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Pharmocology > Receptors and peripheral nerves > Flashcards

Receptors and peripheral nerves Flashcards

1
Q

Cholera toxin

A

ADP-ribosylates the a-subunit of Gs preventing its GTPase activating and therefore sustaining activation of adenyl cyclase

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2
Q

Pertussis toxin

A

ADP-ribosylates the a-subunit of Gi preventing it’s activation and hence preventing the inhibition of Adenyl cyclase leading to sustained activation
Whooping cough

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3
Q

AIF4-

A

Mimics the Y phosphate of GTP and can causes consistent activation of the G-protein

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4
Q

Lithium

A

Inhibits the recycling of IP3 into Inostol in GQ/11 coupled receptors

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5
Q

Carvedilol

A

Third generation B-blocker, activates the B-arrestin pathway

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6
Q

Tyrophostins

A

Act to inhibit receptor tyrosine kinases, used to control neoplastic growth

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7
Q

Procaine

A

Local anaesthetic (ester)
Acts by inhibiting NaV by binding to IFY motif on 6th segment of 4th domain
Preference to pain fibres (Ad+c) and rapidly firing, must block 3 node of Ranvier to inhibit conduction
Weak base - inhibits channel in charged form but must pass through the membrane uncharged
Voltage dependence - inhibition increased with hyperpolarising pre-pulse

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8
Q

Lindocaine

A

Local anaesthetic (amide)
Acts by inhibiting NaV by binding to IFY motif on 6th segment of 4th domain
Preference to pain fibres (Ad+c) and rapidly firing, must block 3 node of Ranvier to inhibit conduction
Shifts inactivation value which results in a greater number of channels being inactivated at membrane potential
Preferentially binds to the channel in its inactive state therefore shows use dependence
Weak base - inhibits channel in charged form but must pass through the membrane uncharged
Voltage dependence - inhibition increased with hyperpolarising pre-pulse
Most effective in ischemic tissue, used in the treatment of ventricular arrhythmia’s

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9
Q

Benzocaine

A

Local anaesthetic (ester)
Acts by inhibiting NaV by binding to IFY motif on 6th segment of 4th domain
Preference to pain fibres (Ad+c) and rapidly firing, must block 3 node of Ranvier to inhibit conduction
Voltage dependence - inhibition increased with hyperpolarising pre-pulse

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10
Q

Quinidine

A

Local anaesthetic, inhibits NaV channel, rate of inhibition and dissociated slow, use dependence, used in the treatment of suproventricular tachycardia

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11
Q

Tetrodatoxin

A

Natural inhibitor of the NaV channel
Bind to outer ring of charged glutamate residues and promotes sodium to leave the cell
NaV channels in the heart glutamate is replaced with cystine therefore toxins have reduced action

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12
Q

Saxitoxin

A

Natural inhibitor of the NaV channel
Bind to outer ring of charged glutamate residues and promotes sodium to leave the cell
NaV channels in the heart glutamate is replaced with cystine therefore toxins have reduced action

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13
Q

Batrachatoxin

A

Poison from the tree frog
Activated the NaV channel at more negative potentials resulting in increased excitability of the cells
Risk of arrhythmia’s

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14
Q

Cd2+ and Mn2+

A

Can cause non-selective block of Voltage gated calcium channels

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15
Q

Nifedipine

A

Dihydropyridine
L-Type selective CaV channel inhibitor
Very lipid soluble
Action seen on cardiac and smooth muscle cells
Preferentially block CaV channels in the heart therefore used was anti-dysrhytmics
Can cause peripheral and coronary vasodilation - used in the treatment of hypertension ??

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16
Q

Verapamil

A 
Phenylalkyamine
L-type selective CaV channel inhibitor 
Reduces affinity for dihydropyridines 
Use dependence 
Preferentially block CaV channels in the heart therefore used was anti-dysrhytmics
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17
Q

Diltiazem

A 
Benzothiazepine 
L-Type selective CaV channel inhibitor 
increases affinity for dihydropyridines 
Use dependence 
Preferentially block CaV channels in the heart therefore used was anti-dysrhytmics
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18
Q

Mibefradil

A

Benzimidazolt tetraline

Inhibits both L and T-type calcium channels

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19
Q

Diazoxide

A

K+(ATP) channel opener
Inhibits ATP binding therefore causes channel to open leading to hyperpolaristion of the cells therefore smooth muscle relaxation
Hypertension, Asthma, IBS

