1-1 Edwardson

Question 1

Benzilylcholine mustard

Answer 1

Irreversibly alkylates muscarinic receptor

Question 2

Cholera toxin

Answer 2

ADP ribosylation of a(s)Inhibits GTPase activitySustained activation of adenylyl cyclase

Question 3

Pertussis toxin

Answer 3

ADP ribosylation of a(i)Prevents activation of Gi in response to receptor stimulation

Question 4

Tyrphostins

Answer 4

Inhibitors of tyrosine kinase

Question 5

Prednisolone

Answer 5

Agonist for glucocorticoid receptors

Question 6

Spironolactone

Answer 6

Antagonist for mineralocorticoid receptors

Question 7

Ethinylestradiol

Answer 7

Agonist for estrogen receptor

Question 8

Tamoxifen

Answer 8

Antagonist for estrogen reveptor

Question 9

Norethisterone

Answer 9

Agonist for progestagen receptor

Question 10

Lidocaine-
2 main uses
-what fibres does it affect?
-what does it bind to?
-acid or base?
-how does it act in different pHs?

Answer 10

• Local anaesthetic Antidysrhythmic agent
• Affects c and Adelta fibres
• Binds preferentially to and stabilises inactivated state (Na channels)
• Weak base
• High ph-greater inhibition, lower potency (when perfused inside)

Question 11

Benzocaine

Answer 11

Local anaesthetic
Uncharged
Extent of block is independent of pH
Faster block - hydrophobic pathway within membrane for uncharged LAs

Question 12

Quinidine

Answer 12

Local anaesthetic
Slow in slow out
Use dependence at low rates of stimulation

Question 13

TetrodotoxinTTX

Answer 13

Guanidinium groups
Block Na channels from outside
Do not show use dependence

Question 14

Bay K 8644

Answer 14

Dihydropyridine (DHP)
Calcium agonist
Lipid soluble

Question 15

Nifedipine

Answer 15

Dihydropyridine (DHP)
Lipid soluble
Calcium antagonist

Question 16

Verapamil

Answer 16

Ca channel blocker 
Bind to site away from DHP binding site Site interact, so reduces DHP binding 
Use dependence 
Prolonged block 
Preferentially cardiac muscle 
Antidysrhythmics

Question 17

Diltiazem

Answer 17

Ca channel blockerBind to site away from DHP binding site Site interact, so enhances DHP bindingUse dependenceProlonged blockPreferentially cardiac muscleAntidysrhythmics

Question 18

Minoxidil

Answer 18

K channel openerHyper polarise cell membraneRelax smooth muscle

Question 19

Nicorandil

Answer 19

K channel openerHyper polarise cell membraneRelax smooth muscle

Question 20

GlibenclamideHow does it work?

Answer 20

Close Katp acting on sulphonylurea receptorDepolarise pancreatic B cell membFires VGCa channelCa influxInsulin release

Question 21

Atropine

Answer 21

Antagonist for muscarinic receptor on smooth muscle

Question 22

D-tubocurarine

Answer 22

Antagonist for nicotinic receptors on skeletal muscle

Question 23

Isoprenaline

Answer 23

B-adrenoreceptor agonistInactive isomer has affinity

Question 24

Adenosine

Answer 24

Conc increases in cell damage
7tm Gprotein coupled
A2a receptor - anti-inflammatory
A1 receptor - heart block in AV node

Question 25

a bungarotoxin

Answer 25

Neurotoxin

binda and irreversibly inhibits nAChR at nmj

Question 26

Lidocaine

• how does it cross the membrane and block the channel?
• dependence?
• what in what out?

Answer 26

-Cross membrane in uncharged form
Blocks channel best in charged form
-Use dependence at high rates of stimulation
Voltage dependence 
-Fast in fast out

Question 27

GlibenclamideWhat is it, what does it do/treat?

Answer 27

Orally acting hypoglycaemic agentTreat type 2 diabetesSulphonylurea