1-1 Edwardson Flashcards
Benzilylcholine mustard
Irreversibly alkylates muscarinic receptor
Cholera toxin
ADP ribosylation of a(s)Inhibits GTPase activitySustained activation of adenylyl cyclase
Pertussis toxin
ADP ribosylation of a(i)Prevents activation of Gi in response to receptor stimulation
Tyrphostins
Inhibitors of tyrosine kinase
Prednisolone
Agonist for glucocorticoid receptors
Spironolactone
Antagonist for mineralocorticoid receptors
Ethinylestradiol
Agonist for estrogen receptor
Tamoxifen
Antagonist for estrogen reveptor
Norethisterone
Agonist for progestagen receptor
Lidocaine- 2 main uses -what fibres does it affect? -what does it bind to? -acid or base? -how does it act in different pHs?
- 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)
Benzocaine
Local anaesthetic
Uncharged
Extent of block is independent of pH
Faster block - hydrophobic pathway within membrane for uncharged LAs
Quinidine
Local anaesthetic
Slow in slow out
Use dependence at low rates of stimulation
TetrodotoxinTTX
Guanidinium groups
Block Na channels from outside
Do not show use dependence
Bay K 8644
Dihydropyridine (DHP)
Calcium agonist
Lipid soluble
Nifedipine
Dihydropyridine (DHP)
Lipid soluble
Calcium antagonist
Verapamil
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
Diltiazem
Ca channel blockerBind to site away from DHP binding site Site interact, so enhances DHP bindingUse dependenceProlonged blockPreferentially cardiac muscleAntidysrhythmics
Minoxidil
K channel openerHyper polarise cell membraneRelax smooth muscle
Nicorandil
K channel openerHyper polarise cell membraneRelax smooth muscle
GlibenclamideHow does it work?
Close Katp acting on sulphonylurea receptorDepolarise pancreatic B cell membFires VGCa channelCa influxInsulin release
Atropine
Antagonist for muscarinic receptor on smooth muscle
D-tubocurarine
Antagonist for nicotinic receptors on skeletal muscle
Isoprenaline
B-adrenoreceptor agonistInactive isomer has affinity
Adenosine
Conc increases in cell damage
7tm Gprotein coupled
A2a receptor - anti-inflammatory
A1 receptor - heart block in AV node
a bungarotoxin
Neurotoxin
binda and irreversibly inhibits nAChR at nmj
Lidocaine
- how does it cross the membrane and block the channel?
- dependence?
- what in what out?
-Cross membrane in uncharged form Blocks channel best in charged form -Use dependence at high rates of stimulation Voltage dependence -Fast in fast out
GlibenclamideWhat is it, what does it do/treat?
Orally acting hypoglycaemic agentTreat type 2 diabetesSulphonylurea
