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?

A

cAMP

25
Q

The intracellular target for cAMP (the

second messenger) is cAMP-dependent kinase which is known as_____.

A

protein kinase A, or PKA

26
Q

phosphodiesterases ___ cAMP.

A

inactivate

27
Q

protein phosphatases remove

_____from proteins.

A

phosphate groups

28
Q

cAMP is activated by___.

A

Activated adenylyl cyclase.

29
Q

Adenylyl cyclase is activated by___.

A

G- protein

30
Q

G-protein is activated by___.

A

Neurotransmitter, stimulating postsynaptic receptor

31
Q

When neurotransmitter detaches from postsynaptic receptors we want the ion channels to ___.

A

Close: signaling communication is over.

32
Q

Why do we want to remove neurotransmitter from postsynaptic receptor after message is conveyed?

A

So it won’t keep repeating the same message over and over again.

33
Q

Ionic channel wont close unless _____.

A

Dephosphorylated via protein phosphatases

34
Q

Another G-protein coupled signaling mechanism that is

commonly employed in neurons is the _____.

A

Phosphoinositol system

35
Q

phospholipase Cβ (PLC) is the primary

effector activated by the_____.

A

G-protein

subunit Gq

36
Q
Both IP3 (inositol trisphosphate) and
DAG (diacylglycerol) are generated as
\_\_\_\_\_through cleavage
of phosphatidylinositol bisphosphate
(PIP2) by phospholipase C
A

Second messengers

37
Q

DAG (diacylglycerol) will bind with the _____ of protein kinase C

A

Regulatory subunit

38
Q

IP3 signals via a receptor along
the _____ for
that organelle to release Ca++ into
the cytosol

A

Endoplasmic reticulum

39
Q

Secondary Effectors:

Protein kinase C is activated by ___.

A

DAG

40
Q

Ca++/calmodulin dependent protein kinase is

activated when Ca++ binds to ___

A

Calmodulin

41
Q

The effectiveness of signaling through the calcium-calmodulin pathway
is based upon an acute increase in the ______.

A

Cytosolic Ca++ concentration

42
Q

The mechanism
for indirect activation of a
K+ channel via a _____receptor.

A

Muscarinc

acetylcholine

43
Q

Nicotinic cholinergic

receptors are ___ gated

A

Directly

44
Q

What is the first messenger, receptor, and second messenger(s) in the cAMP system?

A

Norepinephrine; Beta-adrenergic receptor; cAMP

45
Q

What is the first messenger, receptor, and second messenger(s) in the Phosphoinositol system?

A

ACh; Type 1 Muscarinic ACh receptor; IP3 and DAG

46
Q

What is the first messenger, receptor, and second messenger(s) in the Direct G protein-gating system?

A

ACh; Type 2 Muscarinic ACh receptor; G protein-gated K+ channel

47
Q

In general, G-proteins function as a molecular _____
operated through binding and then release of neurotransmitter
from its postsynaptic receptor.

A

on – off switch

48
Q

α-GDP is active/inactive?

A

Inactive

49
Q

α-GTP is active/inactive?

A

Active

50
Q

_____ receptors: ion channels DO NOT respond
immediately to neurotransmitter binding and releasing
from the receptor.

A

Metabotropic

51
Q

_____ receptors: ion channels RESPOND
immediately to neurotransmitter binding and releasing
from the receptor.

A

Ionotropic

52
Q

The state of ___ to determine whether the channel is open or closed.

A

Phosphorylation

53
Q

Protein kinase A and phosphoprotein phosphatase-1 are _____ signals that are regulated by _____ signaling via membrane receptors.

A

Intracellular; external signaling

54
Q

The “strength” of phosphorylation in response to cAMP is: _____ when PP-1 is inhibited.

A

Enhanced

55
Q

The “strength” of phosphorylation in response to cAMP is: _____ (lessened) when PP-1 is active.

A

Diminished

56
Q

PP-1 (phosphatase-1 ) is regulated via another intracellular signaling molecule, _____.

A

Inhibitor-1

57
Q
\_\_\_\_\_ modulates (lessens) channel phosphorylation in response to
cAMP by causing the DISINHIBITION of PP-1
A

calcineurin

58
Q

Calcineurin is activated by?

A

Calcium