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PCL302 > Term test 1 > Flashcards

Term test 1 Flashcards

1
Q

Propranolol

A

blocks B1 and B2 adrenergic receptor, antihypertensive and antiarrhythmic
antagonist

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2
Q

Nadolol

A

B1 and B2 adrenergic receptor, angina prophylactic

longer half life than propranolol

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3
Q

Metoprolol

A

selective on B1 adrenergic receptor, antiarrhythmic

decrease cardiac output

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4
Q

Carvedilol

A

B1 and A1 adrenergic receptor, heart failure
non-selective antagonist
decrease cardiac output and vasodilation

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5
Q

Salbutamol

A

B2 selective agonist
vasodilation in lungs
last 3-6 hours, treats asthma

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6
Q

Salmeterol

A

B2 selective agonist

lasts 12 hours, treat asthma

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7
Q

BRL37344

A 
B3 adrenergic selective agonist
increase lipolysis
use in treatment of obesity
cardiovascular effect profound hypotension
uterine relaxation
decrease cardiac contractility
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8
Q

Phenylephrine and methoxamine

A

A1 adrenergic receptor agonist
vasoconstrictor, treatment for hypotension
decongestant

side effects: induce angina in patients with coronary heart disease
rebound congestion after use

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9
Q

B1 adrenergic receptor

A

expressed in the heart
increase intracellular Ca level in myocyte
increase force and contractility of heart
increase stroke volume

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10
Q

B2 adrenergic receptor

A 
found in smooth muscle of lungs and blood vessels
muscle relaxation
decrease intracellular Ca level
increase intracellular K level
leads to bronchodilation
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11
Q

B3 adrenergic receptor

A

expressed in adipocytes
increase lipolysis
decrease heart contractility

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12
Q

A1 adrenergic receptor

A 
in smooth muscle, respiratory mucosa and radial muscle of the eye
activated by Gq protein
vasoconstriction
increase in blood pressure
increase intracellular Ca level
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13
Q

3 factors affecting the permeability of ion through the selectivity filter

A
  1. size of ion
  2. hydration shell created with aqueous environment
  3. ability of ion to interact with amino acid in the pore region of channel
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14
Q

3 different subtypes of voltage-gated calcium channels

A

L-type: long lasting (no inactivation)
P/Q type: Purkinje (mild inactivation)
T-type: transient (rapid opening and closing)

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15
Q

B - scorpion toxins

A 
VGIC
enhanced activation
leftward shift of dose response curve
higher sensitivity
Na+ enter cells sooner
increase excitability
more hyperpolarize
less activation energy required to open channel
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16
Q

Tetrodotoxin (TTX), Saxitoxin, u-conotoxin

A

Pore block
site 1
Na+ ions cannot move down the concentration gradient
no ion movement

Tetrodotoxin (TTX) can inhibit spontaneous action potential
leads to treatment of epilepsy and seizure (hyperactivity of channel)

most neuronal Na channels are sensitive to TTX but some are resistant

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17
Q

7 Na+ channel blockers

A

Resveratrol (from red wine)
Lidocaine, Procaine (arrhythmia)
Phenytoin, Carbamazepine, Topiramate (headache, pain and migraine)
Quinidine

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18
Q

L-type calcium channel blocker

A

dihydropyridines (DHP)

verapamil, diltiazem (Non-DHP)

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19
Q

K+ channel blocker

A

Amiodarone

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20
Q

Resveratrol

A

French’s paradox
in red wine
effective inhibition of Na+ current by grape extract
C1 = resveratrol derivative
reduce duration of atrial fibrillation
resveratrol and C1 have many targets -> effect unlikely due to one mechanism (can also block late sodium current)

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21
Q

Resveratrol and C1

A

French’s paradox
in red wine
effective inhibition of Na+ current by grape extract
C1 = resveratrol derivative
reduce duration of atrial fibrillation
resveratrol and C1 have many targets -> effect unlikely due to one mechanism (can also block late sodium current)

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22
Q

M2 muscarinic receptor

A

decrease heart rate, conduction velocity and contractility

  1. G protein inhibit T-type calcium channel
  2. G protein activates K channel move K out
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23
Q

4 nicotinic agonists

A
  1. Ach
  2. Nicotine
  3. Carbachol
  4. Succinylcholine
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24
Q

2 nicotinic antagonists

A
  1. d-tubocurarine at NMJ

2. a-bungarotoxin (irreversible antagonist)

