beta blockers Flashcards
what is responsible for the flight or flight response?
adrenaline
what is the difference between adrenaline and no adrenaline- structurly?
difference of methyl group
what is the pre-cursor of adrenaline?
L-tyrosine
what are the adrenaline endogenous agonists?
adrenaline, noradrenaline ad catechol ring system
what kind of biosynthesis does adrenaline have?
transferase reaction- primary to secondary reaction
what is the sequence in the adrenaline biosynthesis?
l tyrosine>levodopa
>dopamine>na>ad
what do these beta blockers bind to?
B1 receptors
why may there be a lysozyme attached to a b-adrenoreceptor?
to aid crystallisation
what structure is a b-adrenoceptor
g-protein coupled receptor
7 transmembrane helix
what happens in the B-adrenoceptor binding site?
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
true or false a/b receptors floating around the body can selectively bind a over beta or b over alpha
true
what happens when you add isoprenaline?
makes it selective for beta
what is bigger alpha or beta?
beta
what is the difference between agonists and antagonists?
antagonists are usually bigger and work by removing the main binding groups
how do you improve antagonism?
spreading out the binding groups
how was the first antagonist made?
adding 2nd aromatic ring
what the problem with first generation drugs crossing the BBB
cause reactions in people with asthma
want to agonise b2 receptor but first gen antagonises it
how did we get rid of the problem with asthma and first gen bb?
2nd gen- higher affinity H bonding- B1 selective- due to lack of bonding at B2- no side effects and also via para-aromatic substituent
what are 3rd gen bb?
extra lipophilic interactions- extra H bonding
what are BB’s?
they are antagonists of B-adrenoceptors
what reduces agonism?
replacing catechol unit with naphthalene
