Lec2

Question 1

chemical that affects function of living organism

Answer 1

drug

Question 2

specialized macromolc concerned in chemical signaling

Answer 2

receptor

Question 3

diff bn agonist and antagonist

Answer 3

agonist bind receptor, generate effect like endogenous ligand

antagonist (pharmacologic) bind receptor & prevent binding and effect of agonist

Question 4

most drugs were what type of molc

Answer 4

small organic

Question 5

3 large molcs

Answer 5

peptides
polypeptides
proteins

Question 6

use of nucleic acids as drugs to treat diseases

Answer 6

gene therapy

Question 7

who coined the magic bullet concept for synthesis of antibacterials (kill bacteria w/o harming body itself by hitting a specific target)

Answer 7

ehrlich

Question 8

who introduced concept of receptive substance (somethign that reacts when you introduce the drug)

Answer 8

langley

Question 9

first scientist who quantified drug-induced biological responses & thought of pharm as a chemistry

Answer 9

clark

Question 10

what are the 4 physiological receptors

Answer 10

LGIC
GPCRs
growth factor/ cytokine receptors (kinase-linked)
intracellular hormone receptors (nuclear)

Question 11

diff bn pharmacologic and physiologic antagonist

Answer 11

pharm - binds receptor, prevents binding and the effect of endogenous ligand
ex. block Na channels –> inhibit AP

physio - an agonist inhibits effect of another by interacting w receptors that make opposite effect
ex. activate Cl channels –> harder for neurons to reach threshold to get AP

Question 12

bind receptor at site other than that of endogenous ling and potentiate or inhibit the effect of the ligand

Answer 12

allosteric modulator

Question 13

physiological receptors have agonists that make what type of change

Answer 13

electrical or biochemical change aka 2ns messenger

Question 14

ligands include

Answer 14

NT
hormones
growth factors

Question 15

order the physiological receptors from fastest to slowest (include times)

Answer 15

LGIC (msec)
GPCR (sec)
kinase-linked (hours)
hormone or nuclear (hours)

Question 16

diff bn specificity and selectivity

Answer 16

specificity- ability to make effects by a single mechanism of action by intxtn w single target type

selectivity- ability to make a single effect (1 drug –> 1 effect)

Question 17

t/f a drug can be selective but not specific

Answer 17

f: a drug can be specific but not selective

bc target may be present in many tissues

Question 18

which ions have high conc inside? outside?

Answer 18

inside cell - K is high

outside cell - Na, Ca, Cl is high

Question 19

cys-loop LGIC superfam includes

Answer 19

glycine
GABAA
5-HT3
nACH (nicotinic)

Question 20

cys-loop LGIC mediate what type of chemical transmission

Answer 20

fast

Question 21

first LGIC ever identified

Answer 21

nACH

Question 22

where do nACH mediate synaptic transmission

Answer 22

at neuromuscular junctions

Question 23

what are neuronal nAChRs permable to

Answer 23

cations: na, k, ca

Question 24

what LGIC receptir desensitizes rapidly

Answer 24

5HT3

Question 25

only LGIC that doesn't have N and C term outside cell?

Answer 25

glutamate receptor | -N term outside and C term inside

Question 26

which LGIC has a reentrant loop

Answer 26

glutamate receptor (3TM)

Question 27

GPCR classification system

Answer 27

``` GRAFS glutamate rhodopsin adhesion frizzled/taste2 secretin ```

Question 28

7TM 1 structure N term out C term in

Answer 28

GPCR

Question 29

which GPCR subunit has GTPase activity (GTP --> GDP)

Answer 29

alpha

Question 30

GPCR cycle

Answer 30

1. agonist binds to 7TM receptor 2. GDP replaced by GTP --> activates G protein 3. alpha and beta-gamma dissociate --> intxt w effectors 4. agonist dissociates --> alpha cleaves GTP to GDP --> reset

Question 31

diff bn alpha s, i, and q

Answer 31

s- stimulatory and activates AC i-inhibitory q-doesnt intxt w adenylyl cyclase, instead binds and activates PLC-B

Question 32

AC converts

Answer 32

ATP to cAMP

Question 33

cAMP activates

Answer 33

PKA --> phosphorylates targets

Question 34

PLC-B does what

Answer 34

converts PIP2 --> DAG & IP3

Question 35

what does DAG and IP3 activate

Answer 35

DAG --> PKC | IP3 --> Ca channels to let Ca enter cell

Question 36

what receptors involve dimerization --> enzyme activity of receptor domains --> recruits specific domains

Answer 36

kinase linked receptors

Question 37

how is a typical cytokine receptor activated

Answer 37

``` ligand causes receptor dimerization recruit JAK STAT binds --> phosphorylated translocate to nucleus alters transcription ```

Question 38

of the physiological receptors, which one is not in the plasma membrane, but inside the cell rather

Answer 38

hormone receptors

Question 39

what do hormone receptors affect

Answer 39

gene transcription

Question 40

to ge t to hormone receptors, the structure must be

Answer 40

lipophilic (like steroids and corticoids)

Question 41

is enzyme drug effects usually inhibitory or stimulatory

Answer 41

inhibitory

Question 42

enzymes inhibitors act on what 2 categories

Answer 42

invading organisms | in the body

Question 43

penicillin is a ___ type of antibiotic

Answer 43

beta - lactam

Question 44

diff bn DAT and NET compared to SERT

Answer 44

DAT and NEt are symporters | SERT is antiporter - requires K to be brought into cell

Question 45

hwat is the mamajor mechanism for clearing transmitters from synpatic cleft

Answer 45

plasma membrane monoamine transporters

Question 46

where are the N and C terminus of transporters found

Answer 46

in cytoplasm (intracellular)

Question 47

local anesthetics block

Answer 47

Na channels

Question 48

calcium channel blockers are

Answer 48

calcium antagonists

Question 49

what do structural proteins interfere w

Answer 49

microtubule formation --> affects life of cell

Question 50

what class interferes w DNA and uses alkylization

Answer 50

nucleic acids

Question 51

what class interferes directly with signaline molcs

Answer 51

biological mediators

Question 52

incr in copy number of tarfgets gene --> incr amt expressed protein

Answer 52

gene amplification

Question 53

change in receptor number due to transcriptional or post-translational effect

Answer 53

down-regulation and up-regulation

Question 54

develops in chronic conditions where a change in drug response happens (diminished over time)

Answer 54

tolerance

Question 55

receptor effect terminates in contrinued presence of agonist (works less to prevent overstimulation) -rapid loss

Answer 55

desensitization