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3922 > 5 - Transporters and targets of drug action > Flashcards

5 - Transporters and targets of drug action Flashcards

1
Q

What is a primary active transporter

A

Na/K ATPase

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2
Q

What is a secondary active transporter

A

Plasma membrane glutamate transporter (all NT transporters)

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3
Q

Where are neurotransmitter transporters found

A

Post- and pre-synaptic neurones and glial cells

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4
Q

What are the two main neurotransmitter families

A

Glutamate and Neurotransmitter sodium symporter (NSS)

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5
Q

What do the NSS family transport (5)

A 
GABA
Glycine
Dopamine
Noradrenaline
Serotonin
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6
Q

How many subtypes of EAATs are there

A

5

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7
Q

Where is EAAT4 mainly expressed

A

Cerebellum

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8
Q

Where is EAAT5 mainly expressed

A

Retina

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9
Q

Which EAAT transports L-Cysteine as well

A

EAAT3

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10
Q

In the transporter homologue (EAAT) from Pyrococcus horikoshii, how many subunits were there

A

3

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11
Q

What is GLTph

A

A Na+ dependent aspartate transporter

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12
Q

What are all human NSS coupled to

A

Na and Cl

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13
Q

How do GlyT1 inhibitors work to treat schizophrenia

A

In schizophrenia there is reduced NMDAR activity

Inhibition of GlyT1 will elevate excitatory synapses and stimulate NMDAR

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14
Q

What are GlyT2 inhibitors used to treat

A

Reduce transmission of pain signals from spinal cord up to the brain

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15
Q

What shape are dDat transporters

A

Shot glass shape

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16
Q

What does dDAT rely on the co-transport of

A

2 Na and 1 Cl ion

17
Q

What are two inhibitors of GABA tranporters

A

Nipecotic Acid

Tiagabine

18
Q

What are the difference in effects between amphetamine and methamphetamine

A

Methamphetamine produces more exaggerated effects related to higher effective doses and greater propensity for addition

19
Q

What are some effects of chronic methamphetamine use (6)

A

1) Drug-craving
2) Withdrawal-related depression
3) Rapid tooth decay
4) Degeneration of dopaminergic neurons
5) Weight loss
6) Psychosis

20
Q

What is the MOA of amphetamine at DAT

A

Amp is a false substrate

Reduces DA uptake and causes reverse transport of DA

21
Q

What are some additional actions of amphetamines (2)

A

Inhibits MAO

Competes with VMAT (depletes storage of DA in vesicles)

22
Q

What is cocaine (2)

A

Na channel blocker

DAT, NET, SERT inhibitor

23
Q

What are the effects of cocaine (3)

A

Simulate
Appetite suppressant
Topical anaesthetic

24
Q

What is the MOA of cocaine

A

Competitive blocker of dopamine, noradrenaline and serotonin transport

3922 (19 decks)

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