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Psychopharmacology > Chapter 2: Transporters, receptors, and enzymes > Flashcards

Chapter 2: Transporters, receptors, and enzymes Flashcards

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1
Q

P450 inhibitors: STICKFACES.COM Group

A

S - Sodium valproate
T - Ticlodipine
I - Isoniazid
C - Cimetidine
K - Ketoconazole
F - Fluconazole
A - Acute alcohol/amiodarone
C - Ciprofloxacin
E - Erythromycin
S - Sulfonamides
C - Cranberry juice
O - Omeprazole
M - Metronidazole
Group = grapefruit juice

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2
Q

P450 Inducers: BS CRAP GPS

A

B - Barbiturates
S - St. John’s Wort
C - Carbamazepine
R - Rifampin
A - Alcohol (chronic)
P - Pheytoin
G - Griseofulvin
P - Phenobarbital
S - Sulfonylureas

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3
Q

6 most important P450 enzymes

A

1A2
2B6
2D6
2C9
2C19
3A4

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4
Q

Serotonin transporter and gene family

A

presynaptic monoamine SERT/SLC6

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5
Q

Norepinephrine transporter/gene family

A

presynaptic monoamine NET/SLC6

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6
Q

Dopamine transporter/gene family

A

presynaptic monoamine DAT/SLC6

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7
Q

glial and GABA transporters

A

GAT1-4
GlyT1-2
EAAT1-5

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8
Q

GAT1-4 gene family/substrate

A

SLC6/GABA

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9
Q

GlyT1-2 gene family/substrate

A

SLC6/Glycine

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10
Q

EAAT1-5 gene family/substrate

A

SLC1/glutamate and aspartate

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11
Q

vesicular neurotransmitter transporters VMAT1-2 gene family/substrate

A

SLC18/serotonin
dopamine
histamine
norepinephrine

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12
Q

VaChT vesicular transporter gene family/substrate

A

SLC18/acetylcholine

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13
Q

VIAAT vesicular transporter gene family/substrate

A

SLC32/GABA

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14
Q

vGluT1-3 vesicular transporter gene family/substrate

A

SLC17/glutamate

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15
Q

false substrate for SERT

A

MDMA

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16
Q

false substrate for NET

A

dopamine, epinephrine, amphetamine

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17
Q

false substrate for DAT

A

norepinephrine, epinephrine, amphetamine

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18
Q

how do transporters concentrate monoamines into presynaptic neurons (reuptake)

A

sodium-potassium ATPase continually pumps sodium out of the cell to create a downhill gradient that allows for the uphill transport of the neurotransmitter

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19
Q

how do vesicular transporters package neurotransmitters into synaptic vesicles

A

proton ATPase continually pumps positively charged protons out of the vesicles so that the neurotransmitter can be transported into the vesicle to keep the charge the same

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20
Q

what is a neurotransmitter transporter

A

a type of receptor that binds to neurotransmitter prior to transporting it across the membrane

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21
Q

2 major classes of plasma membrane transporters

A

sodium/chloride-coupled transporters (SLC6 gene family)
Glutamate transporters (SLC1)

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22
Q

plasma membrane transporters on presynaptic membranes

A

SERT
NET
DAT

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23
Q

plasma membrane transporters located on glia and neuronal cells

A

GAT1-4
BGT1
Gly T1-2
EEAT1-5

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24
Q

SLC6 sodium/chloride-coupled includes which plasma membrane transporters

A

includes transporters for serotonin, norepinephrine, and dopamine as well as the neurotransmitter GABA and amino acid glycine