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20
Q

Minoxidil

A

K+(ATP) channel opener
Inhibits ATP binding therefore causes channel to open leading to hyperpolaristion of the cells therefore smooth muscle relaxation
Hypertension, Asthma, IBS

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21
Q

Nicorandil

A

K+(ATP) channel opener
Inhibits ATP binding therefore causes channel to open leading to hyperpolaristion of the cells therefore smooth muscle relaxation
Hypertension, Asthma, IBS

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22
Q

Tolbutamide

A 
Hypoglycemic agent 
Closes K(ATP) channel by action on sulphonylurea receptors - causes depolarisation 
Acts in pancreatic B-cells, firing CaV channels stimulating insulin release
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23
Q

Glibencalamide

A 
Hypoglycemic agent 
Closes K(ATP) channel by action on sulphonylurea receptors - causes depolarisation 
Acts in pancreatic B-cells, firing CaV channels stimulating insulin release
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24
Q

Botulinium toxin

A

Preferentially targets Cholinergic neurones - C terminus binds to ganglioside receptor on neurone surface, endocytosed and N-terminus punctures endosome releasing toxin into cytoplasm
Somatic muscle weakness, constipation, blurred vision, urinary retention and dry skin
A+E = SNAP-25
C = SYTAXIN + SNAP-25
B, D, F+G = SYNAPTOBREVIN

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25
Q

Tetanus toxin

A

Retrograde transport to motor neurone cell body and transferred to inhibitory interneuron inhibiting inhibition through the inactivation of SYNAPTOBREVIN
Locked jaw and arched body

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26
Q

Hemicholinium

A

Inhibits choline uptake into the nerve terminal, binds to the outface of the receptor

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27
Q

Triethylcholine

A

ACh false transmitter - Competitive substrate, acetylated within the nerve into acetyltriethycholine and released instead of ACh

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28
Q

Vesamicol

A

Non-comeptitive, reversible inhibitor of VACht (transports ACh into vesicle with ATP, ratio of 10:1)

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29
Q

B-Bungarotoxin

A

Inhibits the release of ACh - 2 chain toxin linked with a disulphide bond, binds to the synaptic K+ channels and through the action of phospholipase A2 acts to break down nerve terminal
Respiratory failure and paralysis of respiratory muscles

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30
Q

A-Ladrotoxin

A

Causes massive release of ACh - bind to neurexins, transmembrane receptors on the pre-synaptic terminal, causes the formation of a divalent cation pore which allow Ca2+ influx and consequent transmitter release, also inhibits K+ channels
Respiratory failure and paralysis of respiratory muscles

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31
Q

Trimetaphan

A

Selective ganglionic nicotinic competitive antagonist, used during surgery to lower blood pressure

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32
Q

A-Bungarotoxin

A

Irrreversible Inhibitor of the NMJ nicotinic receptor, also inhibits the A(7) nicotinic receptor in the brain

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33
Q

Mecamylamine

A

Non-competitive selective inhibitor for the ganglionic nicotinic receptor

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34
Q

Hexamethonium

A

Non-competitive selective inhibitor for the ganglionic nicotinic receptor, causes use dependence block, used to used in the treatment of hypotension, blocks the ganglionic receptor of both parasympathetic and sympathetic pre-ganglionic however - caused decrease in cardiovascular tone, cause dry mouth and skin, and constipation
Has a 2+ charge therefore administered IV

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35
Q

D-Tubocurarine

A

Non-selective, non-depolarising nicotinic receptor antagonist, charged therefore administered IV, leads to flaccid paralysis - action requires 70-80% of receptors to be blocked however

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36
Q

Atracurium

A

Non-depolarising selective antagonist for the NMJ nicotinic receptor, quaternary amide therefore IV, inhibits the production of tetanus following sustained stimulation = tetanic fade achieved by blocking auto transmitters required for +ve feedback on transmitter release
Ester therefore broken down through spontaneous hydrolysis

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37
Q

Panacuronium

A

Non-depolarising selective antagonist for the NMJ nicotinic receptor, quaternary amide therefore IV, inhibits the production of tetanus following sustained stimulation = tetanic fade achieved by blocking auto transmitters required for +ve feedback on transmitter release
Secreted by the kidney, longer acting that atracurium

