is this?
equilibrium; basal activity
R and R* are in _______ which defines the _________ of the receptor.
Full agonist
______ bind only to R*- lead to an increase in basal activity
Partial agonist
________ bind preferentially to R* (some still bind to R)
Full inverse agonist
__________ bind only to R (decrease in basal activity)
Antagonist
__________ have equal affinities for both R & R* (no effect on basal activity)
eutomer
more potent enantiomer
distomer
less potent enantiomer
eudismic ratio
the ratio of eutomer/distomer potencies of enantiomers
d
Distomers are usually ______
a. more potent
b. less potent
c. equally efficacious
d. impure
chiral
What is the typical stereochemistry of drugs? Chiral or racemic ?
3
How many binding sites must the receptor have in order for the drug to bind?