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pharm > Lec2 > Flashcards

Lec2 Flashcards

1
Q

chemical that affects function of living organism

A

drug

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2
Q

specialized macromolc concerned in chemical signaling

A

receptor

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3
Q

diff bn agonist and antagonist

A

agonist bind receptor, generate effect like endogenous ligand

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

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4
Q

most drugs were what type of molc

A

small organic

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5
Q

3 large molcs

A

peptides
polypeptides
proteins

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6
Q

use of nucleic acids as drugs to treat diseases

A

gene therapy

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7
Q

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

A

ehrlich

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8
Q

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

A

langley

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9
Q

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

A

clark

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10
Q

what are the 4 physiological receptors

A

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

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11
Q

diff bn pharmacologic and physiologic antagonist

A

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

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12
Q

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

A

allosteric modulator

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13
Q

physiological receptors have agonists that make what type of change

A

electrical or biochemical change aka 2ns messenger

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14
Q

ligands include

A

NT
hormones
growth factors

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15
Q

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

A

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

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16
Q

diff bn specificity and selectivity

A

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)

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17
Q

t/f a drug can be selective but not specific

A

f: a drug can be specific but not selective

bc target may be present in many tissues

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18
Q

which ions have high conc inside? outside?

A

inside cell - K is high

outside cell - Na, Ca, Cl is high

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19
Q

cys-loop LGIC superfam includes

A

glycine
GABAA
5-HT3
nACH (nicotinic)

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20
Q

cys-loop LGIC mediate what type of chemical transmission

A

fast

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21
Q

first LGIC ever identified

A

nACH

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22
Q

where do nACH mediate synaptic transmission

A

at neuromuscular junctions

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23
Q

what are neuronal nAChRs permable to

A

cations: na, k, ca

24
Q

what LGIC receptir desensitizes rapidly

A

5HT3

25
Q

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

A

glutamate receptor

-N term outside and C term inside

26
Q

which LGIC has a reentrant loop

A

glutamate receptor (3TM)

27
Q

GPCR classification system

A 
GRAFS
glutamate
rhodopsin
adhesion
frizzled/taste2
secretin
28
Q

7TM
1 structure
N term out
C term in

A

GPCR

29
Q

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

A

alpha

30
Q

GPCR cycle

A
  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
31
Q

diff bn alpha s, i, and q

A

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

32
Q

AC converts

A

ATP to cAMP

33
Q

cAMP activates

A

PKA –> phosphorylates targets

34
Q

PLC-B does what

A

converts PIP2 –> DAG & IP3

35
Q

what does DAG and IP3 activate

A

DAG –> PKC

IP3 –> Ca channels to let Ca enter cell

36
Q

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

A

kinase linked receptors

37
Q

how is a typical cytokine receptor activated

A 
ligand causes receptor dimerization 
recruit JAK
STAT binds --> phosphorylated 
translocate to nucleus 
alters transcription
38
Q

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

A

hormone receptors

39
Q

what do hormone receptors affect

A

gene transcription

40
Q

to ge t to hormone receptors, the structure must be

A

lipophilic (like steroids and corticoids)

41
Q

is enzyme drug effects usually inhibitory or stimulatory

A

inhibitory

42
Q

enzymes inhibitors act on what 2 categories

A

invading organisms

in the body

43
Q

penicillin is a ___ type of antibiotic

A

beta - lactam

44
Q

diff bn DAT and NET compared to SERT

A

DAT and NEt are symporters

SERT is antiporter - requires K to be brought into cell

45
Q

hwat is the mamajor mechanism for clearing transmitters from synpatic cleft

A

plasma membrane monoamine transporters

46
Q

where are the N and C terminus of transporters found

A

in cytoplasm (intracellular)

47
Q

local anesthetics block

A

Na channels

48
Q

calcium channel blockers are

A

calcium antagonists

49
Q

what do structural proteins interfere w

A

microtubule formation –> affects life of cell

50
Q

what class interferes w DNA and uses alkylization

A

nucleic acids

51
Q

what class interferes directly with signaline molcs

A

biological mediators

52
Q

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

A

gene amplification

53
Q

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

A

down-regulation and up-regulation

54
Q

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

A

tolerance

55
Q

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

A

desensitization

pharm (6 decks)

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