Ion Channel Receptors Flashcards

(40 cards)

1
Q

What are Ion Channel Receptors?

A

Type of Membrane bound protein that allows the selective passage of ions across the cell membrane in response to stimulus following the electrochemical potential gradients

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is a malfunction of Ion channel, either gain or loss of function called?

A

Channelopathies

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What are the differences between Ion channel receptors and other membrane receptors?

A
  1. Mechanism of Action: Direct ion flow through a channel vs Indirect signalling via second messengers
  2. Response time: Fast (milliseconds) vs Slower (seconds to minutes)
  3. Biological role: Rapid, synaptic transmission, muscle contractions vs Long term modulation of cell function
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What are the differences in mechanism of action of Ion channels vs others?

A

Direct Passage of Ion flow through a channel vs indirect signalling via secondary messengers

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What are the differcnes in Response time between ion channels and others?

A

Millisseconds vs Minutes/seconds

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What are the differcens in Biological role between ion channels and others>?

A

Rapid Synaptic Transmissions, muscle contractions vs Long term modulation of cell function

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Where do Ion channel receptors occur in?

A

Excitable cells: Neurons -neuronal signalling (action potential propagation)
Muscle Cells - muscular contractions

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What is an electrochemical gradient?

A

Conductance, a comination of 2 forces thgat drive hte movement of ions across a mebrane

comprising of
1. Chemical gradient
2. electrical gradient

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What charge is usually the internal of the cell

A

Negative

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What is the equilibrium potential of Na+?

A

+60mV

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What is the equilibrium potential of K+?

A

-80mV

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is Resting potential?

A

the membrane potential difference at which there is no net current and no net solute flow

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Where does resting potential come from?

A

Determined by the balance of equilibrium potentials for K+ and Na+
Represents an average effect of all leaky K+ an Na+ channels

if only K+ leaky channels were present, the potential would rapidly reach -80mV
if only na+ leaky channels present, the potential would rapidly reach +60mV

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is the resting potential and why is that the value?

A

The resting potential is -70mV , which is alot closer to K+ (-80), insetad of the supposed average fo both potential (-10)

This is becasue K+ channels outnumber Na+ channel 14:1

Thus the resting potential is far more influenced by K+ leaky channels than Na+

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What is an action potential?

A

A transient short lasting reversal in membrane potential triggering a wave of electrical activity that propgates across the membrane

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What are the steps of an action potential formation?

A
  1. Resting Potential (-70mV) - Na+/K+ channels are closed, maintained by Na+/K+ pump
  2. Stimulus and depoalrisation towards threshhold - A stimulus from sensory cells or another neuron causes partial depolarisation
    - if threshhold potenial of -55mV is reached, action potential is triggered
  3. Rapid Depoalrisation
    Na+ channeles open, allowing Na influx into the cell, making membrane more positive (+30mV)
  4. Peak and Repolarisation- At the peak of action potential, Na+ channels inactiavte, K+channels open, K+ efflux, restoring negativity and repoalrisation
  5. Hyperpolarisation and refractory period
    Excess K+ efflux causes hyperpoalrisation (-80mV)
    Neuron enters refractory period where it cannot fire another action potential (absolute) or require a stronger than usual stimulus (relative)
  6. Restoration of resting potential
    K+ channels close, Na+/K+ reset resting potential -70mV
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What are the 3 structural features of Ion channels?

A
  1. Selectivity filter - determine which ions can pass throufgh
  2. Gating Mechanism - Control opening and closing in response to external stimuli, regulating membran permeability
  3. Activation sensors - Controlled by elctrical chemical of mechancial stimuli
18
Q

What are the characteristics of Ion Channels?

A
  1. Membran spanning proteins with water filled pores
  2. Ion Selectivity
  3. Rate and direction driven by electrochemical gradient
  4. Gating mechanism
  5. Activity is regualted by phosphorylation
19
Q

What are the 4 types of ion channel receptors?

A
  1. Leakage
  2. Ligand
  3. Voltage
  4. Signal
20
Q

What are leakage channels?

A
  1. Always open, allowing passive ion movement down the concentration gradient
  2. K+ and Na+ leaky channels
    -K+ efflux maintains neuron’s negative resting potential (-70mV)
    Na+ influx partially ofsets K+ movement - prevents excessive hyperpolarisation
21
Q

What are voltage gated ion channels?

