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Neuropharm > GABA B - NF > Flashcards

GABA B - NF Flashcards

1
Q

GABA B structure

A

Two subunits

GABA B R1 (B1a, B1b)
GABA B R2

Obligate heterodimer, R2 with R1

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2
Q

How was it shown that R2 has to couple with R1

A

Immunohistochemical binding

KO studies

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3
Q

GABA B agonists

A

Baclofen

GHB (drowsiness)

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4
Q

Baclofen use

A

Severe spasticity from MS or spinal chord injury

Neuropathic pain

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5
Q

Competitive antagonsts

A

Phaclofen

Saclofen

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6
Q

Allosteric modulators + use

A

CGP compounds

Used in anxiety and arthritic pain

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7
Q

Are there subtype selective ligands

A

No

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8
Q

Mechanism of GABA B presynaptic reduction in NT release - Calcium dependant

A

By subunit inhibits P/Q and N tpye Ca channels

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9
Q

Mechanism of GABA B presynaptic reduction in NT release - Calcium independant

A

alpha i/o subunit inhibits adenyly cyclase activity
lower cAMP, less PKA
Stops vesicle priming as less phosphorlyation of SNARE complex BY PKA

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10
Q

Mechanism of postsynaptic hyperpolarisation

A

By activates GIRK1+2
Allows K out, which hyperpolasies the axon
Makes it less likely for EPSP and keeps Mg block

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11
Q

What receptor provides tonic hyperpolarlisation

A

GABA B

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12
Q

Which heterodimer is found presynaptically on glutamatergic

A

R1a with R2

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13
Q

Which is found postsynaptically on glutamatergic

A

R1b with R2

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14
Q

Structre of GABA extra domains

A

Venus fly trap domain for ligand binding

Coiled coil domain intracellularly

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15
Q

Which subtype has sushi domains

A

R1a

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16
Q

Between which subunits can dimer-dimer GABA B R form

A

BEtween R1 units only

17
Q

What do receptor associated membrane proteins allow

A

Diversity of function

18
Q

What are the 4 pathologies associated with GABA B

A

Memory
Pain
Consciousness
Reward/Addiction

19
Q

What subtype and extra protein are assocaited with better memory

A

Sushi domains on R1a

20
Q

How do GABA B help memory

A

Inhibition stops excess glutamate release
Stops NMDA being saturated and constantly firing
Cannot therefore recruit NMDA so no long term plasticity in dynamic range

21
Q

What does R1a KO cause in mouse tests

A

No novel object recognition

Neuropharm (15 decks)

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