Midterm Flashcards
Furosemide: What is the target?
Na+/K+/2Cl- transporter
Diuretic, makes urine less concentrated
Fluoxetine: What is the target?
SSRI - Prozac
B1-adrenergic antagonists targets ______.
CVD
B2-adrenergic antagonist treats _______.
Asthma
5-HT10 agonist treats _______.
Migraines
NO increases the level of _______
CGMP ( leading to + PKG then contraction)
Sildenafil blocks ______ to stop the break down of ______
PDE5; cGMP
Blocking prostaglandin results in reduced ________.
Inflammation
Bioavailability describes ___
The amount passing BBB vs absorption by the gut
A smaller Kd (dissociation rate) means a better ____.
Affinity
What are scatchard plots used for?
Used to calculate affinity constant of a ligand
Drug efficacy describes
Whether a drug produces more or less effect for a specific dose
What is drug potency?
The dose required to reach a certain efficacy, more potent means you need less dose to reach an effect
What is the effect of an inverse agonist?
Ligand produces opposing effect
What is autologous in stem cell therapy?
Cells come from the self
What is allogenic in stem cell therapy?
Cells com from a donor
What is the resting potential of cardiac vs neuronal cells?
-90 mv vs. -70 mv
How does selectivity filter of K+ channel work?
Involved C=O carbonyl oxygen of AA @ the pore loop interacting with K+ ion and stabilizing it
What is the function of TTX?
Binds to VGSCs, at site 1, BLOCKS pore loop
What is the mechanism of scorpion alpha toxin?
Activation resulting in continuous firing and convulsions
What is the function of lidocaine
Binds to inactivated state of Na+ channel to slow down heart rate
What is the function of procaine?
Slows down depolarization of nerve cell membrane
How do the drugs phenytoin and carbamazepine work for epilepsy?
Slows down the recovery from inactivated state, preventing the next AP
What is TEA used for and how does it work
Probe brain function to study APs. Affects the 2 TM K+ inward rectifier and ATP- activated K+ channel
What receptor does Digoxin and Ouabain affect?
Blocks Na+/K+ pump, inhibits restoration of eq after APs
What are three ways to deliver drugs into the CNS?
- hydrophilic drug enter freely
- lipophilic drugs require pro-drug conjugation
- drug-Ab fusion
What is the function of forskolin
Used to increase cAMP by stimulating AC, used for a variety of purposes, for ex: weight loss
Why are HDAC inhibitors used for cancer therapy?
Inhibits histone deacetylase, inhibits proliferation of tumor cells
What are the 5 ways for termination of NTs?
- uptake by postsynaptic cell
- transport to presynaptic cell
3 uptake by glia - enzyme degradation
- passive diffusion
The 3 steps to exocytotic cycle are ____
- synaptic vesicle approaches active zone
- ATP-dependent priming
- NT release triggered by Ca2+ influx
What is the function of synaptotagmin?
Ca2+ sensor
What is the function of synaptobrevin?
vesicle fusion and targeting
What is the effect of a synaptobrevin antagonist?
prevents NT release by stopping the vesicle’s ability to target the membrane and fuse
What are the two transmembrane SNARE proteins
SNAP-25 and syntaxin
What is the role of SNAP-25 and syntaxin?
stabilizes vesicle at the membrane
What is an example of direct signal transmission
ligand gated ion channel
What is an example of indirect signal transmission
G protein, steroid receptors
Where in the intestine does cholera toxin target?
enterocytes
