L6 Drug-Receptors Flashcards
are drug receptors interactions due to a single interaction or many of them?
combination od binding interactions - the sum of weak forces may create strong interaction (high affinity)
what is a “dirty” drug?
when it binds to receptors that it wasn’t meant to bind to - causes side effects!
what is drug selectivity?
- more selective = better (less side effects)
- cell type specificity of receptors - receptors only found on few cell types
- cell type specificity of receptor-effector coupling - diverse responses between cells
what does an ion channel have
- Both a channel and a receptor combined!
- Subunit site for nicotine – high affinity!
- Endogenous ligand of nicotinic receptor = aCh
- Responsible for neurotransmission signaling that takes place in ganglion
- Needs 2 ligands to occupy binding sites to have open
- Cation pore monovalent (Na+ or K+)
whats an example of an ion channel?
nicotinic receptor
what does a G protein coupled receptor have?
- Have extracellular motif
- 7 transmembrane regions
- binding site for G proteins
whats an example of a G protein coupled receptor?
muscarinic etc.
what does enzymatic cytosolic domains have
- receptor + enzymatic kinase
* phosphorylation
what is an example of enzymatic cytosolic domain receptors?
insulin receptor
what do intracellular receptors have?
- contributes to gene expression
* passes right through
what is an example of an intracelluar receptor?
glucocorticoid receptor
what does Gs activate?
alpha subunit – activate AC – increase cAMP
what does beta gamma do?
controls heart K+ channel activity
what does cAMP activate?
PKA – phosphorylation
what does alpha i do?
inhibitory – depressed cAMP and depress systems that are tonically active
