Neurotransmitters and their Receptors Flashcards

1
Q

Chemical signaling consists of a _____, a _____, and a _____.

A

neurotransmitter
receptor
ion channel

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2
Q

Acetylcholine is an _____ neurotransmitter.

A

excitatory

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3
Q

Glutamate is an _____ neurotransmitter.

A

excitatory

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4
Q

GABA is an _____ neurotransmitter.

A

inhibitory

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5
Q

Glycine is a _____ neurotransmitter.

A

inhibitory

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6
Q

Catecholamines (_____, _____, _____) are _____ neurotransmitters.

A

epinephrine
norepinephrine
dopamine
excitatory

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7
Q

Serotonin is an _____ neurotransmitter.

A

excitatory

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8
Q

Histamine is a _____ neurotransmitter.

A

excitatory

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9
Q

Ionotropic receptors are _____ channels.

A

ligand-gated

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10
Q

Metabotropic receptors are _____ receptors.

A

G-protein-coupled

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11
Q

Ionotropic Receptors (types)

A
  1. Glutamate receptors (NMDA,AMPA/Kainate)
  2. Nicotinic acetylcholine receptor (nAChR)
  3. 5-HT(sub3) receptor
  4. GABA(subA) receptor
  5. Glycine receptor
  6. Purinergic receptors
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12
Q

G-protein coupled receptors are _____ proteins consisting of ______ transmembrane
domains.

A

monomeric

7

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13
Q

Domains ,,_,and _ of GPCRs make up the

neurotansmitter binding region.

A

II, III, VI, and VII

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14
Q

G-proteins bind to both the loop between domains _ and _ and the _____.

A

V
VI
C-terminus (string from helix-7)

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15
Q

Biogenic Amines

A
DA
EPI
NE
Histamine
Serotonin
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16
Q

nAChR consists of _ subunits.
Muscles: _____
Neurons: _____

A

5
αα:β:γ:δ
ααα:ββ

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17
Q

In nAChR, the _____ bind acetylcholine.

A

α-subunits

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18
Q

Each subunit of the nAChR consists of _

transmembrane spanning _____.

A

4

α-helices

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19
Q

The _____ surround the channel of the nAChR.

A

M2 subunits

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20
Q

Binding of acetylcholine to the two alpha subunits

results in a _° rotation of all _____ helices.

A

15

M2

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21
Q

The cytoplasm side of the nAChR receptor has
rings of high _____ charge that determine the
_____ of the receptor and remove the
_____ of the passing ions.

A

negative
cation specificity
hydration shell

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22
Q

Binding of _ ACh molecules results in a _____ of the M2 helices

A

2

twisting

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23
Q

The nAChR is a _____

cation channel.

A

non-selective

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24
Q

Higher driving force for _____ typically results in an _____ current and an _____.

A

Na+
inward
EPSP

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25
Q

Precursors of acetylcholine

A

Acetyl coenzyme A

choline

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26
Q

The enzyme _____ catalyzes Acetylcholine.

A

choline acetyltransferase (ChAT)

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27
Q

_____ load ~_ ACh molecules into each vesicle.

A

Vesicular ACh transporters

10

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28
Q

After release into the synapse, _____ breaks up ACh into

_____ and _____.

A

acetylcholinesterase
acetate
choline

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29
Q

A _____ transporter

takes choline back up into the presynaptic terminal.

A

Na+/choline

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30
Q

Myasthenia gravis is treated with

A

reversible acetylcholine-esterase inhibitors (e.g. neostigmine)

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31
Q

Myasthenia Gravis is the result of ____ caused by ____.

A

an autoimmune response

circulating antibodies that block AChRs at the post-synaptic neuromuscular junction

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32
Q

ACh has difficulty binding due to _____ of the binding site.

A

IgG blockade

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33
Q

Irreversible Acetylcholinesterase inhibitors

A

completely inhibit ACh breakdown

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34
Q

Treatment of acetylcholinesterase inhibition involves combined administration of a _____ and the AChE antagonist _____.

