19 - Pharmacology Flashcards
Examples of non-receptor targets of drugs
✦ Ion channels e.g. Ca2+ channels
✦ Enzymes e.g. cyclo-oxygenase
✦ Carrier molecules e.g. serotonin uptake
✦ DNA
Receptor definition
A receptor is a biological macromolecule or complex
that binds another molecule and initiates or modulates
signalling or effector activity within a cell.
Difference between agonist and antagonist
A ligand that binds to a receptor and activates it is an
agonist. A ligand that binds to a receptor without
activating it will act as an antagonist.
Beta-adrenoceptor
1)
2)
3)
1) GPCR
2) Responsive to adrenaline, noradrenaline
3) Stimulatory in some tissues (cardiac), inhibitory in others (bronchial muscle)
Artificial selective beta-adrenoceptor agonist
Isoprenaline
Artificial selective beta adrenoceptor antagonist
Propanolol
Timescale of ligand-gated ion channels
Miliseconds
Example of a ligand-gated ion channel
Nicotinic ACh receptor (Na+ channel)
Timescale of GPCR
Seconds
Example of a GPCR
Muscarinic ACh receptor
Kinase-linked receptors common substrates
Serine, tyrosine
Kinase-linked receptor timescale
Hours
Example of kinase-linked receptor
Cytokine receptors
Nuclear receptor timescale
Hours
Example of GPCR that isn’t on cell surface
Rhodopsin