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PMCOL 200 > LEC 2 > Flashcards

LEC 2 Flashcards

1
Q

INTRACELLULAR RECEPTORS what are characteristics of drugs that bind to intracellular receptors (2)

A
  1. hydrophobic

2. lipid soluble

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2
Q

INTRACELLULAR RECEPTORS what is mech of action

A
  1. drug crosses PM
  2. drug binds intracellular receptor
  3. receptor displaces HSP to expose DNA binding site
  4. receptor translocates to nucleus
  5. receptor binds to DNA
  6. receptor activates transcription of target gene
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3
Q

INTRACELLULAR RECEPTORS what are characteristic effects of drug binding to intracellular receptor

A
  1. slow onset

2. long lasting

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4
Q

G PROTEIN (TRANS MEM) what are G protein subunits

A
  1. alpha
  2. beta
  3. gamma
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5
Q

G PROTEIN (TRANS MEM) what happens at rest

A
  1. GDP bound to G alpha

2. G alpha bound to recepotr

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6
Q

G PROTEIN (TRANS MEM) what happens when ligand binds to recepotr

A

GDP GTP excahnge

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7
Q

G PROTEIN (TRANS MEM) what does GTP GDP exchange result in

A
  • G alpha unbinds from receptor + acts as effector

- G beta gamma unbinds from receptor + acts as effector

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8
Q

G PROTEIN (TRANS MEM) what is molecular timer mech referring to

A

G alpha hydrolyzes GTP to return sys to rest

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9
Q

G PROTEIN (TRANS MEM) what happens to G beta gamma after unbinding from receptor

A

remains associated w PM

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10
Q

G PROTEIN (TRANS MEM) what are 3 G alpha subtypes

A
  1. G s
  2. G i
  3. G q
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11
Q

G PROTEIN (TRANS MEM) what does Gs target

A

adenylyl cyclase to activate

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12
Q

G PROTEIN (TRANS MEM) what does Gi target

A

adenylyl cyclase to inactivate

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13
Q

G PROTEIN (TRANS MEM) what does Gq target

A

phospholipase C to activate

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14
Q

G PROTEIN (TRANS MEM) what does G alpha have indirect effect on

A

first components of signalling cascade

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15
Q

G PROTEIN (TRANS MEM) what is Gs mech (7)

A
  1. agonist binds to receptor
  2. receptor changes conformation
  3. GTP bound Gs activates AC
  4. AC converts ATP to cAMP
    5 cAMP activates protein kinase A
  5. protein kinase A phosphorylates substrate
  6. phosphorylates substrate generates biological response
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16
Q

G PROTEIN (TRANS MEM) what is Gi mech (7)

A
  1. agonist binds to receptor
  2. receptor changes conformation
  3. GTP bound Gi inhibits AC
  4. suppress cAMP
  5. suppress protein kinase A
  6. suppress phosphorylated substrate
  7. suppress biological response
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17
Q

G PROTEIN (TRANS MEM) what is Gq mech

A
  1. agonist binds receptor
  2. receptor undergoes conformational change
  3. GTP bound Gq activates PLC
  4. PLC hydrolyzes PIP2 ==> PIP3 and DAG

PIP 3

a. IP3 binds to ER
b. ER releases Ca
c. Ca binds to calmodulin
d. Ca-calmodulin complex binds to effector protein
e. effector protein generates biological response

DAG

a. DAG activates protein kinase C
b. protein kinase C phosphorylates substrate
c. phosphorylated substrate generates biological response

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18
Q

TKR (TRANS MEM) what happens when ligand binds to TKR

A
  1. dimerization
  2. phosphorylation ==> each other
  3. phosphorylation ==> substrate
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19
Q

TKR (TRANS MEM) what makes TKR diff from G protein

A

TKR acts as kinases

20
Q

INTRACELLULAR VS MEM BOUND what is circulating form of drug

A
  1. intracellular ==> bound

2. mem bound ==> variable

21
Q

INTRACELLULAR VS MEM BOUND what is speed of response

A
  1. intracellular ==> slow

2. mem bound ==> fast

22
Q

INTRACELLULAR VS MEM BOUND why is speed of response slow for intracellular (2)

A
  1. requires DNA binding

2. requires activating target genes

23
Q

INTRACELLULAR VS MEM BOUND how fast is termination of signal

A
  1. intracellular ==> slow

2. mem bound ==> fast

24
Q

INTRACELLULAR VS MEM BOUND why is termination slow for intracellular(2)

A
  1. large reserve of bounddrug

2. gene expression is slow to reverse

25
Q

ION CHANNEL what is fastest mech for signalling

A

ion channel

26
Q

ION CHANNEL what happens when ions cross PM

A

change in mem voltage

27
Q

ION CHANNEL what are 2 types

A
  1. ligand gated ion channel

2. voltage gated ion channel

28
Q

ION CHANNEL what is ligand gated ion channel

A

pore in channel opens in response to binding of ligand

29
Q

ION CHANNEL what is voltage gated ion channel

A

pore in channel opens in response to changing of voltage

30
Q

what is on x axis of conc response curves

31
Q

what is on y axis of conc response curves

32
Q

what relationship exists bw agonist conc and effect

A

saturating

33
Q

what is E max

A

max biological effect

34
Q

what is EC50

A

conc of drug that produces 50% E max

35
Q

what are2 ways of plotting conc

A
  1. linear scale

2. log

36
Q

what does linear scale result in

A

saturating response

37
Q

what does log scale result in

A

sigmoidal response

38
Q

what does efficacy refer to

A

mag of E max

39
Q

what does large efficacy mean

what does small efficacy mean

A
  • large efficacy ==> high Emax

- small efficacy ==> low Emax

40
Q

what does potency refer to

41
Q

what does weakly potent mean

A

high EC50, large concentration of drug required to generate half Emax

42
Q

what does strongly potent mean

A

low EC50, low concentration of drug required to generate half Emax

43
Q

what is full agonist

A

binds to receptor to generate E max

44
Q

what is partial agonist

A

binds to receptor to generate partial E max

45
Q

what is antagonist

A

binds to receptor to generate no effect (on own)

PMCOL 200 (2 decks)

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