A

muscarinic receptor antagonist (atropine)

pralidoxime

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35
Q

neurotoxins such as snake poisins, curare (plant) and conotoxins (cone snails) are _____.

A

nAChR antagonists

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36
Q

Chewing betel nuts releases _____, a nicotinic agonist.

A

arecoline

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37
Q

Enzyme _____ catalyzes glutamate from glutamine

A

glutaminase

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38
Q

VGLUT

A

vesicular glutamate transporter

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39
Q

EAAT

A

excitatory amino acid transporter

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40
Q

precursor of glutamate

A

glutamine

released by glial cells

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41
Q

glutamate receptors are _____.

A

non-selective cation channels

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42
Q

NMDA-R serves as a _____.

A

coincidence detector

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43
Q

NMDA-Rs require _____ as co-agonist.

A

glycine

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44
Q

NMDA current involvement in an action potential is maximized with ____.

A

no Mg2+ block

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45
Q

Ca2+ influx through NMDA-Rs results in

_____ and eventually _____ and ____.

A

AMPA-R phosphorylation (early phase)
gene transcription
protein synthesis
(late phase)

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46
Q

mGluRs have _____ and can be _____ or _____

A

slow responses
excitatory
inhibitory

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47
Q

mGluR group 1

A

(mGluRs 1 and 5)

excitatory, G(q) coupled

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48
Q

mGluR group 2

A

(mGluRs 2 and 3)

inhibitory, G(i/o) coupled

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49
Q

mGluR group 3

A

(mGluRs 4, 6, 7, and 8)

inhibitory, G(i/o) coupled

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50
Q

Group I mGluRs increase _____ and are mostly _____.

A

NMDA

postsynaptic

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51
Q

Group II mGluRs reduce _____, decrease _____ release, and decrease _____.

A

cAMP
transmitter
NMDA

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52
Q

Group II mGluRs are mostly _____ and on _____.

A

presynaptic

glia cells

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53
Q

Group III mGluRs reduce _____, decrease _____ release, and decrease _____.

A

cAMP
transmitter
NMDA

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54
Q

Group III mGluRs are mostly _____.

A

presynaptic

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55
Q

GAD

A

glutamate decarboxylase;

catalyzes glutamate to GABA

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56
Q

VIAAT

A

vesicular inhibitory amino acid transporter

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57
Q

GAT

A

GABA transporter (removal from synaptic cleft)

58
Q

Ionotropic GABA receptors

A

GABA(A) and GABA(C)

59
Q

The effects of GABA agonists (e.g. benzodiazepines [Valium] and barbiturates)

A
  • anxiolytic (anxiety-reducing)
  • anesthetic
  • sedative-hypnotic
  • anti-convulsive
60
Q

Both _____ or _____ facilitate the ability of GABA to activate the receptor and opening of the chloride channel.

A

benzodiazepines

barbiturates (or alcohol)

61
Q

Barbiturates increase the _____.

A

length of channel openings

62
Q

Benzodiazepines increase the _____.

A

frequency of channel openings

63
Q

Depolarizing synaptic potentials can inhibit neurons as long as the _____ is more hyperpolarized (negative) than the _____.

A

E(Cl-)

action potential threshold

64
Q

In developing neurons the intracellular Cl- concentration is controlled by the _____, yielding high intracellular levels of _____.

A

Na+/K+/Cl- co-transporter

Cl-

65
Q

In adult cells a _____ pumps Cl- out of the cell, lowering the _____, making ECl- much more negative (leads to hyperpolarization).

A

K+/Cl- co-transporter

internal Cl-

66
Q

Shunting inhibition

A

If ECl- is equal to RMP, opening of Cl- channels does not hyperpolarize the cell, yet will act inhibitory on simultaneous EPSPs

67
Q

Metabotropic GABA receptors

A

GABA(B)

68
Q

mGABAR stimulate _____, leading to _____.

A

opening of K+ channels

hyperpolarization

69
Q

mGABAR inhibit _____, leading to _____.

A

Ca2+ channels

hyperpolarization

70
Q

mGABAR have _.

A

7 transmembrane domains

71
Q

Activation of presynaptic GABA(B) autoreceptors can inhibit release of _____ from the terminal.

