Block E Lecture 3

Front 1

what is glutamate

Back 1

a neurotransmitter

Front 2

what are the characteristics of glutamate

Back 2

widely distributed throughout CNS

Excitatory neurotransmitter

main effect is to cause cell depolarisation

Front 3

what does quisqualate do

Back 3

quisqualate is shown to be an agonist at 2 majorly different receptor subtypes

-ionotrophic( ion channel coupled receptors)

-metabotrophic ( second messenger coupled receptors)

Front 4

what are metabotropic receptors

Back 4

7TM G- protein couples receptors

8 identified variants in 3 groups

Front 5

what are the receptor variants for metabotropic receptors I II And III

Back 5

group I- mGlu1, mGlu5

group II- mGlu 2, mGlu3

group III- mGlu4, mGlu6, mglu7, mGlu 8

Front 6

ionitropic receptors, name and explain

Back 6

NMDA, AMPA, kainate, delta

-integral receptor/cation channels

-each receptor composed of 4 subunits

multiple subunits for each major class of receptors

Front 7

name some kainate receptor agonists

Back 7

glutamate, kainate, ATPA

Front 8

name some kainate receptor agonists

Back 8

glutamate, kainate, ATPA

Front 9

name a kainate receptor antagonist

Back 9

2,4 - epi- neodysilherbaine

Front 10

what is kainate receptor effector mechanisms and function

Back 10

non selective cation channel

function- fast excitatory synaptic transmission

Front 11

name some AMPA receptor agonists

Back 11

glutamate, AMPA, quisqualate

Front 12

AMPA receptor antagonist

Back 12

NBQX

Front 13

AMPA receptor channel blocker

Back 13

polysmines, Mg2+ ions

Front 14

AMPA receptors effectior mechanism.

and function

Back 14

effector- non selective cation channel ( only some subtypes pass Ca2+ ions)

function- fast excitatory synaptic transmission

Front 15

NMDA receptors agonists

Back 15

NMDA, glutamate

Front 16

NMDA receptors antagonists

Back 16

D- AP5

Front 17

NMDA receptors ion channel blockers

Back 17

ketamine

Front 18

NMDA receptors effector mechanism and function

Back 18

effector mechanism- non selective cation channel

function- fast excitatory synaptic transmission

Front 19

what do magnesium ions do to NMDA receptors

Back 19

produce a voltage- dependent ion channel block of NMDA receptors, but not Kainate or AMPA receptors

Front 20

what do magnesium ions do to NMDA receptors

Back 20

produce a voltage- dependent ion channel block of NMDA receptors, but not Kainate or AMPA receptors

Front 21

NMDA and EPSP

NMDA and calcium ions

NMDA And gycine

Back 21

EPSP- NMDA Receptoes have a longer time course than AMPA and kainate

calcium- NMDA Receptors are the most highly permeable to calcium ions

glycine- is an allosteric modulator of NMDA receptor function

Front 22

explain NMDA RECEPTORS AND Magnesium

Back 22

Mg2+ binds within the open ion channel

voltage dependent block

occurs physiological Mg2+ concs

Front 23

what does glycine do at NMDA receptors

Back 23

glycine has a binding site on NMDA receptors

glycine facilitates the action of NMDA- allosteric modulation of NMDA function

- NMDA Produces a very small effect on its own without glycine

Front 24

what is the role of EEA receptors

Back 24

mostly concerned with NMDA receptors

5 different potential therapeutic targets

- epilepsy

ischaemic damage in CNS

memory loss

dissociative anaesthesia

psychiatric disorders

Front 25

what are NMDA antagonists

Back 25

anticonvulsant

- worknin animal models of epilepsy

Front 26

why are EAA receptors not clinically effective

Back 26

-too many unwanted effects ( loss of motor)

some newer anticonvulsants have mixed action including inhibition of AMPA receptors

Front 27

how do you get from ischaemia to programmed cell death

Back 27

ischaemia- cell death and damage- glutamate release- NMDA Receptor activation- sustained rise in intracellular Ca2+ - programmed cell death( apoptosis)

Front 28

what is long term potentiation

Back 28

long lasting enhancement of synaptic transmission after high frequency stimulation of afferent inputs

Front 29

what is long term potentiation(LTP) blocked by

Back 29

MK801

preventing NMDA receptor mediated Ca2+ flux

Front 30

what does ketamine do

Back 30

clinically used anaesthetic

blocks NMDA receptor ion channel ( at MK801 site)

produces vivid dreams in adults

Front 31

what does PDP DO

Back 31

phencyclidine, angel dust

produces hallucinations

blocks NMDA RECEPTOR ION CHANNEL

Front 32

what happens in hypofunctioning glutamate receptors

Back 32

contributing factor for developing schizophrenia

Front 33

what happens in hypofunctioning glutamate receptors

Back 33

contributing factor for developing schizophrenia

Front 34

pyschotic symptoms can be produced by what

Back 34

glutamatergic function at NMDA receptors

Front 35

what happens in hypofunctioning glutamate receptors

Back 35

contributing factor for developing schizophrenia

Front 36

pyschotic symptoms can be produced by what

Back 36

glutamatergic function at NMDA receptors

Front 37

what may be useful for some treatments of schizophrenia

Back 37

drugs acing at the glycine site on the NMDA Receptor