Starting flash cards

Question 1

Class A G protein receptors

Answer 1

rhodopsin family
-bind amine neurotransmitters, neuropeptides, purines

Question 2

Class B protein receptors

Answer 2

secretin/glucagon family
-peptide hormone (glucagon, calcitonin)

Question 3

Class C protein receptors

Answer 3

metabotropic gluatamate receptor
-glutamate
-GABA
-Ca 2+

Question 4

Ion channel types

Answer 4

cys loop
lonotropic
P2X
Ca2+ release type

Question 5

kD definition

Answer 5

conc of ligand needed to bind half available receptors

Question 6

Selectivity vs specificity

Answer 6

selectivity in when it will bind many receptors
specificity is when it only binds one ever

Question 7

EC50>=Kd50

Answer 7

partial agonist (even when fully bound 100% effect isn’t reached)

Question 8

Spare receptors

Answer 8

when a drug is very effective and doesn’t need all the receptor it can bind to get 100% tissue response

Question 9

Metrics of polarity

Answer 9

-Log P (low = hydrophilic)
-Polar surface are (High=hydrophilic)

Question 10

Parenteral admin

Answer 10

avoids stomach and liver

Question 11

enteral admin

Answer 11

undergoes FPM

Question 12

Ficks law

Answer 12

the greater the concentration difference the faster diffusion

Question 13

Fg

Answer 13

fraction escaping the gut

Question 14

Fh

Answer 14

fraction escaping liver

Question 15

Eh

Answer 15

hepatic extraction raito (1-Fh)

Question 16

oral bioavailability

Answer 16

Fh * Fg

Question 17

Phase 1 metabolism

Answer 17

Functoinalization
-addition of a water soluble group
-oxidations by CYP P450 mostly

Question 18

where ligands bind to GCPR

Answer 18

N’ terminal

Question 19

Where G proteins bind to receptor

Answer 19

C’ terminal

Question 20

tyrosine kinases

Answer 20

bind Growth factors then phosphoraylze

Question 21

serine/theronine kinases

Answer 21

bind growth factors then phosphoralyze

Question 22

cytokine receptors

Answer 22

When activated they associate intracellular tyrosine kinases to affect gene transcription

Question 23

HRE

Answer 23

Hormone Response Element bound by type 1 nuclear receptors

Question 24

retinoid X receptor (RXR)

Answer 24

form heterodimer with type 2 nuclear receptors

Question 25

ATP-binding cassette (ABC)

Answer 25

Use ATP hydrolysis to efflux

Question 26

solute carrier (SLC)

Answer 26

Are involved in influx of small molecules (AA, sugars, ions)

Question 27

P-type ATPases

Answer 27

Na+/K+ pump

Question 28

Glutathionylation

Answer 28

a Phase 2 detoxification step in addition to excretion

Question 29

Glucuronidation

Answer 29

Phase 2 step by UDP glucuronosyl transferase -In ER and dominates at high [drug]

Question 30

Sulfation

Answer 30

Phase 2 step by sulfotransferases -in hepatocytes -dominates at low [drug]

Question 31

Steady state

Answer 31

when steady dose rate has been given for 5 half lives of elimination