A

GABA

72
Q

Presynaptic GABA(B) receptors inhibit release of ___, ___, and ___.

A

dopamine
norepinephrine
serotonin

73
Q

catecholamines are released by the _____ in response to psychological stress or low blood sugar levels.

A

adrenal glands

74
Q

Effects of catecholamines typically include

A

increases in heart rate
blood pressure
blood glucose levels
general reaction of the sympathetic nervous system

75
Q

In the CNS, catecholamines act as _____, influencing the effects of other classical neurotransmitters.

A

neuromodulators

76
Q

_____ catalyzes the reaction of L-Tyrosine to L-DOPA.

A

Tyrosine Hydroxylase

TH

77
Q

_____ catalyzes the reaction of L-DOPA to DA.

A

Aromatic L-amino acid decarboxylase

AADC

78
Q

_____ catalyzes the reaction of DA to NE.

A

Dopamine B-Hydroxylase

DBH

79
Q

_____ catalyzes the reaction of NE to EP.

A

Phenylethanolamine N-Methyltransferase

PNMT

80
Q

Catecholamines do not evoke EPSP or IPSP by themselves, rather make EPSP / IPSP _____.

A

larger or smaller

81
Q

Catecholamines alter ion channels to modulate _____, so that when synaptic inputs arrive the neuron is either _____ or _____.

A

cell’s excitability
more ready to fire action potentials
hyperpolarized / less excitable

82
Q

The catecholamine _____ is the reate-limiting enzyme in the synthesis of all catecholamines.

A

tyrosine hydroxylase

83
Q

Tyrosine hydroxylase is upregulated by _____, _____, _____, and _____.

A

stress
caffeine
nicotine
morphine

84
Q

Tyrosine hydroxylase is downregualted by _____.

A

antidepressants

85
Q

Symptoms of parkinson’s disease

A
tremors
muscle rigidity
akinesia
bradykinesia
postural instability
86
Q

Treatment of parkinson’s disease involves the replacement of lost DA with _____ or _____.

A

L-DOPA

DA

87
Q

GABAergic neurons in the _____ are the origin of projections that control (disinhibit) the thalamus, which in turn controls areas in the cortex that _____.

A

striatum

initiate movement

88
Q

Parkinson’s Disease

A

Loss of DA inhibition of GABAergic projection neurons.

89
Q

Addictive drugs target the _____, which includes the dopaminergic projections from the ventral tegmental area (VTA) to the _____ and other forebrain structures.

A

brain reward circuit

nucleus accumbens

90
Q

Dependence

A

an adaptive state that develops in response to repeated drug administration

91
Q

Cessation of drug use can lead to ____.

A

withdrawal symptoms

92
Q

Tolerance

A

refers to the diminished effect of a drug after repeated administration at the same dose, or the need to increase the dose to produce the same effect.

93
Q

sensitization

A

repeated drug administration leads to stronger effects at the same dose.

94
Q

Drugs of abuse typically release - times the amount of dopamine that natural rewards do.

A

2

10

95
Q

VMAT

A

vesicular monoamine transporter

96
Q

DAT

A

Dopamine transporter

97
Q

COMT

A

catechol O-methyltransferase

enzyme that degrades all catecholamines

98
Q

MAO

A

monoamine oxidase, enzyme that degrades all monoamines

99
Q

HVA

A

homovanillic acid

100
Q

Cocaine and amphetamines inhibit _____.

A

the re-uptake of dopamine

101
Q

Cocaine blocks _____ which increases the lifetime of dopamine in the synaptic cleft.

A

the dopamine transporter (DAT) (blocks dopamine re-uptake)

102
Q

Amphetamines increase _____ and block _____.

A

dopamine release

re-uptake

103
Q

Amphetamines enter the presynaptic terminal (via DAT, or through direct diffusion) and release _____ from the vesicles by making the dopamine transporters _____.

A

dopamine

work in reverse

104
Q

NE forms at the _____.

A

locus coeruleus

105
Q

EP forms at _____.

