3 L1 GPCRs Flashcards
Compare GPCR v Ion channel activation
Both- Binding of agonist causes conformational change in receptor protein
Ion- Conformational change opens gate for ion flow
GPCR- More stuff happens
Describe GPCR activation
Following conformational change, GTP replaces GDP on alpha subunit - GTP bound alpha subunit breaks off from receptor complex - GTP bound alpha subunit interacts with target protein to modify cell signalling
G protein subunits and subtypes
Subunits- a, B, y
a subtypes- i, s, q
Describe the roles of IP3 and DAG
IP3 increases free Ca from ER
DAG activates PKC (protein kinase C)
Describe Gs proteins
D1 type receptors - Activates adenyl cyclase - Amplifies cAMP - Activates PKA - Activates Na channels
Describe Gi proteins
D2 type receptors - Deactivates adenyl cyclase - Decreases cAMP - Activates AK channels (GIRK) - Closes Ca channels
AMPA and GABA
AMPA- Na ion channel that causes neurons to fire
GABA- Cl ion channel that stops neurons from firing
What does GIRK do
GIRK pushes K out of the postsynaptic neuron making MP more negative- neuron does not fire
3 receptors that are coupled to Gq proteins
Serotonin - Muscarinic - Alpha1 (noradrenaline)
Where are M3 (Muscarinic type 3) found
Intestinal smooth muscle cells
Describe M3 (Muscarinic type 3) pathway
Ach activates M3 receptors to activate PLC - Produces IP3 - Releases Ca from SR - Ca binds to calmodulin - Calmodulin activates myosin light chain kinase - Phosphorylation of myosin light chains and muscle contraction