Pharmacology

Front 1

What are the chromosomal abnormalities associated with the philadelphia chromosome? and what does it cause?

Back 1

Chr. 9 & 22
chronic myeloid leukemia

Front 2

How do you treat CML?

Back 2

interferon

Front 3

What does imatinib do?

Back 3

inhibitor of the BCR-Abl tyrosine kinase encoded by the philadelphia chromosome. Receptor assumes inactive conformation --> inactivation of kinase

Front 4

Where does warfarin act?

Back 4

the S enantiomer is 4x more potent than the R. Interacts with vitamin K epoxide reductase.

Front 5

Describe induced fit

Back 5

binding of a drug to its receptor changes its conformation

Front 6

Describe the structure of nACHR

Back 6

5 subunits
two alpha subunits that allow for ACh binding

Front 7

What do local anesthetics do?

Back 7

block the conductance of Na ions in neurons that transmit pain info

Front 8

What do benzodiazepines do?

Back 8

bind to GABA_A receptors and increase the conductance of Cl ions --> hyperpolarization

Front 9

Describe the structure of a G-protein coupled receptor

Back 9

7-transmembrane regions
1 polypeptide chain
each transmembrane region has a single alpha heli.

Front 10

How does the G-protien coupled receptor look during the resting state? (on the cytoplasmic side of things)

Back 10

noncovalently linked to a G protein made of alpha and beta-gamma subunits

Front 11

Describe G protein dissciation

Back 11

alpha subunit switches GDP for GTP.
a-GTP dissociates from the betagamma subunit
- a, or bg diffuse along the inner leaflet of the plasma membrane to interact with different effectors

Front 12

How does the signaling stop?

Back 12

inherent GTPase activity of the alpha subunit causes hydorlysis of GTP to GDP

Front 13

What does G_s do?

Back 13

- activates adenylyl cyclase
- activates Ca2+ channels

Front 14

What does G_i do?

Back 14

- inhibits adenylyl cyclase
- activates K+ channels

Front 15

What does G_q do?

Back 15

- activates phospholipase C

Front 16

WHat does G_o do?

Back 16

Inhibits Ca2+ channels (opposite of G_s)

Front 17

B_1 adrenergic receptors

Back 17

Control RH

Front 18

B_2 adrenergic receptors

Back 18

relax smooth muscle

Front 19

B_3 adrenergic receptors

Back 19

mobilize energy by fat cells

Front 20

Where does the B1 receptor act?

Back 20

1. SA node
2. Cardiac muscle
3. Adipose tissue

Front 21

Where does the B2 receptor act?

Back 21

1. bronchial and smooth m
2. GI smooth m
3. Uterus
4. Bladder
5. Liver
6. Pancreas

Front 22

Where does the B3 receptor act?

Back 22

Adipose tissue

Front 23

What do tyrosine kinase receptors do?

Back 23

phosphorylate tyrosine residues on the cytoplasmic tail of the receptor
--> recruits and tyrosine phosphoryltation of amny cytosolic signaling molecules

Front 24

Name a famous tyrosine kinase receptor

Back 24

Insulin

Front 25

Where does insulin bind?

Back 25

to the alpha subunits

Front 26

What happens once the beta subunits in the insulin receptor transphosphorylate?

Back 26

insulin receptor substrate (IRS) proteins are recruited

Front 27

What are some main roles of tyrosine kinase receptors?

Back 27

growth and differentiation

Front 28

Describe tyrosine kinase-associated receptors

Back 28

like tyrosine-kinase receptors, except they rely on nonreceptor kinases to phosphorylate target proteins

Front 29

To what family to receptor serine/threonin kinases belong to?

Back 29

TGF-beta receptor superfamily

Front 30

Why ar eserine/threonin kinase receptors important

Back 30

regulated cell grown and differentiation
- implicated in cancer progression

Front 31

Describe Receptor Gyanylyl cyclases

Back 31

have no G proteins. Ligand binding stimulates intrinsic receptor guanylyl cyclase activity
GTP --> cGMP

Front 32

Name an important member of the receptor Guanylyl cyclase family

Back 32

B-type natriuretic peptide
(secreted by ventricles in response to volume overload)

Front 33

How do antimitotic vinca alkaloids act?

Back 33

Diffuse through cellular membrane and target tubulin monomers to prevent polymerization
Arrests cells in metaphase

Front 34

Define tachyphylaxis

Back 34

drugs show diminishing effects over time
(receptor and cell become desensitized to drug)`

Front 35

Define homologous desensitization

Back 35

actions of agonists at only one class of receptors are lessened

Front 36

Define heterologous desensitization

Back 36

effects of agonists on a number of classes of receptors are coordinately diminished

Front 37

how do you get heterologous desensitization?

Back 37

drug-induced alteration in a common point of convergence in the mechanisms of action of the involved receptors
(e.g. a shared effector molecule)

Front 38

How do you get receptor inactivation?

Back 38

phosphorylation of the receptor completely blocks the signaling activity of the receptor

Front 39

Define receptor downregulation

Back 39

continual stimulation cuases endocytosis and sequestration of receptors.

Front 40

Name one 'drug' that does not act with one of the four basic receptor types

Back 40

mannitol. directly changes the osmolarity of the nephron

Front 41

give a nother 'drug' that is unique

Back 41

antacids. neutralize stomach pH

Front 42

What does pravastatin do?

Back 42

reduces cholesterol levels

Front 43

Define K_d in terms of ligand concentration

Back 43

the concentration of ligand at which 50% of all the available receptors are bound

Front 44

What is a graded dose response relationship?

Back 44

describes the effect of variosu doses of a drug on an individual

Front 45

What is a quantal dose response relationship?

Back 45

describes the effect of various doses of a drug on a population of individuals