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38
Q

Decamethonium

A

Depolarising blocker for the nicotinic NMJ

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39
Q

Suxamethonium

A

Depolarising blocker selective for the nicotinic NMJ, short lived ester, can be broken down via BuAChE, used during intubation
1-2% of population mutation in enzyme required for breakdown, can lead to increase in plasma K+ an hence arrhythmia

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40
Q

Carbachol

A

Non-selective cholinergic receptor agonist (muscarinic and nicotinic)

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41
Q

Methacholine

A

Non-selective cholinergic receptor agonist (muscarinic and nicotinic) + isomer broken down by AChE

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42
Q

Cevimeline

A

Muscarinic ACh M3 Selective agonist, used to increase salivation in Sjogren’s syndrome

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43
Q

McN-A-343

A

Muscarinic ACh M1 selective agonist, tissue selective stimulator at ganglionic neurones

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44
Q

Pilocarpine

A

Non-selective muscarinic agonist, used in the treatment of glaucoma, administered via eye drops, causes contraction of colliery muscles and hence opening of clean of schelem

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45
Q

Ipratropium

A

Non-selective muscarinic antagonist, quaternary compound, used in the treatment of asthma

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46
Q

Atroprine

A

Non-selective muscarinic antagonist, dilates pupils, decreases glandular secretions, decreases GI motility, and increases heart rate

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47
Q

Benzilylcholine (mustard)

A

(Irreversible) Non-selectove muscarinic antagonist

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48
Q

Pirenzepine

A

M1 Muscarinic selective antagonist, antisecretory agent in the treatment of gastroduodenal ulcers, acts on the intramural nerves rather than the oxyntic cells directly

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49
Q

Tripitramine

A

M2 Muscarinic selective antagonist

50
Q

Gallamine

A

M2 Muscarinic selective antagonist

51
Q

Darifenacin

A

M3 Muscarinic selective antagonist, used in bladder incontinance

52
Q

Bethanochol

A

Non-selective muscarinic agonist, used in badder dysfunction acts to reduce urinary retention

53
Q

Hyoscine

A

Non-selective muscarinic antagonist, dilates pupils, decreases glandular secretions, decreases GI motility, and increases heart rate

54
Q

Endrophonium

A

Anti-Cholinesterase - short length of action, forms reversible ionic interactions, quaternary ammonium, binds to the anionic site of the enzyme therefore selective for ACeE
Used to diagnose myasthenia gravis and causes a slight increase in muscle tension generation

55
Q

Neostigmine

A

Anti-cholinesterase - Medium length of action, acts as a suicide inhibitor by forming weak covalent bonds, carbomic acid ester, binds to the esteratic site and carbomoylates the enzyme, the enzyme is regenerated slowly
Used IV to reduce neuromuscular blockade after surgery and orally to treat myasthenia gravis

56
Q

Physotigmine

A

Anti-cholinesterase - Medium length of action, acts as a suicide inhibitor by forming weak covalent bonds, carbonic acid ester, binds to the esteratic site and carbomoylates the enzyme, the enzyme is regenerated slowly, used in the treatment of glaucoma - seen to make the ciliary muscles contract

57
Q

Pyridostigmine

A

Anti-cholinesterase - Medium length of action, acts as a suicide inhibitor by forming weak covalent bonds, carbonic acid ester, binds to the esteratic site and carbomoylates the enzyme, the enzyme is regenerated slowly, used in the treatment of mysathenia gravis

58
Q

Dyflos

A

Anti-cholinesterase - Long length on action, forms irreversible strong covalent bonds with the serine residues in the esteratic site
Organophosphorus compound, used in the treatment of glaucoma, long term exposure can lead to demyelination as inhibit an ester in the myelination process,short term exposure can also lead to death through cholinergic overdose - convulsions and respiratory depression

59
Q

Malathion

A

Anti-cholinesterase - Long length on action, forms irreversible strong covalent bonds with the serine residues in the esteratic site
Organophosphorus compound, used as an insecticide to kill lice, long term exposure can lead to demyelination inhibit an ester in the myelination process, short term exposure can also lead to death through cholinergic overdose - convulsions and respiratory depression

60
Q

Tacrine

A

Anti-Cholinesterase - Short length of action, reversible covalent bonds, non-selective between AChE and BuAChE, used in the treatment of Alzhimers disease, uncharged therefore can cross the blood brain barrier

61
Q

Donezepil

A

Anti-cholinesterase - short length of action, forms non-covalent bonds to enzyme, selective for AChE, similar action to tacrine but has fewer peripheral side effects

