Ligand gated ion channel receptors and GPC receptors Flashcards

1
Q

Cationic channels are usually excitatory and often lead to ________

A

depolarisation

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2
Q

Anionic channels generally exert _______ effects once opened

A

inhibitory

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3
Q

The selectivity of ion channels depends on ________ of the transmembrane space and the ________ that line the channel

A

diameter

amino acids

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4
Q

Where are nicotinic receptors found?

A

Neuromuscular junctions

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5
Q

Other than the nicotinic acetylcholine receptor, which other receptor has 5X fold symmetry?

A

GABA (gaba amino butyric acid)

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6
Q

Upon activation, the GABA receptor conducts ____ resulting in hyperpolarisation of the neuron

A

Cl-

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7
Q

What is the diameter of each subunit of acetylcholine?

A

2nm

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8
Q

What is the diameter of a molecule of acetylcholine?

A

9nm

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9
Q

What are the two subtypes that nicotinic receptors are classified into?

A

Muscle type

neuronal type

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10
Q

How many subunits does the nACh receptor have and in what ratio?

A

5 subunits: a, B, Y and s in a 2:1:1:1 ratio

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11
Q

How does the poison function of curare work?

A

It inhibits the nACh receptor (found at neuromuscular junctions). The poison causes weakness of skeletal muscles and at a high dose, eventual death due to paralysis of the diaphragm and cessation of breathing

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12
Q

How do local anaesthetics such as Lidocaine work?

A

Blocks ion channels and hence the passage of Na+ and reduces pain perception

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13
Q

How do sedatives such as Benzodiazepines work?

A

Increase the ability of GABA to conduct Cl- across membranes. This drives membrane potential away from its threshold for activation. This reduces communication between neurons = sedation

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14
Q

Sympathetic and parasympathetic nervous systems are regulated by ligand gated ion channels. True or false?

A

False - regulated by GPC receptors

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15
Q

30% of all drugs work by binding GPC receptors. True or false?

A

True

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16
Q

GPCRs are normally activated by hormones or neurotransmitters. True or false?

A

True

17
Q

Which hormone and which neurotransmitter switch on the beta adrenergic receptor?

A

adrenaline

noradrenaline

18
Q

What is the main clinical use of adrenergic agonists?

A

Treatment of asthma

19
Q

What is the main clinical use of adrenergic antagonists?

A

B-blockers for angina

20
Q

How is the signal of a GPC receptor cancelled?

A

G-alpha subunits have intrinsic GTPase activity (GTP is hydrolysed to GDP)

21
Q

How do nicotinic and muscarinic acetylcholine receptors differ in where they are found?

A

Nicotinic are found on skeletal muscle

Muscarinic found on smooth muscle

22
Q

What is a clinical use for muscarinic agonists?

A

Treatment of glaucoma

23
Q

What is a clinical use for muscarinic antagonists?

A

Treatment of Parkinson’s disease