beta blockers Flashcards

1
Q

what is responsible for the flight or flight response?

A

adrenaline

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

what is the difference between adrenaline and no adrenaline- structurly?

A

difference of methyl group

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

what is the pre-cursor of adrenaline?

A

L-tyrosine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

what are the adrenaline endogenous agonists?

A

adrenaline, noradrenaline ad catechol ring system

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

what kind of biosynthesis does adrenaline have?

A

transferase reaction- primary to secondary reaction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

what is the sequence in the adrenaline biosynthesis?

A

l tyrosine>levodopa

>dopamine>na>ad

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

what do these beta blockers bind to?

A

B1 receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

why may there be a lysozyme attached to a b-adrenoreceptor?

A

to aid crystallisation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

what structure is a b-adrenoceptor

A

g-protein coupled receptor

7 transmembrane helix

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

what happens in the B-adrenoceptor binding site?

A

non-covalent interactions
h bond with alcohol
pi stacking with 6 transmembrane helix with benzene ring
agonsist must have pair of 204 and 207 catechol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

true or false a/b receptors floating around the body can selectively bind a over beta or b over alpha

A

true

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

what happens when you add isoprenaline?

A

makes it selective for beta

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

what is bigger alpha or beta?

A

beta

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

what is the difference between agonists and antagonists?

A

antagonists are usually bigger and work by removing the main binding groups

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

how do you improve antagonism?

A

spreading out the binding groups

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

how was the first antagonist made?

A

adding 2nd aromatic ring

17
Q

what the problem with first generation drugs crossing the BBB

A

cause reactions in people with asthma

want to agonise b2 receptor but first gen antagonises it

18
Q

how did we get rid of the problem with asthma and first gen bb?

A

2nd gen- higher affinity H bonding- B1 selective- due to lack of bonding at B2- no side effects and also via para-aromatic substituent

19
Q

what are 3rd gen bb?

A

extra lipophilic interactions- extra H bonding

20
Q

what are BB’s?

A

they are antagonists of B-adrenoceptors

21
Q

what reduces agonism?

A

replacing catechol unit with naphthalene