62
Q

Sugammadex

A

Steroidal cyclodextrin, acts to remove neuromuscular blockage following surgery, binds to blocker forming and inactive complex on the plasma and is the excreted in the urine

63
Q

Praildoxime

A

Can reverse the inhibition of organophosphorus compounds, contains an oxide group which is a strong nucleophile into close proximity to the phosphorylated serine causing the phosphate group to be transferred, only works a few hours following inhibition as the complex becomes ages

64
Q

A-Methyltyrosine

A

Competitive inhibitor of tyrosine hydroxylase therefore reduced all catecholamine production

65
Q

L-DOPA

A

Used as a Dopamine replacement in the treatment of Parkinson’s disease - a substrate that avoids the rate limiting TOH step

66
Q

Carbidopa

A

Inhibitor of DOPA decarboxylase, often used in conjunction with L-DOPA to prevent catecholamine production in the periphery as cannot cross BBB

67
Q

Droxidopa

A

Under clinical trials for the treatment of Neurogenic Arthrostatic hypotentsion - a condition associated with reduced peripheral Na and Adrenaline
Can be converted into catecholamines via DOPA decarboxylase

68
Q

Disulfiram

A

Inhibitor of Dopamine B-Hydroxylase (also inhibits aldehyde dehydrogenase) used in the treatment of alcohol abuse, functions through chelating the essential Cu ion in the enzyme, induces vomiting

69
Q

Methyldopa

A

False transmitter for catecholamine production, taken up into the nerve terminal in the place of tyrosine and converted into a-methylnoradrenaline
Less responsive at A1 but more response at A2 receptors

70
Q

Reserpine

A

Inhibits the vesicular monoamine transporter (VMAT2) responsible for the packaging of NA into synaptic vesicles, almost irreversibly binds to amine binding site, also causes long lasting depletion of NA stores and causes vesicular leak - recovery requires synthesis of new vesicles
Used to have clinical use as anti-hypertensive but causes physiological depression

71
Q

Tyramine

A

Indirectly acting sympathomimetic amine - taken up into the nerve terminal where it acts to displace NA from the vesicles into the cytoplasm where it is either broken down via MAO of transported into the synaptic clef via NET stimulating post synaptic membrane…
Found in wine, cheese and marmite - causes the ‘cheese effect’ can cause temporary increase in blood pressure
Can also be converted via Dopamine B-Hydroxylase into Octopamine which acts as a false transmitter
Tachyphylaxis

72
Q

Ephendrine

A

Indirectly acting sympathomimetic amine - used as a nasal decongestant
Tachyphylaxis

73
Q

Dexamphetamine

A

Indirectly acting sympathomimetic amine, weak inhibitor of MAO (a-methyl group prevents its breakdown), is itself taken up into the synaptic vesicles where it acts as a weak base reducing the pH and therefore reducing NA storage
Tachyphylaxis

74
Q

Ritalin

A

Indirectly acting sympathomimetic amine

Tachyphylaxis

75
Q

MDMA (Ecstasy)

A

Indirectly acting sympathomimetic amine, also acts upon 5-HT2 receptors
Tachyphylaxis

76
Q

Guanethidine

A

Inhibits NA release from pre-synaptic terminal when stimulated by AP, it odes not inhibit spontaneous release, thought to be as a result of action on the K+ or VGCC causing hyperpolarisation
High doses can act as indirectly acting sympathomimetic amine
Taken up into nerve terminal via uptake 1

77
Q

Bretylium

A

Inhibits NA release from pre-synaptic terminal when stimulated by AP, it odes not inhibit spontaneous release, thought to be as a result of action on the K+ or VGCC causing hyperpolarisation
High doses can act as indirectly acting sympathomimetic amine
Taken up into nerve terminal via uptake 1

78
Q

Cocaine

A

Inhibits the action of NET - transporter for uptake 1 into presynaptic cells

79
Q

Imipramine

A

Tricyclic antidepressant, inhibits the action of NET - transporter for uptake 1 into presynaptic cells, also blocks serotonin and adrenaline uptake

80
Q

Amitryptyline

A

Tricyclic antidepressant, inhibits the action of NET - transporter for uptake 1 into presynaptic cells, also blocks serotonin and adrenaline uptake

