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bms109 phys/pharm > Drugs & Receptors > Flashcards

Drugs & Receptors Flashcards

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
Q

Describe the structure of nuclear receptors

A

DNA linked, has zinc fingers

26
Q

Describe the ligand requirement for nuclear receptors

A

must be able to cross PM

27
Q

Which receptors are ionotropic

A

ligand gated ion channels

28
Q

How many subunits do ligand gated ion channels have

A

3-5

29
Q

Describe the structure of ligand gated ion channels

A

complex arranged to form a central aqueous pore

30
Q

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

A

opening

31
Q

describe the synaptic transmission of ligand gated ion channels

A

fast

32
Q

What ionotropic receptors are positive

A

acetylcholine, nicotinic, 5HT3

33
Q

What are positive ionotropic receptors selective for

A

cations

34
Q

What are negative ionotropic receptors selective for

A

anions

35
Q

Which ionotropic receptor has 4 transmembrane domains

A

nicotinic

36
Q

Describe acetylcholine ionotropic receptors

A

excitatory, cause depolarisation

37
Q

Describe the structure of nicotinic receptors

A

pentameric structure, heteromeric assembly,

38
Q

How do nicotinic channels open

A

two ACh molecules bind

39
Q

What do ACh molecules bind to on nicotinic channels

A

interfaces between alpha subunits

40
Q

what is the agonist for neuromuscular junction brain

A

nicotine

41
Q

What is the antagonist for neuromuscular brain junction

A

tubocurarine

42
Q

What does activation of ionotropic receptors for inhibitory neurotransmitters do

A

inhibits membrane depolarisation, reduces AP firing

43
Q

What is the antagonist of GABA

A

picrotoxin

44
Q

How many subunits do GPCRs ahve

A

3

45
Q

What are the subunits of GPCRs

A

alpha, beta, gamma

46
Q

What are the endogenous ligands for GPCRs

A

hormones, neuropeptides, small molecule transmitters

47
Q

What are the functions of GPCRs

A

transduce signals and bind guanine nucleotides

48
Q

Describe GPCRs at rest

A

GDP - inactivated, bound

49
Q

Describe GPCRs when activated

A

GTP

50
Q

What is the effect of an agonist binding to a G-Protein

A

activates G-protein, induces exchange of GDP - GTP

51
Q

Describe the structural changes of an activated G-Protein

A

protein dissociates into alpha and beta subunits

52
Q

What effectors are regulated by GPCRs

A

enzymes, ion channels

53
Q

What is cAMP

A

2nd messenger, small molecule

bms109 phys/pharm (22 decks)

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