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DRUGS > Drugs 2 - Amino acids > Flashcards

Drugs 2 - Amino acids Flashcards

1
Q

what are the excitatory transmitters?

A

Glutamate, aspartate and NAAG (n-actelyaspartate glutamate)

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2
Q

Types of glutamate receptors

A

inotropic (AMPA, kainate and NMDA) and metabotropic (GLu1-8) GluR1,2,3

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3
Q

glutamates journey in neurons

A

released by ca2+ in vesicles, reuptaken by EEAT, Repackaged by VGluT (vesicular glutamate transporter)

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4
Q

glutamates journey in glia

A

when it escaoes from the synapse it is reuptaken by EEAT, converted into Gln before being released back to the neuron (to avoid excitation). reuptaken by GlnT, converted to GLu and repackaged.

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5
Q

Why is targeting Glu metabolism not possible?

A

because it is the centre of all amino acid metabolism so would have huge downstream effects.

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6
Q

Ampa receptor structure and location

A 
4 subunits (all Glu binding sites). 2 must be filled for activation. can be heteromeric or homomeric. 
widespread in the CNS
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7
Q

AMPA permeable to

A

K NA CA

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8
Q

AMPA agonist

A

quisine

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9
Q

Kainate receptor structure

A

similar to AMPA but not as widespread or permeable to Ca. mainly found presynaptically.

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10
Q

NMDA receptors

A

require both glutamate and glycine to bind and depolarisation to activate

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11
Q

NMDA permeability

A

more permeable to ca but mediated by Mg block

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12
Q

why are NMDA receptors a good drug target?

A

They have multiple points to block - Glu, Gly, channel, allosteric

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13
Q

NMDA channel blocker

A

AP5/APV/CPP

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14
Q

mGluR1:

A

1 5

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15
Q

mGluR2:

A

2 3

AGONISTS decrease glutamate release

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16
Q

mGluR3:

A 
4 6 (retina only) 7 8
agonists decrease glutamate release
17
Q

uses for mGluR1:

A

ANATAGONISTS used in treatment of pain parkinsons and epilepsy.
They can lift the Mg2+ block by causing longer slower depolarisations

18
Q

the mGlu family

A

don’t share their structure with any other metabotropic receptor family

19
Q

mGluR3: location

A

nerve terminals

20
Q

mGluR2: location

A

somatodendritic and nerve terminals

21
Q

mGluR1: location

A

somatodendritic

22
Q

GABA in the CNS

A

20% of neurons are gabs ergic and it acts at 30% of synapses. its found in brain tissue as well as synapses.
usually neurons are short and local but in the striatum to globus pallidus/SN they are longer

23
Q

GABAa structure

A

inotropic ligand gated ion channel (cl-). Pentameric structure made of 2a2b1gamma units. binding sites for gaba are at the a/b interfaces. BZD site is at the y/a interface.
They can be found extrasynaptically.
They are usually post synaptic.

24
Q

extrasynaptic GABAa receptors

A

they have a different subunit structure and produce longer tonic inhibition. they are acted on by anaesthetics and BZDs.

25
Q

GABAb receptors

A

can be found both pre and post synaptically. K channel activators or Ca channel inhibitors. also inhibit adenyl cyclase.

26
Q

GABAa agonists:

A

Gaba site - muscimole
antag - bicuculline
BZD site - BZDs and anxiolytic
BZD site antagonist - flumazenil

27
Q

Glycine:

A

found mainly in the spine (GlyT2) but also in the brain (GlyT1- reuptake). It is inhibitory and has particular effect on Renshaw cells to stop over activation or relaxation of muscles in the spinal cord.

28
Q

Glycine synthesises

A

from serine or obtained from diet

29
Q

Glycine R structure

A

pentameric like GABAa

30
Q

kinetics of glutmate receptors

A

NMDA - slow (+slowEPSPs?)

AMPA and Kainate - fast

31
Q

locations of glutmate receptors

A

NMDA - pre/post synaptic and glial cells
AMPA - post synaptic and glial cells
Kainate - pre synaptic mainly but some post

32
Q

functions of kainate receptors

A

pre synaptic inhibition

33
Q

fucntions of NMDA receptos

A

excititoxicity, plasticity, LTP/LDP

DRUGS (7 decks)

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