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25
presynaptic SLC6 transporters
SERT NET DAT
26
glial SLC6 transporters
GAT1-4 BGT1 GlyT1-2
27
SLC1 glial transporter
EAAT1-5 (glutamate)
28
3 subclasses of intracellular synaptic vesicle transporters
SLC18 SLC32 SLC17
29
what are the two types of molecular transporters
plasma membrane transporters intracellular synaptic vesicle transporters
30
SLC18 intracellular synaptic vesicle transporters
VMAT1-2 (vesicular monoamine transporters) VAChT (vesicular acetylcholine transporter)
31
which monoamines are transported VMAT1-2 intracellular synaptic vesicle transporters
serotonin norepinephrine dopamine histamine
32
SLC32 gene family intracellular synaptic vesicle transporters
VIAATs (vesicular inhibitory amino acid transporters)
33
SLC17 gene family intracellular synaptic vesicle transporters
VGluT1-3 (vesicular glutamate transporters)
34
false substrate for SERT presynaptic transporter
MDMA (Ecstasy)
35
false substrates for presynaptic transporter NET
dopamine epinephrine amphetamine
36
false substrates for presynaptic transporter DAT
norepinephrine, epinephrine, amphetamine
37
synaptic vesicle transporter for all 3 monoamines
VMAT2 (vesicular monoamine transporter 2)
38
what are the 3 monoamines
sertraline dopamine norepinephrine
39
does it take energy to concentrate monoamines into presynaptic neuron?
yes
40
how is energy generated to concentrate monoamines into the presynaptic neuron
downhill transport of sodium coupled with uphill transport of the monoamine
41
what does "the sodium pump" (adenosine triphosphatase) do to generate the energy to concentrate monoamines in the presynaptic neuron
continuously pumps sodium out of neuron creating a downhill gradient which creates an uphill gradient for the monoamine
42
binding sites on SLC6 transporters
2 sodium ion binding sites other binding sites for drugs (SSRIs)
43
what happens when a drug binds to a receptor on an SLC6 transporter
prevents monoamine reuptake
44
what binds to the SLC6 transporter in the absence of sodium
nothing; not sodium or monoamine
45
how do you increase monoamine action
prevent it from binding to its transporter so it accumulates in the synapse
46
which transporters are blocked by ADHD stimulants and cocaine
DAT NET
47
which tra nsporters are blocked by most drugs for unipolar depression
SERT NET DAT
48
what conditions are treated by blocking neurotransmitter transporters
anxiety, fibro neuropathic pain, postherpetic neuralgia, peripheral neuropathy and other pain conditions, eating disorders, impulsive-compulsive disorders, OCD, trauma/stress related disorders (PTSD)
49
what condition are NOT treated by blocking monoamine binding to transporters
bipolar depression with mixed features
50
what is the only medication that blocks GABA transporter GAT1 to increase synaptic GABA concentration
anticonvulsant tiababine
51
what happens when glutamate is transported into glia
it is converted into glutamine to enter the presynaptic neuron for conversion back to glutamate
52
differences of SLC1 to SLC6 transporters
glutamate is excitatory exact location on pre/post synaptic neurons/glia is under investigation. no drugs are known to block them glutamate transport almost always has countertransport of potassium. may work as timers rather than dimers
53
transporters for neurotransmitter histamine
no presynaptic transporter vesicular transporter is VMAT2 (same as monoamines)
54
histamines inactivation
entirely enzymatic
55
VMATs vesicular transporters are members of what gene family
SLC8
56
VaChT
vesicular transporter for acetylcholine
57
VIAAT is a vesicular transporter that is a member of what gene family
SLC32
58
what gene family does vesicular transporter vGluT1-3 belong to
SLC17 vesicular transporter for glutamate
59
SV2a transporter
novel vesicular transporter with 12 transmembrane regions that binds to anticonvulsant levetiracetam whic may reduce seizures by blocking neurotransmitter release
60
how is energy generated to move neurotransmitters into synaptic vesicles
proton ATPase (proton pump) pumps positively charged protons out of synaptic vesicles continuously. neurotransmitters are able to then concentrate against the gradient by substituting their own + charge in the vesicle for the + charge being pumped out SO neurotransmitters go in while protons go out, keeping the charge in the vesicle the same
