Flashcards in Lecture 4/5 - Pharmacodynamics Deck (65)
What is different about how corticosteroids interact with the cell?
Act on nuclear receptors, altering genes expressed. this causes its effects to be expressed for several weeks even with the drugs gone
What is an electrostatic interaction?
Attraction between functional groups w/ opposite charges
Can be either strong or weak depending on the charge strength
Describe hydrogen bonds.
Hydrogen covalently bonded to an electronegative atom
What tends to act on intracellular receptors?
Hormone/drug crosses plasma membrane
What is commonly the effect of intracellular receptor activation?
As a complex, stimulates gene transcription OR removes an inhibtion
What is the typical characteristics of intracellular receptor reaction time?
Normally has a lag period but will persist over time
What five examples given in lecture activate intracellular receptors?
What is the structure of a transmembrane protein?
Polypeptides w/ extracellular hormone binding domain + cytoplasmic enzyme domain
What are the three kinds of enzymes involved with the transmembrane proteins?
Tyrosine kinase + Serine kinase + Guanylyl cyclase
What happens to the transmembrane protein receptors once stimulated?
They are down regulated
What are three examples given in lecture of protein tyrosine kinase receptors?
Insulin + Epidermal GF + PDGF
Describe ligand-gated channels.
Receptor is linked to an ion channel, when ligand binds channel is opened and ions rush in or out of the cell
What ion is paired with acetylcholine/nicotinic receptors?
What ion is paired with GABA receptors?
What ion is paired with benzodiazepine receptors?
What ion is paired with the glutamate receptor?
Ca or Na
Describe a G-protein coupled receptor.
Coupled with G-protein to intracellular second messengers, spans the whole membrane
What do G proteins interact with?
GTP, stimulate binding + hydrolysis = GDP
What do Gs receptors do?
Stimulation the formation of cAMP
What do Gi receptors do?
Inhibit the formation of cAMP
What does cAMP do if it is activated?
PDE breaks down cAMP
cAMP also binds to intracellular protein kinases = phosphorylation of PKA + CREB
What is a major Gs receptor?
What is a major Gi receptor?
What compounds stimulate Gs?
EPI - NE - Isoproterenol - Dobutamine - Histamine - FSH - ACTH
What compounds stimulate Gi?
NE - EPI - Dexmedetomidine - Acetylcholine - Morphine - Serotonin
What does Gq activate?
What does PLC do?
Hyrolyze PIP2 into
What does IP3 do?
release calcium stores
What does DAG do?