lecture 1 to 8 Flashcards
(23 cards)
pharmacology
the study of how drugs affect the body and how the body affects drugs
what was the worlds first synthetic drug
salvarsan
three routes to create drugs
folk medicine ie the nautral product eg aspirin and cocaine
serendipity eg penicillin
synthetic chnemistry eg procian and salvarsan
pharmacodynamics
mechanism of drug action
pharamacokinetics
handling of the drug by the body
intracellular drug targets
nuclear hormone recptors and enzymes
extracellular drug targets
voltage gated ion channel tyrosine kinase repctor transporter enzyme ligand gated ion channel and g coupled protein repcptor
what are ligand gated channels named after
their activating ligand, not the ubstance they transport eg GABA a
pharmacognosy
study of drugs from nautral sources
ligand gated ion channels exaples
gaba type a receptor
nicotinic acetylcholine recptor
glycine recptor
ionotrpic glycine recptor
ligand gated channel strcutre
pentamer- five subunits 2 alpha 1 beta one delta and one epsilon
2 binding sites for acetylcholine
each subunit has 4 transmembrane domains, the second tmd forms the linning of the ion channel, contains hydrophilic amino acids
agonist bindig site located in large loop between TM3 and TM4
`strcutre of voltage gagted channel
larger alpha subunit and smmller beta subunit
aphasubunit has for pseudosubunits each containing 6 transmembrane domains
membrane dippin gdomians between tm5 and tm6 form lining of channel
tm4 is the voltage ensor
GPCRs
seven transmembrane domains
most diverse
muscarinic receptors
adrenergic receptors
affinity
how tightly something binds
kd
used to emasure affinity
is the dissociation constant , the concentration of drug that gives 50% the maximum occupancy
the higher the kd
rhe lower the affinity
ec50
conc of drug giving 50% of the maximal effect
pitency
the conc of drug required to give certain resonse
competitive antagonisjm
surmountable
parallel curve to the right with no change in maximum response
reversible
ic50
concentration of antagonist fiving 50% of the control response
changes with agonist concentration
selectivity
is the rekative potency or sffinity at one receptor compared with another
non competivie
reduces maximum effect]is unsurmoutable
uncompetitive
use dependent