Pharmacology DSA

Question 1

What does VMAT-2 do?

Answer 1

transports NE, epi, DA, and serotonin into vesicles –> release upon AP and Ca2+ influx

Question 2

What does reserpine do?

Answer 2

blocks VMAT-2 so NE, Epi, DA, and serotonin are not put into vesicles

Question 3

What does hemicholinium do?

Answer 3

blocks choline’s transport into a cell for synthesis

Question 4

What parts of epinephrine synthesis occur in the nerve cytoplasm?

Answer 4

Tyrosine –> dopa –> dopamine

Question 5

What parts of epinephrine synthesis occur in the vesicle?

What part is mainly in the adrenal medulla?

Answer 5

Dopamine –> norepinephrine –> epinephrine

norepi –> epi is in adrenal medulla

Question 6

What is the effect of alpha2 receptor stimulation?

Answer 6

decreased insulin secretion
aggregation
decreased release of NE
vascular SM contraction

Question 7

What is the effect of beta2 receptor stimulation?

Answer 7

smooth muscle relaxation

glycogenolysis, uptake of K+

Question 8

What transports tyrosine into a nerve terminal?

Answer 8

Na+ - dependent tyrosine transporter

Question 9

Where are M1 receptors located and what is their effect?

Answer 9

CNS, ganglia

Gq = activation of PLC, IP3, DAG cascade

Question 10

Where are beta3 receptors found?

what is their effect?

Answer 10

adipose tissue

lypolysis

Question 11

What does dopamine act on?

Answer 11

CNS and renal vascular smooth muscle

Question 12

What are the 2 major enzymes that metabolize catecholamines?

what is their final product that can exit the cell?

Answer 12

monoamine oxidase (MAO) and COMT

final product = VMA

Question 13

What does NET do?

Answer 13

imports NE into nerve terminal (reuptake)

Question 14

How does beta1 respond to epi and NE preferentially?

Where is it located?

Answer 14

epi = NE
juxtaglomerular cells
heart

Question 15

Where are nAChRs located?

Answer 15

CNS
autonomic ganglia
adrenal medulla

Question 16

What would low blood pressure do to a baroreceptor?

Answer 16

decrease baroreceptor stim –> decrease parasympathetic and increase sympathetic

Question 17

How does beta2 respond to epi and NE preferentially?

Where is it located?

Answer 17

epi&raquo_space;Ne
smooth muscle (vascular, bronchial, GI, GU)
skeletal muscle

Question 18

What NT is used for sweat gland stimulation?

Answer 18

ACh

Question 19

What type of gpcr is beta1?

Answer 19

Gs –> increases adenylyl cyclase, cAMP, L-type Ca2+ channel openings

Question 20

Where are M4 receptors located and what is their effect?

Answer 20

CNS

Gi = inhibit AC, decrease cAMP, activate K+ channels

Question 21

What are the main parts of the body with parasympathetic innervation?

Answer 21

cardiac and smooth muscle
gland cells
nerve terminals

Question 22

Where are muscarinic AChRs located?

Answer 22

CNS
autonomic ganglia
effector organs
sweat glands

Question 23

What is the major mechanism of terminating actions of catecholamines?

Answer 23

reuptake into nerve terminals

Question 24

What is acetylcholine mainly used in?

Answer 24

all preganglionic autonomic fibers
all pre and post ganglionic parasympathetic fibers
few postganglionic sympathetic (sweat glands)

Question 25

Where are M2 receptors located and what is their effect?

Answer 25

heart, nerves, smooth muscle | Gi = inhibit AC, decrease cAMP production, activate K+ channels

Question 26

How does alpha1 respond to epi and NE preferentially? | Where is alpha1 located?

Answer 26

``` epi greater than or equal to NE in vascular, GU SM liver intestinal smooth muscle heart ```

Question 27

What is norepinephrine used in?

Answer 27

postganglionic sympathetic fibers

Question 28

What is the effect of alpha1 receptor stimulation?

Answer 28

contraction glycogenolysis, gluconeogenesis hyperpolarization and relaxation increased contractile force, arrhythmias

Question 29

How is the adrenal gland stimulated to release epi and NE?

Answer 29

sympathetic ACh --> NAChrs --> 80% epi and 20% NE

Question 30

What is the effect of Beta1 receptor stimulation?

Answer 30

increased renin secretion | increased force and rate of contraction and AV nodal conduction velocity

Question 31

What are sympathomimetic agents?

Answer 31

drugs that mimic or enhance alpha and beta receptor stimulation

Question 32

What type of gpcr is alpha1?

Answer 32

Gq

Question 33

What type of gpcr is beta2?

Answer 33

Gs --> increases adenylyl cyclase

Question 34

Where are M3 receptors located and what is their effect?

Answer 34

glands, smooth muscle, endothelium | Gq = activation of PLC, IP3, DAG cascade

Question 35

How does alpha2 respond to epi and NE preferentially? | where is it located?

Answer 35

``` epi >/= NE pancreatic islets platelets nerve terminals vascular smooth muscle ```

Question 36

What would high blood pressure do to a baroreceptor?

Answer 36

increase baroreceptor stimulation --> increase parasympathetic NS and decrease sympathetic

Question 37

What is the sequence of events of epinephrine synthesis?

Answer 37

Tyrosine --> dopa --> dopamine --> norepinephrine --> epinephrine

Question 38

Where does epinephrine synthesis occur?

Answer 38

adrenal medulla | in a few epinephrine-containing pathways in the brain

Question 39

What are the main parts of the body with sympathetic innervation?

Answer 39

sweat glands cardiac and smooth muscle, certain gland cells renal vascular smooth muscle

Question 40

Which muscarinic receptors are Gi?

Answer 40

M2, M4

Question 41

Which muscarinic receptors are Gq?

Answer 41

M1, M3, M5

Question 42

What is the function of nAChRs?

Answer 42

excitatory | release of catecholamines (in sympathetic ns?)

Question 43

What is the function of muscarinic AChRs?

Answer 43

excitatory and inhibitory | sweat secretion

Question 44

What type of gpcr is alpha2?

Answer 44

Gi

Question 45

What does cocaine do?

Answer 45

inhibits NET so there is more NE hanging out in the synapse

Question 46

What does DAT do?

Answer 46

reuptakes DA into nerve terminal

Question 47

How does the parasympathetic NS achieve vasodilation?

Answer 47

no innervation of SM | ACh --> mAChRs on endothelial cells --> NO released --> vasodilation

Question 48

Where are M5 receptors located and what is their effect?

Answer 48

CNS | Gq = activate PLC cascade, etc

Question 49

What type of gpcr is the beta3 receptor? | How does it preferentially respond to epi and NE?

Answer 49

Gs | NE > Epi