Receptors

Question 1

receptors required for action potential

Answer 1

ligand gated and voltage gated ion channels

Question 2

Neuronal action potentials, after ACh binds to ligand gated ion channel what happens next?

Answer 2

Voltage gated Na+ channel opens THEN a voltage gated Cl-channel opens

Question 3

an action potential starts with a _________ gated ion channel

Answer 3

Ligand gated ion channels

Question 4

leads to action potential, positive ions go into the cell

Answer 4

Excitatory

Question 5

Hyperpolarization, negative ions into the cells

Answer 5

Inhibitory

Question 6

ligand binds to a receptor and activates it

Answer 6

agonist

Question 7

ligand binds to receptor and prevents it from activating

Answer 7

antagonist

Question 8

antagonist that acts on the main binding site

Answer 8

orthosteric antagonist

Question 9

antagonist that acts on an accessory binding site

Answer 9

allosteric antagonist

Question 10

antagonist that physically obstructs ion channel

Answer 10

pore blocker

Question 11

pentamer

Answer 11

cys-loop receptors

Question 12

tetramer

Answer 12

ionotropic glutamate receptors

Question 13

cys-loop receptors

Answer 13

nicotinic ACh receptors
glycine receptors
5HT-3 Receptors (serotonin)
GABA-A receptors

Question 14

ionotropic glutamate receptors

Answer 14

NMDA receptors
Kianate receptors
AMPA receptors

Question 15

inhibitory cys-loop receptors

Answer 15

Glycine

GABA- A

Question 16

excitatory cys-loop receptors

Answer 16

Nicotinic ACh Receptors

5HT-3 (Serotonin) Receptors

Question 17

named fro the loop made by a disulfide bond

Answer 17

cys-loop receptors

Question 18

physical gate of cys-loop receptors

Answer 18

the second transmembrane domain of the ALPHA subunit

Question 19

causes ALPHA subunit to change conformation

Answer 19

agonist binding

Question 20

drugs that act on nAChR

Answer 20

Nicotine

Varenicline (Chantix)

Question 21

drugs that act on GABA-a

Answer 21

Ambien (Zolpidem), Barbituates, Benzodiazepines, Alcohol

Question 22

T/F drugs have distinct binding sites that allow it to effect receptors in a unique way

Answer 22

True

Question 23

drugs that act on NMDA receptors

Answer 23

Ketamine

Question 24

drugs that act on AMPA receptors

Answer 24

Aniracetam (cognition enhancer)

Question 25

nAChR subunits at neuromuscular junction

Answer 25

alpha, beta, gamma, delta

Question 26

subunits at neuronal nAChR

Answer 26

alpha and beta

Question 27

Receptor that pass Na, K, Ca Has non-selective cation channels composed of five subunits ion passage depends on subunits

Answer 27

nAChR

Question 28

drug that causes an UPREGULATION of receptors in response to chronic presence of drug

Answer 28

Nicotine - this is why it is hard to quit smoking

Question 29

ACh binds to _________ subunit

Answer 29

ALPHA

Question 30

not passing ion but ligand is bound

Answer 30

receptor in desensitized state

Question 31

receptor cannot be activated because a ligand is bound

Answer 31

receptor in desensitized state

Question 32

state of receptor when no ligand is bound

Answer 32

closed

Question 33

when ligand is bound and ions are actively passing receptor is

Answer 33

open

Question 34

two things that effect the propensity of a receptor to fall into a desensitized state

Answer 34

1. what agonist is bound to the receptor | 2. the subunit composition of the receptor

Question 35

AMPA, Kainate, NMDA

Answer 35

Ionotropic glutamate receptors

Question 36

only inotropic glutamate receptor that can pass calcium

Answer 36

NMDA

Question 37

the 2nd transmembrane domain forms the ion pore

Answer 37

ionotropic glutamate receptors

Question 38

each subunit has a binding site, but they are not all for glutamate

Answer 38

ionotropic glutamate receptors

Question 39

ALL 4 binding sites of these receptors MUST be occupied for the channel to open

Answer 39

ionotropic glutamate receptors

Question 40

what needs to be bound for NMDA receptors to open?

Answer 40

2 Glutamate, 2 Glycicne

Question 41

What needs to be bound for AMPA receptors to open?

