Phase One: Week Eight Flashcards
Explain the mechanism of GABA-A receptor
GABA is a main inhibitory neurotransmitter of the CNS. It binds to a ligand-gated chloride channel on the post-synaptic nerve cell. Chlorine will flow into the cell and cause hyperpolarisation and this inhibits action potential formation.
What is Myasthenia Gravis?
This is muslce weakness. This is an autoimmune antibody attach of Ach receptor at the neuromuscular junction.
What kind receptors do adrenaline and serotonin bind to?
G-protein coupled
What are the three main G-alpha effectors?
Adenylyl cyclase, Phospholipase C and RhoGEFS
What does adenylyl cyclase make?
cAMP
What does phospholipase make?
IP3 and DAG
Explain the process of protein kinase A activation
This is activated by cAMP. cAMP will bind to the two regulatory units of the PKA and this causes the catalytic subunits to become activated and dissociate.
What is the affect of phospholipase C activation?
IP3 will be activated and this will cause calcium release into the endoplasmic reticulum. This will then activate calcium-depending kinases. DAG activates protien kinase C.
Explain the process of adrenaline binding to a beta-one receptor
Adrenaline will bind and activate G-alpha and this will stimulate adenylyl cyclase. There will be an increase in cAMP. As beta-one receptors are located on heart muslce, their activation will cause increases heart rate and contraction.
What is an example of selective beta-blockers (ones that only block beta-one)?
Atenolol
Explain the process of adrenaline binding to a beta-two receptor
Adrenalin will bind and will activate G-alpha subunit. Adenylyl cyclase will be activated and this will increase cAMP. Due to their location being on the airway smooth muscle and vascualr smooth muscle, the effect is bronchodilation and vasodilation. This will cause increased blood supply to the muslce.
What is sublingual administration?
Under the tongue
What is topical administration?
Mucous membranes
What is drug bioavailability?
The fraction of drug that reaches the systemic blood
What is drug bioavailability?
This is the fraction of administered drug that reaches the systemic circulation.