A

Open or close in response to changes in membrane potential
selective for certain ions
Found in neurons, muscles cardiac cells

Axons- responsible for action potential generation and propoagation

22
Q

What are Ligand gated ion channels?

A

Open in response to ligand (chemical) binding
Allow selective ion flow

23
Q

What are Signal Gated Channels?

A

Open and close in response to intracellular signalling molecules, not direct ligand binding
linked ot GPCR

24
Q

What is the purpose of Na+ voltage gated channels?

A

Open for Depolarisation, initaiting action potential

25
What is the purpose of K+ voltage gated channels?
Open for Repolarisation, restoring action potential
26
How do blockage of Na+ voltage gated channels distrupt nerve signal transmission?
1. Increases excitation threshold, neurons less likely to fire 2. Slowing impulse conduction, reducing nerve signal speed 3. Decrease rate of rise of amplitude of acton potential, weakening nerve excitability 4. Prevent propagation when Na+ current is bloced at critical part of nerve
27
What is an exmaple of clinical use of Na+ channel blocker?
Lidocaine - local and regional anesthesia, to inhibit sensory nerve signals, preventing pain perception
28
What are voltage gated L-Type Calcium Channel Blockers?
Play a role in heart and vascualr system, 1. Regulate cardiac contractability - decreasing LTCC leads to weaker heart contractions 2. Controls Vascular tone - LTCC activation causes vasoconstriction Reduce Ca2+ Influx into muscle cells - vasodilation - decrease blood pressure - decrease heart rate
29
What is the clinical use of LTCC blockers (CCB)?
Verapamil - Treat hypertension, angina, arrythmias by reducing heart contractability and heart rate
30
What are LGIC?
Ligand gated Ion Channels - ionotropic receptors, transmembrane proteins that open upon binding of nerutransmitter or ligand crucial role in rapid synaptic transmission 3-5 subunits, either heteromultimer, or homomultimer 2 main functional domains 1. Ligand binding domain - extracellular, lock and key 2. Chanel Pore
31
What is GABAa receptor - chloride channel complex?
Key inhhibitory receptor in central nervous system Primary moelcualr target for modern hypnotics - Benzodiazepine
32
What is the mechanism of action of GABAa receptor chloride channel complex?
higher chloride conc outside ensures insward flow when channel opens, reducing neruonal excitability Activation causes Chloride influx - hyperpoalrisation and neuronal inhibition Selective Agonist : Isoguavacine
33
What is Isoguavacine?
Selective Agonist for GABAa receptor chloride channel complex, enhances receptor activation ,leading ot more Cl influx, and hyperpolarisation and reduced neuronal excitability
34
What is Benzodiazepenes?
Enhance GABA action by increasing frequency of GABA induced channel opening, leading to greater inhibition of CNS Anti anxiety, sedative, anti epiletptic, general anasthesia
35
What is Phenobarbitol?
Increase both frequency and duration of Cl channel opening, causing prolonges neuronal suspension
36
What are nicotinic acetylcholine receptors?
Ligant gated ion channels activated by acetylcholine Found in skeletal muscles, neurons and autonomic ganglia Mediate fast synaptic transmission
37
What is a-bungarotoxin?
A selective antagonist, binding irrervesibly and blocking nicotnicn recptor function
38
What is Long QT Syndrome?
A cardiac Channelopathy Mutation in Na+ and K+ channels causing Long QT, increasing susceptibility to cardiac arrythmia Mutation of K+ channel, results in loss of function and reduced K+ current, delaying repolarisation Dstrupts normal heart rhythm
39
What is Cystic Fibrosis?
Genetic disease with mutation in CFTR chloride channel CFTR dysdfunction leads to impaired chloride transport in secreatory epithelial cells in Lungs, defective Cl- conductance leads to dehydration of airways ,causing thick mucus buildup ,promoting bacterial growth, increasing risk of chronic infections
40
What is the treatment of Cystic Fibrosis?
Ivacaftor (CFTR Potentiator) improves CFTr fucntion by enhancing possibility of Cl channel opening in specific mutations