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25
Q

3 positive allosteric modulators of Nicotinic cholinergic receptor

A
  1. Galantamine
  2. Physostigmine/Neostigmine
  3. a7 PAM (positive allosteric modulator) (inhibit breakdown of acetylcholine, increase ACh concentration at synaptic cleft)
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26
Q

3 phosphorylation of nicotinic cholinergic receptor

A
  1. PKA
  2. PKC
  3. TK (tyrosine kinase)
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27
Q

a-bungarotoxin

A

irreversibly binds to and block the nicotinic receptor
NMJ blockade at skeletal muscle
paralysis
death by respiratory depression

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28
Q

b-bungarotoxin

A

prevents release of ACh from motor nerve endings
not enough release of ACh to stimulate muscle movement
paralysis

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29
Q

D-Tubocurarine

A 
non-depolarizing NMJ blocking drug
antagonist
compete with agonist
prevent binding of ACh on receptor
zero efficacy
30
Q

Neostigmine

A

ACh esterase inhibitor
prevent breakdown of ACh leads to increase ACh concentration
overcome non-depolarizing NMJ blockade (d-tubocurarine)

31
Q

Succinylcholine

A

depolarizing blockade
2 molecules of ACh binding together
binds to nicotinic receptor and leads to activation
not metabolized by ACh esterase
longer activation leads to desensitization of receptor
leads to flaccid paralysis

32
Q

GABAa receptor

A 
allow Cl- to enter cell
fast activation and inactivation
pentamer
M2 region
leads to hyperpolarization
33
Q

Benzodiazepine (diazepam)

A

increase frequency of GABA channel opening and affinity/potency for GABA for receptor
shift dose response curve left
leads to sedative, muscle relaxation, anticonvulsant, coma

34
Q

GABAa receptors inverse agonist (NAM)

negative allosteric modulators

A

reduce influx of Cl- into cells

accompanied by anxiety (anxiogenic)

35
Q

Where is the high affinity binding site for benzodiazepine (diazepam)?

A

between a1 and y2 (histidine 101)

insensitive to a4 and a6 containing receptor

36
Q

TP003

A 
plus maze experiment
selective for a2/a3 containing GABA receptor
anxiolytic effect (reduce anxiety)
37
Q

a1 GABA receptor subtype

A

mediates sedation

Zolpidem acts at BZD site

38
Q

a2 and a3 GABA receptor subtype

A

anxiolytic effect
if inverse agonist at a3 = anxiogenic
no selective drug on market currently

39
Q

3 types of Glutamate receptor

A 
modulate Na, Ca and K
1. NMDA (most permeable to calcium)
2.AMPA
3. Kainate (KA)
3 TM region, 2nd region is a hairpin loop within the membrane
40
Q

PCP and Ketamine

A

acts on glutamate receptor

hallucinogen, dissociative anesthetic

41
Q

How does NMDA (memantine) antagonist improve Alzheimer disease?

A

reduce calcium toxicity, reduce loss of neurons, protect neuronal function

42
Q

Furosemide and Toreasemide

A

inhibit NKCC2 at TAL
block Na/Cl reabsorption at H2O impermeable segment
impairs H2O clearance
increase K secretion
inhibit Ca and Mg reabsorption and increase their secretion

43
Q

Adverse effect of furosemide and torasemide

A

intravascular volume depletion
reduced GFR
hypokalemia (metabolic alkalosis due to hydrogen loss)
hyperuricemia (increase uric acid in plasma, crystal forming leads to gout)
acute rapid infusion may lead to transient deafness (NKCC1 in inner ear)

but generally tolerated really well

44
Q

Gitelman’s Syndrome

A 
reduce expression of NCC at distal convoluted tubule
reduce reabsorption of Na
increase H2O excretion
low blood pressure
salt wasting
hypokalemia and metabolic alkalosis
45
Q

Chlorothiazide and hydrochlorothizide

A

blocks NCC
increase K secretion
decrease Ca excretion (stimulate Ca reabsorption in DCT)
treat hypertension, edema

adverse effect: hypokalemia, hyponatremia, hypercalcemia

46
Q

Dopamine Transporter

A

12 TM regions
use Na gradient
regulates dopamine level in synaptic cleft
DAT deletion leads to hyperactivity, motor and cognitive deficits
increase depression

47
Q

Serotonin receptors (SERT) and Selective serotonin reuptake inhibitors (SSRIs)

