Lec 10 Flashcards
Metabotropic receptors
Slower processes that have longer and more diverse metabolic effects
Metabotropic receptor mechanism
G-protein coupled receptor (GPCR)
Act as molecular switches
When receptor is bound to GTP, they are ‘on’
When receptor is bound to GDP, they are ‘off’
2nd messenger
Intercellular signals
1st messenger
The neurotransmitter
Why is the G-protein the lazy middle man
It acts on the effector protein which sends the second messenger to open an ion channel
How may domains do G-coupled receptors have
7 transmembrane domains (TM1-7)
Where does the G-protein generally bind to
T5-T7 region, but sometimes includes T3 and/or T4
G protein subunits
Alpha
Beta
Gamma
The receptor being off means
GDP is bound to a subunit
The receptor being on means
GDP has been exchanged with GTP
G-protein separated into alpha and beta/gamma
1st type of metabotropic receptor sequence
G-protein opens an ion channel without a 2nd messenger
1st type of metabotropic receptor sequence steps (6)
1) ACh binds to the receptor
2) GDP replaces GTP on the alpha subunit of the G-protein
3)G-protein separates into alpha and beta/gamma subunits
4)Beta/gamma subunit binds to K+ channel
5)K+ flows out of cell causing IPSPs
6)Heart rate decreases
2nd type of metabotropic receptor sequence
G-protein coupled receptor uses cyclic AMP as a second messenger
2nd type of metabotropic receptor sequence steps (7)
1) Norepinephrine binds to receptor
2)G protein “finds” an activated receptor, binds to it, and is itself activated as GDP is replaced with the GTP subunit
3)G-protein separates and the alpha-subunit activates adenylate cyclase
4) This converts ATP to cyclic AMP which activates a protein kinase A which can phosphorylate: (5, 6 or 7)
5)Membrane ion channel proteins causing them to open or close
6)Cytoplasmic proteins causing their enzymes to be activated or deactivated
7)Nuclear proteins causing gene expression
3rd type of metabotropic receptor sequence
G-protein coupled receptor uses cyclic GMP as a 2nd messenger