Ways in which drugs are discovered

Question 1

Three secondary plant metabolites

Answer 1

1. Phenylpropanoids -resveratrol
2. Isoprenoids-evolutionarily present in all known libing organisms
3. Amino-acid derivatives-alkaloids, evolve to be bitter , very bioactive in small concentrations.

Question 2

Where to looks for drug templates

Answer 2

1. Nature
2. Repurposing
3. Rational design -based on known receptor (must consider that receptors are not static.
4. Me-too , similar drug structure to one that is known (analogue).

Question 3

Drug concentration graph talked about is two things

Answer 3

sigmoidal and represents concentration on a log scale

Question 4

True or false, receptors are must smaller than drugs and drugs cover the entire receptor?

Answer 4

False!! Receptors are much bigger than drugs and drugs only bind to a portion of the receptors.

Question 5

Some drugs bind covalently the only way to recover from the effects is

Answer 5

for the body to make new receptors. -Example is aspirin

Question 6

Agonist

Answer 6

binds and causes activation

Question 7

Antagonist

Answer 7

binds and fails to activate

Question 8

Agonist and antagonist are

Answer 8

competitive and binds to where ligand does

Question 9

If agonist or antagonist binds to a different spot, they are referred to as

Answer 9

allosteric activator or allosteric inhibitor

Question 10

Drugs synthesized by a fungus

Answer 10

statins

Question 11

Efficacy

Answer 11

the highest effect that can be achieved with a drug.

Question 12

Potency

Answer 12

The more potent, the lower the EC50

Question 13

Example of competitive binding

Answer 13

Nicotinic receptor binding Ach. Nicotine binds where Ach does.

Question 14

Lower KD =

Answer 14

more potent

Question 15

Constitutive activity

Answer 15

intrinsic activity, different than zero

Question 16

All receptors are present in both the active form and the inactive form

Answer 16

Ra and Ri

Question 17

High affinity for the active form and stabilization of the active form

Answer 17

Full agonist

Question 18

Has affinity for for both the active and inactive form

Answer 18

Partial agonist

Question 19

KD =

Answer 19

concentration of a drug required to bind 50% of receptors in a system.

Question 20

Full agonist + partial agonist, the partial agonist acts as an

Answer 20

antagonist

Question 21

Binds mostly to the inactive form and stabilizes the inactive form and cause the opposite effect to what a full agonist produces

Answer 21

Inverse agonist (GABA receptor)

Question 22

Interacts with the drug itself and not the receptor to inactivate the drug

Answer 22

Chemical antagonist

Question 23

Have the opposite effect to the natural ligand, but binds to a different receptor than the natural ligand

Answer 23

Physiological antagonist

Examples: histamine-bronchiorestricton
Epi-bronchiodilation