A

12 TM regions
transport of Na, Cl and 5HT into presynaptic cells
associated with mood, anxiety, sleep, appetite, gastrointestinal cortical areas…
hyperactivity - anxiety
hypoactivity - depression

48
Q

Fluoxetine (Prozac) and Sertraline (Zoloft)

A

antidepressant
treat anxiety, OCD, eating disorder
delayed efficacy
long half-lives (7-15 days)

unwanted effects: sexual dysfunction, weight gain, headache nausea, suicidal ideation, akathisia (movement disorder, hard to stay still)

49
Q

Aspirin and celecoxib

A

anti-inflammatory

celecoxib more selective for COX2 than aspirin, less side effect

50
Q

3 structural features of GPCRs

A

7 TM domains
EC N terminus and 3 loops
IC C terminus and 3 loops

51
Q

2 types of Class A GPCRs

A

dopamine receptor (d1 and d2) and B-adrenergic receptor

52
Q

1 type of class B GPCRs

A

secretin receptors

53
Q

2 types of Class C GPCRS and its features

A

Glutamate receptor and GABA-B receptors
contains VFT (Venus flytrap) domain and CRD (cysteine rich domain)
form obligate dimer, either homodimers or heterodimers

54
Q

RGS protein

A

promote GTP hydrolysis and turn off G alpha protein signal

55
Q

RGS protein acting as effector in GPCR signalling

A

bind to RhoGEF (p115-RhoGEF)
activates GEF activity
RhoA-GDP -> RhoA-GTP
leads to cytoskeleton rearrangement and transcriptional upregulation

56
Q

Structure of adenylyl cyclase

A

2 groups of 6 TM domains

linked by C1 domain and C2 domain at C-terminus

57
Q

Structure of voltage gated ion channels (VGIC)

A

4 domains each with 6 TM regions

a-subunit

58
Q

2 Monoclonal antibodies for ErbB therapeutics

A

Herceptin (ErbB2 breast and gastric cancer)

Cetuximab (ErbB1 colorectal cancer)

59
Q

ErbB1 inhibitors and ErbB1 + ErbB2 inhibitors

A

ErbB1 only:

  1. Gefitinib
  2. Erlotinib

ErbB1 + ErbB2

  1. Lapatinib
  2. CI-1033
  3. EKB-569

(approved for non-small-cell lung cancer treatment)

60
Q

Trastuzumab (Herceptin) and cetuximab

A

Herceptin binds to ErbB2 breast and gastric cancer treatment in combination of paclitaxel
cetuximab binds to ErbB1 for colorectal cancer

61
Q

4 effects after insulin stimulation

A
  1. increased glucose synthesis
  2. increased glycogen synthesis in liver and muscle
  3. increased fatty acid synthesis
  4. increased uptake of amino acids (and protein synthesis)
62
Q

IGF-1 excess leads to?

A

gigantism, acromegaly (excess insulin growth factor after puberty)

63
Q

IGF-2

A

single peptide
fetal growth factor
binds to mannose 6 phosphate receptor
growth effects through IGF-1 receptors (similar effect)

64
Q

Which dopamine receptor is important for treating schizophrenia (antipsychotics)?

A

D2 dopamine receptors

chlorpromazine

65
Q

Signal transduction pathway of ErbB (start from PI3K)

A

PI3K -> PIP2 -> PIP3 -> PDK -> PKB/AKT -> mTOR -> protein synthesis

PKB/AKT —> Ras/MAPK PIP2 -> IP3 + DAG -> PKC

66
Q

ErbB1

A

forms homo/hetero dimer
1,2,3,4
recruits Grb2/Shc/Sos -> Ras -> MAPK

67
Q

ErbB2

A 
no specific ligand
can dimerize without ligand
hetero with 1,3,4
potent stimulators of cell proliferation and internalize slowly
high expression in tumor
68
Q

ErbB3

A 
ligand: heregulin, neuregulin
have an inactive kinase domain
has six different PI3K binding domains
knockout has atrioventricular defects
hetero with 1,2
69
Q

ErbB4

A 
binds neuregulin and other ligands
forms homo and hetero dimers with 1,2,4
recruits Grb2/Shc/Sos -> Ras -> MAPK
knockout has heart developmental defects
may play a role in schizophrenia
70
Q

Psoriasis

A

lesions caused by rapid production of keratinocytes with inflammation
hyperactive response to growth factors amphiregulin and ErbB1-3 expression

PCL302 (2 decks)

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