Pharmacology 1&2 Flashcards
Name some examples of a response that can be evoked from a receptor
Signal transduction Contractile activity Rate of proliferation Secretory activity Metabolism Membrane permeability
Intracellular receptors
Steroid hormones are lipophobic
Diffuse into cell and effect transcription
NO diffuse into neighbouring cells and target guanylyl cyclase to make cGMP
Ionotrophic
Receptor also an ion channel
Fast EPSP and IPSP
Receptor alters enzyme activity
JAK kinase - enzyme separate
G protein
3 subunits and alpha goes off to regulate activity of other enzyme
Adenylyl cyclase
cAMP==> PKA
What does the transmitter and second messenger regulate?
Glucose across membrane calcium voltage channels Protein synthesis Glycogen and lipid breakdown Microtubule secretion
2nd messengers
Intracellular signalling molecules released by cell to trigger changes eg proliferation
PLC
2 secondary messengers - DAG and IP3
- PKC and calcium
Calcium sources
IP3 release from ER
Gated channel
Inhibit calcium transport out of cell
Effects of calcium
Target protein
Bind to calmodulin then activate protein
Calcium binding protein eg troponin
Drug
Any chemical agent that affects a biological system
Affinity
Determined by strength of chemical reaction between drug and receptor - low EC50 = high affinity
EC50
Effective concentration of drug at 50% maximal response
Efficacy
Determined by how good a drug is at activating receptor