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PCL302 > Term test 1 > Flashcards

Term test 1 Flashcards

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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
3 positive allosteric modulators of Nicotinic cholinergic receptor
1. Galantamine 2. Physostigmine/Neostigmine 3. a7 PAM (positive allosteric modulator) (inhibit breakdown of acetylcholine, increase ACh concentration at synaptic cleft)
26
3 phosphorylation of nicotinic cholinergic receptor
1. PKA 2. PKC 3. TK (tyrosine kinase)
27
a-bungarotoxin
irreversibly binds to and block the nicotinic receptor NMJ blockade at skeletal muscle paralysis death by respiratory depression
28
b-bungarotoxin
prevents release of ACh from motor nerve endings not enough release of ACh to stimulate muscle movement paralysis
29
D-Tubocurarine
``` non-depolarizing NMJ blocking drug antagonist compete with agonist prevent binding of ACh on receptor zero efficacy ```
30
Neostigmine
ACh esterase inhibitor prevent breakdown of ACh leads to increase ACh concentration overcome non-depolarizing NMJ blockade (d-tubocurarine)
31
Succinylcholine
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
GABAa receptor
``` allow Cl- to enter cell fast activation and inactivation pentamer M2 region leads to hyperpolarization ```
33
Benzodiazepine (diazepam)
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
GABAa receptors inverse agonist (NAM) | negative allosteric modulators
reduce influx of Cl- into cells | accompanied by anxiety (anxiogenic)
35
Where is the high affinity binding site for benzodiazepine (diazepam)?
between a1 and y2 (histidine 101) | insensitive to a4 and a6 containing receptor
36
TP003
``` plus maze experiment selective for a2/a3 containing GABA receptor anxiolytic effect (reduce anxiety) ```
37
a1 GABA receptor subtype
mediates sedation | Zolpidem acts at BZD site
38
a2 and a3 GABA receptor subtype
anxiolytic effect if inverse agonist at a3 = anxiogenic no selective drug on market currently
39
3 types of Glutamate receptor
``` 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
PCP and Ketamine
acts on glutamate receptor | hallucinogen, dissociative anesthetic
41
How does NMDA (memantine) antagonist improve Alzheimer disease?
reduce calcium toxicity, reduce loss of neurons, protect neuronal function
42
Furosemide and Toreasemide
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
Adverse effect of furosemide and torasemide
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
Gitelman's Syndrome
``` 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
Chlorothiazide and hydrochlorothizide
blocks NCC increase K secretion decrease Ca excretion (stimulate Ca reabsorption in DCT) treat hypertension, edema adverse effect: hypokalemia, hyponatremia, hypercalcemia
46
Dopamine Transporter
12 TM regions use Na gradient regulates dopamine level in synaptic cleft DAT deletion leads to hyperactivity, motor and cognitive deficits increase depression
47
Serotonin receptors (SERT) and Selective serotonin reuptake inhibitors (SSRIs)
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
Fluoxetine (Prozac) and Sertraline (Zoloft)
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
Aspirin and celecoxib
anti-inflammatory | celecoxib more selective for COX2 than aspirin, less side effect
50
3 structural features of GPCRs
7 TM domains EC N terminus and 3 loops IC C terminus and 3 loops
51
2 types of Class A GPCRs
dopamine receptor (d1 and d2) and B-adrenergic receptor
52
1 type of class B GPCRs
secretin receptors
53
2 types of Class C GPCRS and its features
Glutamate receptor and GABA-B receptors contains VFT (Venus flytrap) domain and CRD (cysteine rich domain) form obligate dimer, either homodimers or heterodimers
54
RGS protein
promote GTP hydrolysis and turn off G alpha protein signal
55
RGS protein acting as effector in GPCR signalling
bind to RhoGEF (p115-RhoGEF) activates GEF activity RhoA-GDP -> RhoA-GTP leads to cytoskeleton rearrangement and transcriptional upregulation
56
Structure of adenylyl cyclase
2 groups of 6 TM domains | linked by C1 domain and C2 domain at C-terminus
57
Structure of voltage gated ion channels (VGIC)
4 domains each with 6 TM regions | a-subunit
58
2 Monoclonal antibodies for ErbB therapeutics
Herceptin (ErbB2 breast and gastric cancer) | Cetuximab (ErbB1 colorectal cancer)
59
ErbB1 inhibitors and ErbB1 + ErbB2 inhibitors
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
Trastuzumab (Herceptin) and cetuximab
Herceptin binds to ErbB2 breast and gastric cancer treatment in combination of paclitaxel cetuximab binds to ErbB1 for colorectal cancer
61
4 effects after insulin stimulation
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
IGF-1 excess leads to?
gigantism, acromegaly (excess insulin growth factor after puberty)
63
IGF-2
single peptide fetal growth factor binds to mannose 6 phosphate receptor growth effects through IGF-1 receptors (similar effect)
64
Which dopamine receptor is important for treating schizophrenia (antipsychotics)?
D2 dopamine receptors | chlorpromazine
65
Signal transduction pathway of ErbB (start from PI3K)
PI3K -> PIP2 -> PIP3 -> PDK -> PKB/AKT -> mTOR -> protein synthesis PKB/AKT ---> Ras/MAPK PIP2 -> IP3 + DAG -> PKC
66
ErbB1
forms homo/hetero dimer 1,2,3,4 recruits Grb2/Shc/Sos -> Ras -> MAPK
67
ErbB2
``` 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
ErbB3
``` ligand: heregulin, neuregulin have an inactive kinase domain has six different PI3K binding domains knockout has atrioventricular defects hetero with 1,2 ```
69
ErbB4
``` 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
Psoriasis
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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