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Pharmacology 2100 > DRug receptors > Flashcards

DRug receptors Flashcards

(58 cards)

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1
Q

what is pharmacodynamic

A

what the drug does to the body

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2
Q

what is pharmacokinetics

A

what the body does to the drug

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3
Q

what is a ligand

A

substance that forms complex with receptors ex.drugs

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4
Q

what is a receptor

A

proteins that can bind to ligands

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5
Q

where can receptors be located

A

cell membrane
cytoplasm
nucleus

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6
Q

what does the receptor binding to the ligand do to post receptor signalling

A

activates or inactivates

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7
Q

what are the four receptor families

A

g protein coupled receptors
ion channels
enzyme linked receptors
intracellular receptors

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8
Q

what is the most common site of drug action

A

g protein coupled receptors

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9
Q

describe the structure of a receptor

A

single alpha helical peptide with seven transmembrane domains
extracellular domain contains the ligand binding area

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10
Q

describe the structure of a g protein

A

alpha subunit with diff forms

beta gamma subunit

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11
Q

what does the alpha subunit do

A

can bind to GDT and GTP

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12
Q

what does the BY subunit do

A

inhibits alpha subunit

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13
Q

how does the g protein function

A

occupied receptor changes shape and interacts with g protein which releases GDP and binds GTP. alpha subunit dissociates and activates adenylyl cyclase. hormone no longer present receptorconverts to resting state and GTP hydrolyzed to GDP

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14
Q

alpha subunits act on what? which on is inhibitory

A

adenylate cyclase

i is inhibitory

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15
Q

subunit q activates what

A

Phospholipase C

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16
Q

what are the second messengers activated by g proteins

A

camp
IP3
DAG
Ca

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17
Q

how do ligand channels work

A

ligand binding triggers confomational change in receptor and the channel opens

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18
Q

what is the ligand gated sodium channel

A

nicotinic acetylcholine

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19
Q

what is theligand gated calcium channel

A

NMDA

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20
Q

what is the ligand gated chloride channel

A

GABA

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21
Q

how are voltage gated channels different from ion gated

A

activated by changes in membrane ds potential not ligan

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22
Q

what is an ion pump

A

transmembrane protein that moves ions across pm against their concentration gradient

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23
Q

what is the cell membrane enzyme linked receptor

A

tyrosin kinase receptor

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24
Q

what is the structure of a tyrosin kinase receptor

Study These Flashcards
A

spans the membrane in the form of dimers or multisubunit complexes

25
how does the tyrosin kinase receptor function
ligand binds to receptor causing a conformational change forming dimers and converts kinases to active forms induces receptor autophosphorylation
26
what is an example of a intracellular enzyme lonked receptor
soluble guanylyl cyclase
27
what is the structure of guanylyl cyclase
forms hterodimer with alpha and beta subunit regulatory domain coiled coil domain cyclase domain
28
how does guanylyl cyclase function
activated by nitroc oxide | activates second messenger cGMP
29
what is the structure of a intracellular nuclear receptor
ligand binding part and DNA binding part | in nucleus
30
how do nuclear receptors function
ligand diffuses into cell and interacts with the nuclear receptor then translocates to the nucleus activated receptor binds to promoter region of gene resulting in gene expression
31
what is bmax
maximal specific bindign of a ligand to receptor
32
what is kd
concentration of drug where half maximal binding is observed
33
describe affinity
how attracted the drug is to the receptor
34
how does kd relate to affinity
as kd decreases the affinity increases
35
describe selectivity
preference for one receptor over another
36
what is e max
max effect induced by the drug
37
ec50
concentration of the drug that produces an effect that is half the max
38
describe potency
amount of drug needed to produce a given magnitude
39
describe efficacy
ability of a drug to elicit a biological response by agonist, determined by emax
40
what is an agonist
agent that can bind to a receptor and elicit a biologic response
41
what is a full agonist
produces max response, mimics
42
what is a partial agonist
activates receptor with a lower efficacy, will reduce effects of full agonist
43
what is an inverse agonist
has a negative effect on the receptor
44
what is an antagonist
drug combines wiht receptor but produces no response
45
how do competitive antagonists work
compete with agonist by binding to the same site on the receptor, can be overcome by increasing concentration of agonist
46
how do non competitve antagonists work
bond covalently or with such high affinity those receptors are unavailable to agonists
47
how do allosteric antagonists work
bind to allosteric site which prevents receptor from activating even when agonist is attached
48
define adverse effect
undesired harmful effect resukting from a medication
49
what is TD50
drug dose that produces toxic effect in 50% of patients
50
what is ED50
drug dose that produces therapeutic effect in 50% of patients
51
how is ED50 and EC50 different
EC is to reach 50% of max biological response which ED is for 50% to reach therapeutic response
52
how do you calculate the therapeutic index
TD50/ED50
53
what does it mean if TI is high
there is a wide therapeutic window so it has high safetyy
54
define idiosyncratic
individuals exhibit an unusual drug response
55
define tachyphylaxis
acute rapid loss of response to a drug
56
define tolerance
decreased response to a drug when the drug is taken repeatedly
57
what is receptor desensitization
mechanism that reduces the receptor response to an agonist
58
what are the four phases in drug development
1: small number, screen for safety 2: study efficacy 3: larger, safety and efficacy 4: large number post marketing studies

Pharmacology 2100 (13 decks)

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