Drugs & Receptors Flashcards

(53 cards)

1
Q

Name some drug targets

A

ion channels, enzymes, carriers

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2
Q

What drugs target ion channels

A

lignocaine, apamin, nifedipine

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3
Q

What does lignocaine bind to

A

voltage gated sodium channels

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4
Q

What is the effect of lignocaine

A

stops action potential firing, stops transmission of pain

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5
Q

What does apamin effect

A

potassium channels

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6
Q

What do dihydropyridines target

A

voltage gated calcium channels - heart

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7
Q

What do dihydropyridines treat

A

high BP

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8
Q

Name an ACE inhibitor

A

captopril

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9
Q

What does captopril treat

A

low BP

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10
Q

What does aspirin inhibit

A

COX enzyme

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11
Q

What drugs target enzymes?

A

aspirin, pargyline, captopril

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12
Q

What are pargyline and clorgyline

A

anti-depressants

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13
Q

What does pargyline inhibit

A

enzyme MAO-B

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14
Q

What is the effect of pargyline

A

prevents neurotransmitters being broken down

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15
Q

What drug binds to sodium potassium ATPase

A

digoxin

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16
Q

What does digoxin treat

A

heart failure

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17
Q

What is fluoxetine

A

anti-depressant

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18
Q

What is the effect of fluoxetine

A

binds and inhibits serotonin transporter

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19
Q

What is the effect of agonist binding to ligand gated ion channels

A

channels open

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20
Q

What is usually the agonist for ligand gated ion channels

A

ACh

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21
Q

How many times do GPCRs span the membrane

A

7 times

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22
Q

Describe the structure of kinase linked receptors

A

single transmembrane domain, enzyme built in

23
Q

Where are nuclear receptors foudn

A

inside the cell

24
Q

What is the function of nuclear receptors

A

regulate gene transcription

25
Describe the structure of nuclear receptors
DNA linked, has zinc fingers
26
Describe the ligand requirement for nuclear receptors
must be able to cross PM
27
Which receptors are ionotropic
ligand gated ion channels
28
How many subunits do ligand gated ion channels have
3-5
29
Describe the structure of ligand gated ion channels
complex arranged to form a central aqueous pore
30
What is the effect of agonist binding to ligand gated ion channels
opening
31
describe the synaptic transmission of ligand gated ion channels
fast
32
What ionotropic receptors are positive
acetylcholine, nicotinic, 5HT3
33
What are positive ionotropic receptors selective for
cations
34
What are negative ionotropic receptors selective for
anions
35
Which ionotropic receptor has 4 transmembrane domains
nicotinic
36
Describe acetylcholine ionotropic receptors
excitatory, cause depolarisation
37
Describe the structure of nicotinic receptors
pentameric structure, heteromeric assembly,
38
How do nicotinic channels open
two ACh molecules bind
39
What do ACh molecules bind to on nicotinic channels
interfaces between alpha subunits
40
what is the agonist for neuromuscular junction brain
nicotine
41
What is the antagonist for neuromuscular brain junction
tubocurarine
42
What does activation of ionotropic receptors for inhibitory neurotransmitters do
inhibits membrane depolarisation, reduces AP firing
43
What is the antagonist of GABA
picrotoxin
44
How many subunits do GPCRs ahve
3
45
What are the subunits of GPCRs
alpha, beta, gamma
46
What are the endogenous ligands for GPCRs
hormones, neuropeptides, small molecule transmitters
47
What are the functions of GPCRs
transduce signals and bind guanine nucleotides
48
Describe GPCRs at rest
GDP - inactivated, bound
49
Describe GPCRs when activated
GTP
50
What is the effect of an agonist binding to a G-Protein
activates G-protein, induces exchange of GDP - GTP
51
Describe the structural changes of an activated G-Protein
protein dissociates into alpha and beta subunits
52
What effectors are regulated by GPCRs
enzymes, ion channels
53
What is cAMP
2nd messenger, small molecule