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Medicinal chemistry > Dugga 3- Adrenergic > Flashcards

Dugga 3- Adrenergic Flashcards

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1
Q

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

A

adrenaline and noradrenaline

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2
Q

What is noradrenaline?

A

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

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3
Q

What is adrenaline?

A

A hormone

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4
Q

Is the action of noradrenaline opposite to that of acetylcholine?

A

Yes (Tissue is under dual control)

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5
Q

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

A

No

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6
Q

What does adrenaline look like?

A

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

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7
Q

How does noradrenaline differ from adrenaline?

A

Same structure but no Me on the N

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8
Q

What kind of receptors are the adrenergic?

A

G protein coupled receptors (alpha and beta)

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9
Q

What is the major use of adrenergic agonists?

A

Asthma

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10
Q

What is the major use of adrenergic antagonists?

A

Cardiovascular

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11
Q

What are catecholamines?

A

Adrenaline, noradrenaline and dopamine

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12
Q

How are cathecholamines synthesised?

A

From tyrosine. Levodope is an intermediate

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13
Q

How are catecholamines metabolised?

A

By monoamine oxidase and cathecol-o-transferase

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14
Q

What is the main target for adrenergic drugs?

A

Adrenergic receptors

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15
Q

What are the important binding groups in catecholamine?

A

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

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16
Q

How do you make selectivity for beta receptors?

A

Placing a bulky alkyl group on the amine

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17
Q

How do you increase affinity for beta receptors?

A

extending N alkyl substituents to include hydrogen bonding group

18
Q

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

A

Replacing the phenol group with hydroxymethylene

19
Q

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

A

Increasing lipophilic character

20
Q

What are antagonists of beta adrenoceptors known as?

A

Beta blockers

21
Q

How can you change an agonist into a partial agonist?

A

Changing the catherolring to a naphtalene ring

22
Q

What is important in aryloxypropanolamines?

A

ionised amine, side chain alcohol, ether linkage

23
Q

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

A

Yes

24
Q

What does cocaine do?

A

Increases peripheral adrenergic activity by blocking noradrenaline reuptake

25
Q

What are amphetamines?

A

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

26
Q

What do monoamine oxidase inhibitors do?

A

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

27
Q

What is PNS?

A

Peripheral nervous system

28
Q

What are the important messengers in the adrenergic system?

A

The hormone adrenaline and the neurotransmitter noradrenaline

29
Q

What does noradrenaline counteract to give dual control?

A

The acetylcholine messenger

30
Q

From where is adrenaline secreted?

A

Adrenal medula gland

31
Q

Which two adrenergic receptors exist?

A

a (to G0 )
subtype a1 to ITP/DG
subtype a2 cAMP

and b (to Gs)
subtype b1 cAMP
b2 cAMP
b3 cAMP

32
Q

What does alpha and beta do in most cases?

A

Alpha contraction of smooth muscle
Beta relaxing of smooth muscle

33
Q

Does the beta adrenoreceptor have a larger hydrophobic pocket?

A

Yes

34
Q

What is the SAR for catecholamines?

A

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

35
Q

How is adrenaline metabolised?

A

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

36
Q

How do you avoid metabolism of adrenaline analogues?

A

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

37
Q

What are alpha 1 antagonists used for

A

Hypertension

38
Q

What are beta 1 antagonists used for?

A

Attenuate (reduce) heart rate

39
Q

What are beta 2 agonists used for?

A

Treating asthma

40
Q

What are the names of third generation beta blockers?

A

Epanolol
primidolol
Xamoterol

41
Q
A

Medicinal chemistry (10 decks)

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