61
which vesicular transporters are NOT known to be targeted by drugs
ones for GABA (SLC32), acetylcholine (SLC18), and glutamate (SLC17)
62
which vesicular transporters are targeted by many drugs
VMATs (SLC18 family)
63
drugs that target VMAT vesicular transporters
amphetamine (both monoamine and vesicular transporters) methylphenidate and cocaine (only monoamine transporters) tetrabenzine and its derivatives as inhibitors
64
structure of G-protein-linked receptors
7 transmembrane regions (spans membranes 7 tiems) that cluster around a central core that contains a neurotransmitter binding site
65
how do drugs lead to modification of g-protein-linked-receptors
they mimick or block neurotransmitter function that normally happens at binding or allosteric sites on the receptor
66
difference between neurotransmitters and drugs on g-protein-linked receptors
neurotransmitters interact with all receptor subtypes. Drugs interact only with a specific receptor subtype
67
action of agonists on g-protein-linked receptors
turns on the synthesis of the second messenger to the greatest extent possible so downstream proteins are fully phosphorylated and genes are maximally expressed
68
what are the 2 ways to stimulate G-protein-linked receptors with full agonist action
drugs bind directly to neurotransmitter sites or indirectly boost levels of the neurotransmitters themselves
69
2 ways drugs boost levels of neurotransmitters themselves
inhibition of monoamine transporters blocking enzymatic destruction of neurotransmitters
70
2 ways to block enzymatic destruction of neurotransmitters
inhibition of SERT, NET, DAT and GABA transporter GAT1 inhibition of enzyme acetylcholinesterase
71
action of antagonist on g-protein-linked receptors
produces conformational change in receptor that causes signal transduction to remain at constitutive levels
72
clinical purpose of antagonists on g-protein-linked receptors
block excessive neurotransmission reverses agonists, partial agonists, and inverse agonists
73
action of partial agonists on g-protein-linked receptors
produce signal transduction that is more than constitutive but less than agonist depending on how close the partial agonist is to the full agonist
74
action of inverse agonist on g-protein linked receptors
causes conformational change to stabilize receptor in inactive form essentially, turning action down below consitutive
75
what happens when an enzyme is bound
it cannot bind with its substrate so it is inactivated can be reversible or irreversible
76
irreversible binding of an enzyme
cannot be displaced by the substrate (essentially killing it)
77
reversible binding of an enzyme
when a substrate can compete for the receptor site and shove it off of the enzyme
78
few drugs that bind enzymes used in clinical practice
MAOIs acetylcholinesterase glycogen synthase kinase (GSK)
79
agents that target GSK enzymes that are used in clinical practice
lithium may target in this enzyme in the signal transduction pathway of neurotrophic factors
80
what acts through phosphoprotein GSK-3 to promote cell death
neurotrophins, growth factors, and other signaling pathways it is also possible that valproate and ECT act of GSK3
81
consequences of inhibiting GSK3
may have neuroprotective actions, long term plasticity, and may contribute to mood stabilizing effects of lithium
82
what are CYP enzymes
drug metabolizing enzymes that are mediated through the liver and gut that are responsible for a large amount of psychotropic drugs
83
are pharmacokinetics or pharmacodynamics responsible for mechanism of action of psychotropic drugs
pharmacodynamics
84
6 most important CYP450 enzymes
1A2 2B6 2D6 2C9 2C19 3A4
85
extensive metabolizers
people who have "normal" rates of drug metabolism by CYP4550 enzymes
86
what happens if there is reduced activity of CYP450 enzymes
risk for elevated drug levels as they are not metabolized fast enough patients need less than standard doses
87
ultra-rapid metabolizers
people who have elevated CYP450 enzyme activity
88
consequences of being an ultra-rapid metabolizer
may require higher than standard doses due to resultant subtherapeutic drug levels

Psychopharmacology (13 decks)

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