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Biomembranes > GABA receptors > Flashcards

GABA receptors Flashcards

1
Q

What receptor is this?

G0 beta/gamma complex component inhibits calcium entry at presynaptic terminal and therefore causes autoinhibition by lowering neurotransmitter release upon second stimulation.

A

GABA-b receptor

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2
Q

what receptor is this?
Gi beta/gamma complex facilitates opening of K channels
- hyperpolarization of postsynaptic membrane and therefore direct synaptic inhibition

A

Postsynaptic, metabotropic GABAb receptor

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3
Q

what occurs if EPSP precedes IPSP?

A

no effect on on EPSP– normal excitation

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4
Q

what occurs if IPSP precedes EPSP

A

inhibitory effect— EPSP is abolished

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5
Q

Barbiturate, benzodiazepines are:
- enhancers or inhibitors?
- bind the different/same sites on GABAaR?

A
  • enhance receptor function
  • bind different sites
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6
Q

Drugs that enhance GABAa receptor function are known as what?

examples
anxiolytic, anticonvulsant, analgesic, sedative, amnestic

A

positive allosteric modulators (PAMS)

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7
Q

pro-convulsant, anxiogenic drugs are characteristic to what kind of GABAa receptor drugs

A

GABAa inhibitors

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8
Q

how do benzodiazepines enhance GABAa receptors?

A

increase channel opening probability

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9
Q

mechanism of barbiturates on GABAa receptor enhancement?

A
  • longer duration channel opening
  • direct receptor activation at high barbiturate concentration
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10
Q

which GABAar enhancers can induce anesthetic “unconscious state?

A
  • propofol, etomidate, barbiturates

NOTE: benzodiazepines do NOT

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11
Q

effect of Picrotoxin, bicuculline on GABAa receptor?

A

GABAar blockers

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12
Q

a1b1 GABAar and their response to (activation/no effect):
- GABA
- benzodiazepine
- Bicuculline
- picrotoxin

A
  • enhanced
  • enhanced (A1 has H101)
  • inhibited
  • inhibited
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13
Q

what is the determining characteristic of DIAZEPAM sensitive GABAaRs (i.e. GABAa1-5 are sensitive) ?

A
  • H residue at position 101

ex. A1-5 are sensitive (have H101)

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14
Q

what do GABAa recpetor subtypes A4,A6 have in common? (think in terms of DIAZEPAM sensitivity?)

A
  • not sensitive to DIAZEPAM
  • have R instead of H at position 101
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15
Q

result of R101 mutation to H (in terms of diazepam sensitivity)?

A

receptor becomes sensitive

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16
Q

result of A1H101R knock-in in mice? (in terms of diazepam sedative/anxiolytic effects)
- what does this say about the function of A1 beta/gamma receptor

A
  • diazepam no longer sedative
    still anxiolytic

suggests sedative effects is mediated by A1 beta/gamma2 receptors

17
Q

effect of diazepam on A2H101R mouse knock in (in terms of diazepam sedative/anxiolytic effect)

what does this tell us about A2?

A
  • No longer anxiolytic
  • remains sedative
  • potential drug target for anti-anxiety medication
18
Q

Resulting etomidate effect on Beta2 N265S mutation (in terms of GABAaR enhancement/sedative/hypnotic)?

A
  • reduced GABAa receptor enhancement
  • lowered sedative effects
  • impaired hypnotic action
19
Q

effect of etomidate/propofol on Beta3 N265M mutation ( in terms of GABAa enhancement/hypnotic action)?

A
  • reduced GABAaR enhancing effects
  • greatly impaired hypnotic action
20
Q

alpha1 GABAa receptor isoform mediates what Benzodiazepine behavior?

A

sedation

21
Q

What GABAa receptor isoform(s) mediate anxiolytic/analgesic behavior?

A
  • Alpha2
  • Alpha3
22
Q

beta3 subunit mediates what benzodiazepine effect?

A
  • anaesthesia/immobility
23
Q

beta2 subunit of GABAa receptor mediates what benzodiazepine behavior

A
  • sedation/anaesthesia
24
Q

Alpha5 GABAa receptor isoform mediates what benzodiazepine effect?

A
  • effect on cognition
25
Q

What residue (located in Transmembrane region 2 ) dictates beta subunit specificity in:
- Beta2,3
- Beta 1

A
  • B2,3: Asparagine
    B1: Serine

Biomembranes (8 decks)

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