Postsynaptic Receptors Flashcards

1
Q
CONVERSION  of a message from one form (neurotransmitters)
into another (increased membrane conductance. Is know as what?
A

Transduction

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2
Q

The transduction mechanism is described as direct-gating

(or ligand-gating). This is used by which type of receptors?

A

Ionotropic

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3
Q

The transduction mechanism is described as indirectgating. This is used by which type of receptors?

A

Metabotropic-type receptors

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4
Q

Ionotropic-type receptors uses ___ gating that neurotransmitter binding to the receptor
causes a CONFORMATIONAL CHANGE in the ion channel complex
to open the gate and provide conductance across the
membrane for a selected ion, or ions.

A

Direct

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5
Q

The neuromuscular ACh receptor is classified as _____.

A

Nicotinic cholinergic

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6
Q

two molecules of ACh must bind
to the two ___subunits to activate
the receptor

A

Alpha

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7
Q

The selectivity filter of ___ is cation selective,

providing conductance for both Na+ and K+

A

Neuromuscular junction

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8
Q

INDIRECT GATING is used by what type of ___ receptors?

A

Metabotropic-type

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9
Q

Is there an measurable delay in metabotropic receptors compared to ionotropic receptors?

A

YES.

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10
Q

With ___ receptors, the extracellular signal (neurotransmitter)
must be brought into the cell (“internalized”) to effect the functional
response

A

Metabotropic

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11
Q

What is the first messenger that takes extracellular message into the cell?

A

Neurotransmitter

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12
Q
  1. ___ (→ “first messenger”) binds to
    the receptor
  2. the ligand-activated receptor complex activates a
    G-protein (_____)
  3. the activated G-protein translocates along the
    membrane to activate a _____.
  4. the activated primary effector generates an
    intracellular _____.
  5. the second messenger activates a _____.
A
  1. neurotransmitter
  2. transducer
  3. primary effector
  4. second messenger
  5. secondary
    effector
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13
Q

Is second intracellular?

A

Yes.

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14
Q

What is the function of the second messenger?

A

Process the message (internalizing) brought into intracellular side from extracellular side.

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15
Q

What enzyme serves as the primary effector?

A

Adenylyl cyclase

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16
Q

What will activate adenylyl cyclase?

A

G-protein

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17
Q

When G- protein is in an inactive state, adenylyl cyclase is___.

A

INACTIVE (G-protein will not activate adenylyl cyclase)

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18
Q

The signaling cascade starts with ___ binding to its
receptor, which activates the ___, leading to activation of the
___ and generation of the second messenger.

A
  1. neurotransmitter
  2. G-protein
  3. primary effector
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19
Q

The ligand-receptor complex
continues to reactivate inactive Gproteins until the neurotransmitter
_____ from the receptor

A

detaches

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20
Q

To cause the gate on an ion channel to open, there must be an
intracellular signal … this is provided by ___ of the
channel.

A

phosphorylation

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21
Q

Attaching an inorganic phosphate (Pi
) to an internal segment of the
membrane-spanning channel. This is known as?

A

Phosphorylation

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22
Q

When a channel is DE-phosphorylated, what happens?

A

Channel will close

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23
Q

When a channel is phosphorylated, what happens?

A

Channel will open

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24
Q

What is the second messenger known as?

25
The intracellular target for cAMP (the | second messenger) is cAMP-dependent kinase which is known as_____.
protein kinase A, or PKA
26
phosphodiesterases ___ cAMP.
inactivate
27
protein phosphatases remove | _____from proteins.
phosphate groups
28
cAMP is activated by___.
Activated adenylyl cyclase.
29
Adenylyl cyclase is activated by___.
G- protein
30
G-protein is activated by___.
Neurotransmitter, stimulating postsynaptic receptor
31
When neurotransmitter detaches from postsynaptic receptors we want the ion channels to ___.
Close: signaling communication is over.
32
Why do we want to remove neurotransmitter from postsynaptic receptor after message is conveyed?
So it won't keep repeating the same message over and over again.
33
Ionic channel wont close unless _____.
Dephosphorylated via protein phosphatases
34
Another G-protein coupled signaling mechanism that is | commonly employed in neurons is the _____.
Phosphoinositol system
35
phospholipase Cβ (PLC) is the primary | effector activated by the_____.
G-protein | subunit Gq
36
``` Both IP3 (inositol trisphosphate) and DAG (diacylglycerol) are generated as _____through cleavage of phosphatidylinositol bisphosphate (PIP2) by phospholipase C ```
Second messengers
37
DAG (diacylglycerol) will bind with the _____ of protein kinase C
Regulatory subunit
38
IP3 signals via a receptor along the _____ for that organelle to release Ca++ into the cytosol
Endoplasmic reticulum
39
Secondary Effectors: | Protein kinase C is activated by ___.
DAG
40
Ca++/calmodulin dependent protein kinase is | activated when Ca++ binds to ___
Calmodulin
41
The effectiveness of signaling through the calcium-calmodulin pathway is based upon an acute increase in the ______.
Cytosolic Ca++ concentration
42
The mechanism for indirect activation of a K+ channel via a _____receptor.
Muscarinc | acetylcholine
43
Nicotinic cholinergic | receptors are ___ gated
Directly
44
What is the first messenger, receptor, and second messenger(s) in the cAMP system?
Norepinephrine; Beta-adrenergic receptor; cAMP
45
What is the first messenger, receptor, and second messenger(s) in the Phosphoinositol system?
ACh; Type 1 Muscarinic ACh receptor; IP3 and DAG
46
What is the first messenger, receptor, and second messenger(s) in the Direct G protein-gating system?
ACh; Type 2 Muscarinic ACh receptor; G protein-gated K+ channel
47
In general, G-proteins function as a molecular _____ operated through binding and then release of neurotransmitter from its postsynaptic receptor.
on – off switch
48
α-GDP is active/inactive?
Inactive
49
α-GTP is active/inactive?
Active
50
_____ receptors: ion channels DO NOT respond immediately to neurotransmitter binding and releasing from the receptor.
Metabotropic
51
_____ receptors: ion channels RESPOND immediately to neurotransmitter binding and releasing from the receptor.
Ionotropic
52
The state of ___ to determine whether the channel is open or closed.
Phosphorylation
53
Protein kinase A and phosphoprotein phosphatase-1 are _____ signals that are regulated by _____ signaling via membrane receptors.
Intracellular; external signaling
54
The “strength” of phosphorylation in response to cAMP is: _____ when PP-1 is inhibited.
Enhanced
55
The “strength” of phosphorylation in response to cAMP is: _____ (lessened) when PP-1 is active.
Diminished
56
PP-1 (phosphatase-1 ) is regulated via another intracellular signaling molecule, _____.
Inhibitor-1
57
``` _____ modulates (lessens) channel phosphorylation in response to cAMP by causing the DISINHIBITION of PP-1 ```
calcineurin
58
Calcineurin is activated by?
Calcium