Medicines for Cardiovascular Disease Flashcards
What is intramolecular bonding
bonding within the same molecule including covalent bonding
what is intermolecular bonding
bonding between two neighbouring molecules non covalent
what type of bonding is involved in drug binding interaction
intermolecular
what are the main types of intermolecular bonding
Electrostatic Hydrogen bonding Van der waals Dipole - Dipole & ion dipole Repuslion forces Pi stacking
what is the lock and key hypothesis
rigid structure and the substrate + active site of enzyme are complementary in shape however does not explain multiple substrates
what is the induced fit model
substrate and enzyme NOT complementary but similar in shape, as the substrate makes contact with the active site it undergoes a conformational change to become complementary to the substrate.
This change is driven by maximisation of intermolecular binding. Binding interaction must be strong enough to hold substrate but must allow release of products or neurotransmitter.
what are the main structural requirements for selective binding ot the alpha 1 subunit of L type calcium channel for amlodipine
chloro group on the aromatic ring lock the ring perpendicular to dihydropyridine
worth noting that the terminal amino group is important for formulation and ionic interaction in membranes
protonation at physiological pH allows formulation as the maleate salt
what do agonists do
mimic the natural messenger and need to bind to the receptor in such a way to activate it.
when making an agonist what do we need to consider
drug must have correct binding groups
binding groups must be in the correct position
drug must be correct size for binding site
why would we give a patient salbutamol to alieve the symptom of bronchospasm due to an overdose of atenolol
atentolol is a adrenergic receptor antagonist whilst salbutamol is a beta 2 receptor agonist.
bronchospasm due to excessive action from atenolol on beta 1 and 2 receptors, adding an agonist will return normal levels of activity
why is atenolol an antagonist and salbutomal an agonist for the same receptor
agonists are smaller maximizing induced fit.
Similar placement of h bonding group but have same binding interactions but means that these are in a slightly different position for atenolol reducing induced fit
tert butyl group on salbutamol could be advantageous