A

meduallary epinephrine neurons

106
Q

_____ catalyzes the reaction of DA to NE.

A

Dopamine B-Hydroxylase

107
Q

NET

A

NorEpinephrine Transporter

108
Q

NE and EP are degraded by ____.

A

MAO

109
Q

MAO

A

enzyme that degrades all monoamines

110
Q

NE and EP act _____ on 2 types of GPCRs: ____ and ____.

A

postsynaptically
A-
B-Adrenergic Receptors

111
Q

_____ inhibits VMAT and depletes NE stores.

A

Reserpine

112
Q

_____ inhibits COMT.

A

Tropolone

113
Q

_____ inhibits tyrosine hydroxylase and NE synthesis.

A

AMPT

114
Q

_____ is a norepinephrine and dopamine reuptake inhibitor.

A

Methylphenidate (Ritalin)

115
Q

Clonidine is an _____.

A

α2 adrenergic agonist

116
Q

α2-receptors are _____ (inhibits NE release).

A

autoreceptors (presynaptically)

117
Q

5 groups of Neuropeptides:

A
  • brain / gut peptides
  • Opioid peptides
  • Pituitary peptides
  • Hypothalamic releasing hormones
  • “other peptides”
118
Q

Pre-propeptides are present on the _____.

A

rough ER

119
Q

Propeptides are present on the _____.

A

trans-Golgi network

120
Q

Can different peptides can be released from the same vesicle?

A

yes

121
Q

Morphine, heroin, and synthetic opiates such as methadone and fentanyl are potent _____.

A

analgesics

122
Q

3 groups of endogenous opioid receptor ligands:

A
  • Endorphins (ENDOgenous moRPHINE)
  • Enkephalins
  • Dynorphins
123
Q

Enkephalins, endorphins and dynorphins are released in the _____.

A

periaqueductal gray

124
Q

Enkephalins are also released directly in the spinal cord to blunt the effects of _____.

A

nociceptor (C-FIBER) activation

125
Q

The _____ have a high affinity for enkephalins and beta-endorphin, but low affinity for dynorphins.

A

μ opioid receptors

126
Q

Morphine (heroin) and codeine bind to _____.

A

μ opioid receptors

127
Q

Main locus of action of heroin and codeine is in the _____.

A

VTA

128
Q

______ is the main active component of marijuana.

A

tetrahydrocannabinol (THC)

129
Q

Endocannabinoids:

A

2-AG

anandamide

130
Q

2 types of cannabinoid receptors (G-protein coupled receptors):

A
  • CB1 mainly expressed in the CNS and

* CB2 mainly expressed in immune cells

131
Q

low doses of cannabinoids tend to reduce _____, whereas high doses _____ theses behaviors.

A

anxiety-like behaviors

increase

132
Q

Anxiolytic effects:

A
  • Euphoric feelings of happiness, talkativeness, dream-like state.
  • Feelings of dizziness or fuzziness.
  • Contagious laughing or joking
  • Increases appetite “munchies”
133
Q

THC has _____ as seen in studies with drug discrimination, brain stimulation reward, and intravenous self-administration.

A

acute reinforcing effects

134
Q

THC increases the release of dopamine in the shell of the _____.

A

nucleus accumbens

135
Q

Physiological effects of (Endo-) cannabinoids

A

Various effects, including
• inhibition of adenylate cyclase,
• modulation of voltage-dependent calcium, and
• potassium channels

136
Q

Enhancement of endocannabinoid signaling produces _____.

A

anxiolytic and antidepressant-like effects

137
Q

endocannabinoid system is involved in the regulation of ____.

A

emotional states

138
Q

Endocannabinoids act as a retrograde messenger to regulate ____.

A

GABA release

139
Q

Nitric oxide (NO)

A

gaseous (retrograde) messenger

140
Q

Nitric oxide, is synthesized from _____ by various nitric oxide synthase (NOS) enzymes.

A

arginine and oxygen

141
Q

NO readily passes through ___.

A

membranes

142
Q

NO stimulates synthesis of _____.

second messenger that activates a protein kinase

A

cGMP (via guanyl cyclase)