Receptors

Question 1

Purpose is to approve or reject applications from drug companies to market new drugs; old drugs which fail to meet, purity, safety or efficacy standards may be removed from the market

Answer 1

FDA

Question 2

Purpose is to establish a balance between legitimate medical needs while minimizing the availability of the drug for abuse

Answer 2

DEA

Question 3

Regulates the manufacture, distribution, dispensing, use and possession of all CNS drugs with abuse potential with the exceptions of alcohol and tobacco

Answer 3

1970-comprehensive drug abuse, prevention and control act

Question 4

What schedule class has the highest potential abuse?

Answer 4

C-1

Question 5

What drugs are included in C-1 drugs

Answer 5

Heroin, LSD, marijuana, mescaline, PCP….illegals

Question 6

What drugs are common in C2

Answer 6

Morphine and methylphenidate

Question 7

What class does Tylenol #3 belong to

Answer 7

C-III

Question 8

What class are benzodiazepines part of

Answer 8

C-IV

Question 9

Which class has the least abuse potential

Answer 9

C-V

Question 10

What class are gabapentin and some codeine-containing cough syrups part of

Answer 10

C-V

Question 11

What is a true receptor

Answer 11

Elicits a biological response when bound by an agonist

Question 12

Receptor ligand binding theory

Answer 12

Drug molecule and biological target must come together (don’t act at a distance, must result in selective binding

Question 13

What are most receptors

Answer 13

Proteins

Question 14

When a drug binds and there is no detectable changes in function of the biological system

Answer 14

Insert binding sites

Question 15

Ionization and binding

Answer 15

It can affect binding

Question 16

Physical characteristics of drugs

Answer 16

Solid
Liquid
Gas

Question 17

Drug size

Answer 17

Related to specificity for a receptor and movement within the body

Question 18

What is the order of bonds from strongest to weakest?

Answer 18

Covalent 
Ionic 
Hydrogen 
Dipole-dipole 
Hydrophobic

Question 19

What is the order of bonds from selective to not so selective

Answer 19

Hydrophobic
Dipole-dipole
Hydrogen 
Ionic 
Covalent

Question 20

Which drugs are usually more selective?

Answer 20

Drugs which bind via weak bonding to their receptors. They have less places to bind to

Question 21

__________ is crucial for proper binding (lock and key)

Answer 21

Drug shape

Question 22

What aspect of drug shape is most important

Answer 22

Chirality

-mirror images, but nonsuperimposable

Question 23

What are two examples of ion channel receptors

Answer 23

• ligand gated ion channels

- voltage gated ion channels

Question 24

Examples of ligand gated ion channels

Answer 24

Nicotinic Ach receptors
Glutamate receptors
GABA receptors

Question 25

Where are nicotinic Ach receptors found

Answer 25

- ligand-gated ion channel | - found on muscle cell end plate NM junction, at all autonomic ganglia, in the CNS

Question 26

How do nicotinic Ach receptors open the channel

Answer 26

Binding of 2 molecules of Ach opens channel, both alpha subunits must be occupied

Question 27

Prolonged Ach contact with nicotinic receptor

Answer 27

Desensitization

Question 28

How many subunits on nicotinic Ach receptor

Answer 28

5, alpha subunit must bind 2 Ach

Question 29

Main excitatory NT in the CNS

Answer 29

Glutamate

Question 30

What kind of receptors are glutamate receptors

Answer 30

Either ligand-gated ion channels (ionotropic) or G-protein coupled (metabotropic)

Question 31

Glutamate agonists

Answer 31

AMP, kainite, and N-methyl-D-aspartate (NMDA)

Question 32

What kind of glutamate receptors are plugged with Mg2+ until depolarization?

Answer 32

NMDA

Question 33

What is the primary inhibitory NT of the CNS?

Answer 33

GABA

Question 34

What kind of receptors are GABA receptors

Answer 34

Inhibitory, hyperpolarization. | Ion channels

Question 35

What are clinical examples of GABA receptors

Answer 35

Drugs that treat anxiety and sleep

Question 36

What are voltage gated ion channels not activated by

Answer 36

NT

Question 37

Where are voltage gated ion channels present

Answer 37

In excitable tissues (cardiac)

Question 38

What do voltage gated Na, Ca, or K channels open in response to

Answer 38

Action potentials or something that changes the voltage/membrane potential

Question 39

Receptor binding activated adenylyl cyclase which converts ATP to cAMP: cAMP activated protein kinase A

Answer 39

Gs protein

Question 40

Receptor binding inhibits adenylyl cyclase whihc prevents the conversion of ATP to cAMP and therefore the activation of protein kinase A

Answer 40

GI proteins

Question 41

Receptor binding activates phospholipase C; phospholipase C releases inositol triphosphate (IP3) and DAG from membrane phosphatidylinositol; IP3 activates Ca2+ and calmodulin-dependent proteins kinases; DAG activates proteins kinase C

Answer 41

Gq protein

Question 42

What does IP3 activate

Answer 42

Ca2+ and calmodulin dependent protein kinases

Question 43

What does DAG activate

Answer 43

Protein kinase C

Question 44

Activates Ca2+ channels, activates adenylyl cyclase

Answer 44

Gs

Question 45

Activates K+ channels, inhibits adenylyl cyclase

Answer 45

Gi

Question 46

Activates phospholipase C

Answer 46

Gq

Question 47

Examples of Gs receptors

Answer 47

``` B adrenergic (B1, B2, B3) Dopamine D1 receptors ```

Question 48

Examples of Gi receptors

Answer 48

- muscarinic M2 - dopamine D2 receptors - alpha2 adrenergic

Question 49

Examples of Gq receptors

Answer 49

A1 adrenergic Muscarinic M3 Muscarinic M1

Question 50

What are receptor tyrosine kinases activated by

Answer 50

Growth FACTORs and insulin

Question 51

What are cytokines receptors activated by

Answer 51

Growth HORMONE, erythropoietin, interferons

Question 52

How do receptor tyrosine kinases work

Answer 52

Have an extracellular ligand binding domain, a single transmembrane domain and in intracellular domain which contains the intrinsic kinase activity for signaling. After ligand binding, receptors dimerize. Phosphorylates itself from ATP, not activated

Question 53

How do cytokines receptors work

Answer 53

Similar mechanism to receptor tyrosine kinases, but kinase activity is not intrinsic but rather mediated by the JAK family of proteins. JAK activates STATs by phosphorylation

Question 54

Types of intracellular receptors

Answer 54

Steroid hormones and nitric oxide

Question 55

What do steroid hormones do

Answer 55

Stimulate transcription of genes by binding to a cytoplasmic receptor

Question 56

Steroid receptor ligand complex inside the cell

Answer 56

Transported to the nucleus where transcription is activated

Question 57

Where does nitric oxide come from

Answer 57

Endothelial cells, diffuse into smooth muscle