Tissues 9 Flashcards
How do Ionotropic receptors work?
- Ligand binds to receptor protein
- Channel protein changes conformation - opens pore
- Allows ions to move freely - depending on concentration gradients.
Give 2 examples of ionotropic receptors.
- Nicotinic Acetylcholine receptors.
2. GABA receptors
What physiological effect does GABA have?
Depression of activity (influx of Cl).
Blocking GABA receptors gives hyperexcitability of CNS
Explain how G-protein coupled receptors work.
- “G protein” initially not linked to the G-protein receptor (receptor aka known as 7-TM receptor)
- Ligand binds to receptor and changes its conformation
- Stimulates G-protein to bind to associate with G-protein receptor
- GDP exchanged for GTP.
- G-protein dissociates into 2 active components.
- Alpha subunit
- By subunit
- Each subunit binds to its target protein.
- Once alpha subunit binds to target protein, internal GTP-ase activity causes GTP to change to GDP.
- Alpha subunit unbinds from target protein. Heterotrimer with GDP reforms.
G proteins are called heterotrimers. What is the meaning of this.
Alpha, beta and gamma subunits.
Beta and Gamma don’t dissociate in G protein
G(s) Protein Linked Receptor. What does it do.
- Stimulates Adenylyl Cyclase.
- Adenyl cyclase converts ATP to cAMP.
- cAMP increases Protein Kinase A (PKA) levels
Give an example of Gs Protein linked receptor
Beta1-adrenergic receptor
beta-blockers act on this receptor
G(i) Protein Linked Receptor. What does it do.
- Inhibits Adenyl cyclase.
2. Reduces levels of cAMP and PKA.
Give an example of Gi protein linked receptor.
M2 - Muscarinic receptor
What does the G(q) protein linked receptor do?
- Stimulates Phospholipase C (PLC)
- PLC converts PIP2 to IP3 and DAG
- IP3 causes an increase in intracellular Ca
- DAG activates PKC
What are G(s), G(i) and G(q)?
All types of G(a) subunits.
What is the effect of the G(q) receptor?
Works on the AT-1 angiotensin receptor. Effect is vasoconstrictor
What is the most potent vasoconstrictor in the body?
Angiotensin
Explain how enzyme linked receptors work.
- Ligand binding causes receptors to cluster.
- Receptor clustering activates enzymes within cytoplasm.
- Enzymes phosphorylate receptor.
- Phosphorylation causes signalling proteins to bind to the cytoplasmic domain.
- Signalling proteins recruit other signalling proteins and signal generated.
What are the majority of enzyme linked receptors related to?
Tyrosine Kinase Enzymes