Ligand Gated Ion Channels Flashcards

1
Q

T/F: Ligand gated ion channels cannot initiate depolarization.

A

False

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2
Q

T/F: Ligand gated ion channels can have Excitatory Postsynaptic Potential (EPSP) or Inhibitory Postsynaptic Potential (IPSP)

A

True

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3
Q

Cholinergic Neurotransmitters

A

transmit Acetylcholine

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4
Q

Purine Neurotransmitters

A

transmit ATP

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5
Q

Biogenic Amine Neurotransmitters

A

transmit serotonin

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6
Q

Amino Acid Neurotransmitters

A

transmit Glutamate

transmit Glycine, GABA

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7
Q

Cationic channels affect EPSP or IPSP?

A

EPSP

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8
Q

Anionic channels affect EPSP or IPSP?

A

IPSP

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9
Q

Four examples of Cationic channels and what they transmit

A
  • Cholinergic = acetylcholine
  • purines = ATP
  • biogenic amines = serotonin
  • amino acids = glutamate
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10
Q

Example of anionic channels and what they transmit

A

amino acids = glycine, GABA

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11
Q

Purine Receptor Subunit

A
  • P2X receptors
  • nonselective cation channels
  • cytosolic N & C termini w/ 1 extracellular loop (loop thought to contain ligand binding spot)
  • widely distributed in CNS, PNS, and neuroglia
  • may have role in neuropathic pain
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12
Q

Acetylcholine (nicotinic), GABAa, and Glycine Receptors

A
  • 4 membrane spanning domains per subunit
  • 5 subunits make 1 channel
  • extracellular N & C termini
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13
Q

Subunits of nAch Receptors

A
  • 2 alpha
  • beta
  • gamma
  • delta
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14
Q

Subunits of GABAa Receptors

A
  • 2 alpha
  • 2 beta
  • gamma
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15
Q

Subunits of Gly Receptors

A
  • 3 alpha

- 2 beta

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16
Q

What is the primary inhibitory neurotransmitter in the brain and spinal cord?

A

GABA

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17
Q

What is the inhibitory neurotransmitter in the brain and spinal cord that affects antagonistic muscles?

A

Glycine

18
Q

Glutamate Receptor subunits

A
  • 3 transmembrane segments
  • a predicted ‘P’ loop
  • 4 or 5 subunits per channel
  • All receptor types permeant to Na+ and K+
19
Q

Nicotinic Acetylcholine Receptor shape

A

heteropentamer

possibilities of:

  • alpha 1-9
  • beta 1-4
  • gamma
  • delta
  • epsilon
20
Q

Subunits of an adult muscle nicotinic acetylcholine receptor

A
  • 2 alpha
  • beta 1
  • gamma
  • delta
21
Q

Subunits of a neonatal muscle nicotinic acetylcholine receptor

A
  • 2 alpha
  • beta 1
  • gamma
  • epsilon
22
Q

Subunits of a nerve nicotinic acetylcholine receptor

A
  • 2 alpha

- 3 beta

23
Q

Agonists of nAch Receptors

A
  • nicotine
  • carbamylcholine
  • succinylcholine
  • acetylcholine
  • lemamisole
  • pyrantel target helminth homolog
24
Q

Antagonists of nAch Receptors

A
  • trimethaphan
  • alpha Bungarotoxin
  • curare
25
Q

What is responsible for binding to acetylcholine in nAch Receptors?

A

alpha subunits

26
Q

Why is alpha Bungarotoxin considered functionally irreversible?

A

takes 20 minutes to release from binding site

not “real time” for physiological purposes

27
Q

How many subunits are there per receptor for nAchR, GlyR, HT3R, and GABAa receptors?

A

5 subunits

28
Q

Extracellular Subunit Topology

A
  • Both N and C terminus
  • consensus sites for glycosylation
  • 2 cystine residues separated by 13 aa, that form a disulfide bond
  • responsible for ligand binding
29
Q

Transmembrane Subunit Topology

A

-4 segments (M1,M2,M3,M4)

30
Q

In the transmembrane subunits, what is responsible for ion selectivity?

A

M2

M2 is contributed by each of the subunits forms aqeous pore/ ion channel.

31
Q

Intracellular Subunit Topology

A
  • responsible for intracellular processing, targeting, and anchoring
  • natural mutations have occurred here and disease have been assoc. with these mutations
32
Q

Do Glutamate and Purinergic receptors have the same topology as nAchR, GlyR, HT3R, and GABAa Receptors?

A

They do NOT share the same topology

33
Q

How many subunits are there in serotonin HT3 Receptors?

A

5 - It’s a heteropentamer

A, B, C, D, and E exist

34
Q

Agonist of serotonin HT3 Receptor

A

2-methyl serotonin

35
Q

Antagonists of serotonin HT3 receptor

A
  • Dolasetron
  • Ondasetron
  • Granisetron
  • Palonosetron
  • Alosetron (withdrawn)
36
Q

nAchR, Receptor targeting, and anchoring

neuromuscular junction
[5 steps]

A
  1. Post-synaptic cell synthesizes rapsyn
  2. Rapsyn interacts with intracellular domain of nAchR
  3. At same time, nerves secrete agrin
  4. Agrin interacts with dystroglycan
  5. Rapsyn interacts with beta dystroglycan and with cytoskeleton
37
Q

What does rapsyn do in regards to the neuromuscular junction?

A

causes clumping of receptors

38
Q

What does agrin do in regards to the neuromuscular junction?

A

provides targeting cell for clumped receptors

39
Q

T/F: Ligand-gated channels respond to chemical messenegers

A

True

40
Q

What accounts for localization, activity, conductance, and pharmacology in many ligand-gated channels?

A

common structural motif

41
Q

Acetylcholine- and serotonin-gated channels are _______ in nature.

A

excitatory

ie - strongly depolarizing

42
Q

T/F: Ligand-gated channels provide examples of cooperativity and competitive and noncompetitive inhibition.

A

True