Ch3

Front 1

Rate theory

Back 1

Activation of receptors is proportional to thetotal number of encounters of a drug with itsreceptor per unit time.

- does notrationalize why different types of compoundsexhibit the characteristics they do.

Front 2

occupancy theory

Back 2

Intensity of pharmacological effect is directlyproportional to number of receptors occupied

- does not rationalize why different types of compounds exhibit the characteristics they do.

Front 3

modified occupancy theory

Back 3

(1) binding, or affinity,

(2) initiation ofresponse, called either intrinsic activity (alpha) or efficacy

Front 4

Efficacy

Back 4

Efficacy is the property of a compound that producesmaximum response or ability to initiate a response

Front 5

efficacy is also known as

Back 5

intrinsic activity

Front 6

Back 6

All are full agonists (sameefficacy; different affinities)

Front 7

Back 7

5 different drugs (same affinitiesbut different efficacies)

Front 8

when alpha =1

Back 8

full agonist

Front 9

when alpha is less than one

Back 9

partial agonist

Front 10

A full or partial agonist displays _______ efficacy

Back 10

positive efficacy

Front 11

An antagonist displays _____ efficacy

Back 11

zero efficacy

Front 12

A full or partial inverse agonist displays _____ efficacy.

Back 12

negative efficacy

Front 13

agonist, antagonist, partial agonist: which one induces a conformational change?

What theory is this?

Back 13

agonist and partial agonist

induced fit theory

Front 14

Activation -Aggregation theory

Back 14

Receptor is always in a state of dynamic equilibrium between activated form and inactive form

Front 15

which one is active and which one is inactive

Back 15

R- active T -inactive

Front 16

partial agonist bind to: R or T

Back 16

both

Front 17

agonist shift equilibrium to R or T?

Back 17

R

Front 18

antagonists shift equilibirum to R or T?

Back 18

T

Front 19

Two-state (Multi-state) Receptor Model

Back 19

have two states R and activated R*

Front 20

in the two state model where does agonist bind?

Back 20

R*

Front 21

in the two state model where does partial agonist bind?

Back 21

R*

Front 22

in the two state model where does antagonist bind?

Back 22

R and R*

Front 23

in the two state model where does full inverse agonist bind?

Back 23

only R

Front 24

all receptors are ______ and always _____

Back 24

chiral and S

Front 25

racemic drugs have

Back 25

S or R form

Front 26

what is the pharmacophore for antihistamine

Back 26

Front 27

the more potent enantiomer is called the

Back 27

eutomer

Front 28

the less potent enantiomer is called the

Back 28

distomer

Front 29

what is the eudismic ratio and when is it high

Back 29

Ratio of eutomer/distomer potencies of enantiomers

High eudismic ratio when antagonist has chiral center inpharmacophore

Front 30

a distomer is really an

and may do what

Back 30

impurity (isomeric ballast )

May contribute to side effects and/or toxicity–the eutomer of the side effects

Front 31

example of a distomer

Back 31

S thalinomide

Front 32

how many points of interaction does a receptor need to distinguish an enantionmer

Back 32

3

Front 33

diasteromers

Back 33

non mirror images of one another, geometric isomers.. E and Z

Front 34

conformational isomers (conformers)

Back 34

differ by change in conformation

Front 35

conformationally rigid analogs allow you to do what and how

Back 35

To determine the active conformation, make conformationallyrigid analogs. The flexible lead molecule is locked into variousconformations by adding bonds to rigidify it. Pharmacophoricgroups are locked into various configurations; most potent isprototype for structural modification

Front 36

Atropisomerism occurs when there is

Back 36

hindered rotation about asingle bond as a result of steric or electronic constraints, causingslow interconversion of two conformers (a rule of thumb is a halflife> 1000 sec)

Front 37

considering 3D structures of rings... tranquilizers have what kind of angle

Back 37

aplha

Front 38

considering 3D structures of rings... alpha and beta give you

Back 38

mixed

Front 39

considering 3D structures of rings... alpha, beta, gamma give you

Back 39

antidepressants