Dugga 3- Adrenergic

Question 1

Which chemical messengers does the adrenergic nervous system make use of?

Answer 1

adrenaline and noradrenaline

Question 2

What is noradrenaline?

Answer 2

A neurotransmitter released by sympathetic nerves which feed smooth muscle and cardiac muscle

Question 3

What is adrenaline?

Answer 3

A hormone

Question 4

Is the action of noradrenaline opposite to that of acetylcholine?

Answer 4

Yes (Tissue is under dual control)

Question 5

The adrenergic nervous system can facilitate the release of adrenaline during danger or stress, can the cholinergic do the same?

Answer 5

No

Question 6

What does adrenaline look like?

Answer 6

Aromatic ring with two OH groups and side chain with two carbons one OH group and one NMe group

Question 7

How does noradrenaline differ from adrenaline?

Answer 7

Same structure but no Me on the N

Question 8

What kind of receptors are the adrenergic?

Answer 8

G protein coupled receptors (alpha and beta)

Question 9

What is the major use of adrenergic agonists?

Answer 9

Asthma

Question 10

What is the major use of adrenergic antagonists?

Answer 10

Cardiovascular

Question 11

What are catecholamines?

Answer 11

Adrenaline, noradrenaline and dopamine

Question 12

How are cathecholamines synthesised?

Answer 12

From tyrosine. Levodope is an intermediate

Question 13

How are catecholamines metabolised?

Answer 13

By monoamine oxidase and cathecol-o-transferase

Question 14

What is the main target for adrenergic drugs?

Answer 14

Adrenergic receptors

Question 15

What are the important binding groups in catecholamine?

Answer 15

Two phenolic groups, aromatic ring, secondary alcohol and ionised amine

Question 16

How do you make selectivity for beta receptors?

Answer 16

Placing a bulky alkyl group on the amine

Question 17

How do you increase affinity for beta receptors?

Answer 17

extending N alkyl substituents to include hydrogen bonding group

Question 18

How do you avoid beta-2-agonists being metabolised by cat-o-transferase?

Answer 18

Replacing the phenol group with hydroxymethylene

Question 19

How can you make anti-asthma drugs more long lasting?

Answer 19

Increasing lipophilic character

Question 20

What are antagonists of beta adrenoceptors known as?

Answer 20

Beta blockers

Question 21

How can you change an agonist into a partial agonist?

Answer 21

Changing the catherolring to a naphtalene ring

Question 22

What is important in aryloxypropanolamines?

Answer 22

ionised amine, side chain alcohol, ether linkage

Question 23

Can the uptake and release of noradrenaline from storage vesicles be inhibited by certain drugs?

Answer 23

Yes

Question 24

What does cocaine do?

Answer 24

Increases peripheral adrenergic activity by blocking noradrenaline reuptake

Question 25

What are amphetamines?

Answer 25

They compete with noradrenaline for the transport proteins. Adrenergic activity is then increased in CNS.

Question 26

What do monoamine oxidase inhibitors do?

Answer 26

Inhibit the metabolic enzyme monoamine oxidase and result in increased levels of noradrenaline and other cathecholamines

Question 27

What is PNS?

Answer 27

Peripheral nervous system

Question 28

What are the important messengers in the adrenergic system?

Answer 28

The hormone adrenaline and the neurotransmitter noradrenaline

Question 29

What does noradrenaline counteract to give dual control?

Answer 29

The acetylcholine messenger

Question 30

From where is adrenaline secreted?

Answer 30

Adrenal medula gland

Question 31

Which two adrenergic receptors exist?

Answer 31

a (to G0 ) subtype a1 to ITP/DG subtype a2 cAMP and b (to Gs) subtype b1 cAMP b2 cAMP b3 cAMP

Question 32

What does alpha and beta do in most cases?

Answer 32

Alpha contraction of smooth muscle Beta relaxing of smooth muscle

Question 33

Does the beta adrenoreceptor have a larger hydrophobic pocket?

Answer 33

Yes

Question 34

What is the SAR for catecholamines?

Answer 34

Two OH groups on aromatic ring and one OH group on an N alkyl

Question 35

How is adrenaline metabolised?

Answer 35

With MAO oxidised to make a COOH group instead of NH2 With COMT puts a methyl on the OH group

Question 36

How do you avoid metabolism of adrenaline analogues?

Answer 36

Change OH groups on aromatic ring and add an extension on the N group

Question 37

What are alpha 1 antagonists used for

Answer 37

Hypertension

Question 38

What are beta 1 antagonists used for?

Answer 38

Attenuate (reduce) heart rate

Question 39

What are beta 2 agonists used for?

Answer 39

Treating asthma

Question 40

What are the names of third generation beta blockers?

Answer 40

Epanolol primidolol Xamoterol