Answer 41

4 Glutamates

Question 42

Gage at which cell can understand how often it is working

Answer 42

NMDA receptor activity

Question 43

_________ receptors are blocked by a _________ ion. This block is _________ dependent.

Answer 43

NMDA Mg++ voltage

Question 44

in long term potentiation how does the NMDA receptor open?

Answer 44

Depolarization of the neuron relieves the Mg+ block and the receptor can open to pass ions

Question 45

in long term potentiation after the NMDA receptor opens what ions are passed?

Answer 45

Ca++ and Na++ come into the cell

Question 46

What specifically leads to more AMPA receptors being inserted onto the synapse?

Answer 46

NMDA receptors pass calcium which ACTIVATES Ca MKII (calcium calmodulin kinase II)

Question 47

in long term potentiation there is also a __________ messenger that goes back to the __________ terminal

Answer 47

Retrograde, pre-synaptic

Question 48

what does having more AMPA receptors on the surface mean?

Answer 48

It is a stronger synapse

Question 49

What signals to the intercellular AMPA receptors to be inserted onto the pre-synaptic terminal?

Answer 49

Calcium Calmodulin Kinase II

Question 50

Coincidence Receptors

Answer 50

NMDA Receptors

Question 51

In long term potentiation first the _______ receptors are activated which then depolarize the neuron and causes the _______ to be relieved and activate the _________ receptors which then allow a __________ influx activating ___________ to signal to the neuron to insert __________ receptors on the surface of the neuron.

Answer 51

``` AMPA Magnesium Pore Blocker NMDA Ca++ and Na+ Calcium calmodulin kinase II AMPA ```

Question 52

GPCR Class A

Answer 52

Adrenergic receptors | Muscarininc ACh receptors

Question 53

GPCR class B

Answer 53

Parathyroid hormone receptor

Question 54

GPCR class C

Answer 54

Metabatropic Glutamate receptors | GABA-b Receptors

Question 55

Excitatory Activate Adenylyl Cyclase increase cAMP

Answer 55

G alpa sub S Receptors

Question 56

Inhibitory Inhibit Adenylyl Cyclase Decrease cAMP

Answer 56

G alpha sub I Receptors

Question 57

Excitatory Activates Phospholipase C Increase in IP3 Release on Ca++ from intracellular stores

Answer 57

G alpha sub Q Receptors

Question 58

What is a primary factor in GPCR Desensitization?

Answer 58

B-Arrestin

Question 59

what causes B-arrestin to bind to the receptor?

Answer 59

A ligand bound to the GPCR for a prolonged period of time

Question 60

When B-arrestin binds it...

Answer 60

Tags the GPCR for internalization

Question 61

An internalized GPCR by B-Arrestin contributes to...

Answer 61

Drug tolerance

Question 62

The GPCR-B-Arrestin complex is brought inside the cell via an _________.

Answer 62

Endosome

Question 63

Three things that an endosome can do with the GPCR-B-Arrestin complex

Answer 63

1. Degrade the complex 2. cause an activation of signaling cascades from inside the cell that are INDEPENDENT of G Protein signaling 3. Return the complex to the cell surface

Question 64

Time it take for B-arrestin to bind to GPCR

Answer 64

Seconds to minutes

Question 65

Time it takes B-Arrestin to internalize a GPCR

Answer 65

Minutes

Question 66

What is GRK? What does it do?

Answer 66

GPCR Kinase. It adds a phosphate to the G-protein inside the cytoplasm. This phosphate is what attracts B-Arrestin

Question 67

What to drugs that target the GRK (G protein coupled receptor kinase) do?

Answer 67

They can optimize agonist binding

Question 68

What is the main reason for the downstream effects of the cholera toxin?

Answer 68

Cholera toxin does not allow GTP to become a GDP resulting in A GPCR that is permanently on

Question 69

What is the GPCR that is permanently on when the cholera toxin is present and what are the downstream effects?

Answer 69

G alpha S - causes cAMP to increase dramatically. This activates Cl- pumps which then release more Cl- into the intestinal lumen Na+, K+ and HCO3- ions follow H2O follows the ions to balance the osmolarity Increased H20 in lumen = really bad diarrhea!