beta blockers Flashcards

1
Q

what is responsible for the flight or flight response?

A

adrenaline

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2
Q

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

A

difference of methyl group

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3
Q

what is the pre-cursor of adrenaline?

A

L-tyrosine

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4
Q

what are the adrenaline endogenous agonists?

A

adrenaline, noradrenaline ad catechol ring system

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5
Q

what kind of biosynthesis does adrenaline have?

A

transferase reaction- primary to secondary reaction

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6
Q

what is the sequence in the adrenaline biosynthesis?

A

l tyrosine>levodopa

>dopamine>na>ad

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7
Q

what are the recognition motifs of beta blockers

A

TM6 - asparagine residue (OH + Phe pi-stacking)
TM5 - 2 serine residues (phenol OH’s)
TM3 - aspartate residues (amine)

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8
Q

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

A

to aid crystallisation

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9
Q

what structure is a b-adrenoceptor

A

g-protein coupled receptor

7 transmembrane helix

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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

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11
Q

How were 3rd generation BB made and examples

A

By adding chain extensions. Ex. Epanolol, Primidilol, Xamoterol

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12
Q

what happens when you add isoprenaline?

A

makes it selective for beta

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13
Q

what has a bigger hydrophobic pocket, alpha or beta?

A

beta

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14
Q

what is the difference between agonists and antagonists?

A

Agonists bind to receptors causing physiologocial effects. Antagonists are usually more spread out and work by removing the main binding groups

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15
Q

how do you improve antagonism?

A

spreading out the binding groups

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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 CNS kike dizziness and sedation. Caused bronchoconstriction in people with asthma

18
Q

Making gen 2 BB

how did we get selectivity between beta 1 and beta 2 receptors

A
  • Increase polarity so it cant pass BBB by adding functional groups
  • extra H-bonding interactions and para substitutions instead if meta
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