81
Q

Fluoxetine

A

Inhibits the serotonin 5-HT2 transporter, new generation of antidepressants

82
Q

Normetanephrine

A

Inhibits ENT or OCT3 Uptake 2 transporters into the postsynaptic cell

83
Q

Phenoxybenzamine

A

Irreversibly inhibits ENT or OCT3 involved in uptake 2

84
Q

Clogiline

A

Selectively inhibits MAO-A, used in the treatment of depression

85
Q

Selegiline

A

Selectively inhibits MAO-B used in the treatment of Parkinson’s disease

86
Q

Tranylcypromine

A

Irreversibly inhibits MAO (non-selective) used in the treatment of refractory depression

87
Q

Encatapone

A

Inhibits COMT, used in the treatment of Parkinson’s

88
Q

Mirabegron

A

Selective B3 adrenoceptor agonist

89
Q

Bupranolol

A

Selective B3 adrenoceptor antagonist

90
Q

Phenylepherine

A

Selective A1 adrenoceptor agonist, used to raise blood pressure in acute hypotension

91
Q

MethlyINA

A

Selective A2 adrenoceptor agonist

92
Q

Clonidine

A

Slightly selective A2 adrenoceptor agonist, acts on the hindbrain as an anti-hypertensive

93
Q

Xylazine

A

Selective A2 adrenoceptor agonist, used as a sedative in veterinary medicine

94
Q

Salbutamol

A

Selective B2 adrenoceptor agonist, asthma

95
Q

Dobutamine

A

Selective B1 adrenoceptor agonist, used in cariogenic shock

96
Q

Phentolamaine

A

Non-selective A-adrenoceptor antagonist

97
Q

Phenoxybenzamine

A

Non-selective A-adrenoceptor antagonist

98
Q

Prazosin

A

Selective A1-adrenoceptor antagonist

99
Q

Yohimbin

A

Selective A2-adrenoceptor antagonist

100
Q

Idazoxan

A

Selective A2-adrenoceptor antagonist

101
Q

Propanolol

A

Non-selective B-adrenoceptor antagonist

102
Q

Atenolol

A

Selective B1-adrenoceptor antagonist, used during the removal of a phaeochromacytoma

103
Q

Butaxamine

A

Selective B2 adrenoceptor antagonist

104
Q

Labetalol

A

Non-selective adrenoceptor (A+B) antagonist, 4 different isomers, used to treat hypertension in pregnancy, third-generation beta-blocker

105
Q

Xylometazoline

A

Non-selective A-adrenoceptor agonist, used to relive nasal congestion

106
Q

Tamsulosin

A

Selective A1-adrenoceptor antagonist, used in begin prostatic hyperplasia - relaxes smooth muscle in prostrate

107
Q

Carvedilol

A

Third generation beta-blocker, combines antagonism with vasodilation

108
Q

Nebivolol

A

Third generation beta-blocker, combines antagonism with vasodilation

109
Q

Ergotamine

A

Ergot Alkaloid derived from fungus, used in the treatment of migraines due to action on 5-HT2 receptors, when ingested causes St-Anthony’s fire = intense peripheral vasoconstriction ca lead to gangrene

110
Q

Suramin

A

P2X ATP receptor inhibitor

111
Q

Caffeine

A

A1 Adrenoreceptor antagonist, prevents the induction of sleep, also inhibits phosphodiesterase’s increasing rate and force of contraction

112
Q

Dipyramidamole

A

Inhibits Adenosine uptake (and therefore inactivation) into cells, potentiates its response

113
Q

glycerol Trinitrate

A

NO donor, used to cause vasodilation and relaxation of smooth muscle

114
Q

Isorbide Dinitrate

A

NO donor, used in the treatment of angina

115
Q

Sidenafil

A

Selective inhibitor for Phosphodiesterase - 5 which selectively breaks down C-GMP, used in the treatment of impotence

116
Q

Amyl Nitrate

A

Used in the treatment of angina, administered through inhilation, acts to lower cardiac oxygen demand, causes relaxation of anal sphincter however

117
Q

L-NMMA

A

Non-selective NOS inhibitor

118
Q

L-NAME

A

Non-selective NOS inhibitor

119
Q

7-NI

A

Selective nNOS inhibitor

120
Q

L-NIO

A

Selective iNOS inhibitor

121
Q

Assymetic dimethylamine

A

Endogenous inhibitor of NOS, synthesised during post-translational methylation, elevated in renal failure, feedback regulator for NOS production

Pharmocology (10 decks)

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