Neuropharm Exam #1

Front 1

Draw a graph that shows Kd and Bmax. Label both. Then draw a Scatchard plot and label both axes once again.

Front 2

Distinguish between fluoxetine and furosemide and tells how each differs. Why does it take longer for fluoxetine to "kick in"?

Back 2

Fluoxetine- antidepressant that binds to and inhibits serotonintransporters. while furosemide- a diuretic that binds to Cl- channels in theascending loop of Henle in the nephrons of the kidney. Furosemide causesmore Cl- to remain in the lumen of the nephron tubule, which in turn requiresmore H2O to remain in the tubule. The same effect is exerted on allnephrons in the kidney and the increase in H20 within each individual kidneycauses diuresis. Dieuresis occurs as soon as effective drugconcentrations reach the kidney's extracellular fluid. Drugs in the nervous system only work on a subset of neurons (100,000 out of 100 billion). Inhibits serotonin re uptake, thus causing seritonergic transmission, but which of the 14 known serotonin receptors must be activated to get the correct antidepressant response. N']H

Front 3

What are the criteria for the production of good ligands in the lab?

Back 3

1.) specific, stereoselective, steady state can be achieved.

-The amount of ligand that binds receptors is dependent on the concentration of the ligand.

Front 4

Define specific binding

Back 4

The fraction of total binding that may be displaced by incubating the radiolabeled ligand tissue with a large excess of unlabeled ligand ---> theoretically saturable and fully reversible.

Front 5

Define dissociation constant (Kd)

Back 5

Concentration of ligand at which half of thespecific binding sites are occupied. Large Kd values reflect lower affinities of the drug or ligand for thereceptor.

Front 6

Define Bmax

Back 6

Bmax ( the total amount of binding)- Thehighest drug concentration that can be bound.

Front 7

Define Ki

Back 7

A measure of the affinity of the drug for thebinding site in the context of the specific radioligand. The point atwhich half of the radioligand is displaced by the drug.