ion channels 2 Flashcards

1
Q

IKto

A
  1. – (Kv4.3 tetramer + KChiP2)

2. voltage-dependent inactivation

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2
Q

IKr

A
  1. (HERG tetramer + miRP1)

2. “rapid” delayed rectifier

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3
Q

IKs

A
  1. (KvLQT1 tetramer + minK)

2. “slow” delayed rectifier

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4
Q

Time-dependent cation current

A
  1. If (or Ih)
  2. (HCN tetramer)
  3. Evoked by hyperpolarization
  4. Na+ & K+ permeable
  5. Erev ~ -30 mV
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5
Q

Inward Rectifier potassium currents

A
  1. IK1

2. IKACh

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6
Q

IK1

A

(Kir tetramer)

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7
Q

IKACh

A
  1. (GIRK tetramer)
  2. Increased by activation of muscarinic receptors
  3. slows pacemaking
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8
Q

Pacemaker Depol.

A
  1. Turning on of If
  2. Activation of ICa-T
  3. Deact. of IKr & IKs
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9
Q

HERG is an

A

“anti-target” tested in preclinical evaluation of new drugs

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10
Q

HERG produces

A

Ikr

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11
Q

HERG is important for

A

duration of slow and fast APs

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12
Q

Reducing Ikr can cause

A

arrhythmias

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13
Q

HERG is blocked by

A

diverse compounds

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14
Q

in the heart, electrical activity functions to

A
  1. Generates repetitive firing in specialized, “pacemaker” regions
  2. Propagates within the myocardium and via specialized conductive pathways
  3. Serves as a trigger for contraction of the myocardium
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15
Q

The cardiac action potential is the trigger for an

A

increase in the intracellular concentration of calcium ions, which, in turn, causes contraction of the myocardium.

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16
Q

pacemaker cells

A

initiate cardiac AP

slowly depolarize to threshold in the absence of extrinsic input

17
Q

The rate at which a normal heart beats is controlled by

A

pacemaker cells in the sinoatrial node (SA node).

18
Q

The SA node is a

A
  1. cluster of small (7 μm diameter), round and spindle-shaped cells that contain few myofilaments.
  2. automaticity
  3. rhythmicity
19
Q

automaticity

A

cells are spontaneously active

20
Q

rhythmicity

A

will fire action potentials at a frequency of about 100/min

21
Q

The SA node is innervated by

A

both sympathetic and parasympathetic axons.

Ongoing activity in the parasympathetic axons (parasympathetic tone) typically slows the rate at which cells in the SA node fire to 60-80 action potentials/min.

22
Q

overdrive suppression

A

an action potential will spread to them from the SA node before they reach threshold on their own

23
Q

ectopic pacemaker

A

Under abnormal circumstances these cells (or others, especially cells in damaged regions of the myocardium) can take over initiation of the heartbeat

24
Q

Because heart rate is controlled by electrical activity of the SA node, the propagation of this activity to other regions of the heart has to occur such that

A

the two atria contract and relax in a coordinated fashion, that two ventricles contract and relax in a coordinated fashion, and that ventricular contraction occurs during atrial relaxation (and vice versa).

25
Q

High Voltage activated (HVA) types

A
  1. L type

2. neuronal

26
Q

L type channels include

A

CaV1.1, CaV1.2, CaV1.3, CaV1.4

27
Q

Neuronal channels include

A

CaV2.1, CaV2.2, CaV2.3

28
Q

Low voltage activated (LVA) types

A

T type, which includes: Cav3.1, 3.2, 3.3

29
Q

L-type calcium channels containing CaV1.2 are predominant in

A

ventricular and atrial myocardium and cells of the SA and AV nodes and conductive pathways.

30
Q

SA nodal cells also express

A

L-type channels containing CaV1.3.