metabotropic receptors Flashcards

(13 cards)

1
Q

pathways of GPCR include

indirect channel modulation

A

cAMP (a SU)- Gs/ Gi

PLC (a SU) - Gq - IP3

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2
Q

direct channel modulation

A

via G protein itself
not via enzymes/ 2nd

  • beta/gamma SU binds directly to GIRK K channel; on cardiac myocytes
  • triggers hyper polarisation of cells
  • decreased excitability
  • mAChRs
  • reduced HR - PNS
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3
Q

pre SN R

Post SN R

A

effect NT release at synapse

effect neuronal excitability and AP firing - mAChR (GIRK)

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4
Q

post-ganglionic SNS neurone (pre- SN)

A
  • synapses with smooth muscle target in periphery
  • NAd release
  • pre SN a2 R + VGCa
  • modulation of Ca current via beta/gamma SU
  • activation of a2 inhibits VGC via beta/gamma signalling directly
  • reduced ca conductance/influx
  • reduced Nad release from terminals
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5
Q

regulation of pre- synaptic transmission can be via

A

inhibition of NT release (reduced ca influx)

facilitation of NT release (VGKC) - inhibit delayed rectifier channel

  • prolonged AP
  • enhanced ca influx due to more pos Vm because of reduced K conductance
  • longer EPSP
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6
Q

receptors can be activated by

A

same
or different neurones in that chain

  • CNS
  • Nad release from neighbouring synapses can reduce the release of glutamate from glutaminergic neurones - a2 R
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7
Q

post SN modulation on..

A

autonomic ganglia

  • ACh always
  • post G neuron
  • modulates AP firing in that cell
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8
Q

Fast EPSP

A
  • ACh binds to nAChR
  • single AP
  • na influx
  • large depol
    (synapse not stimulated)- current stimulus only
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9
Q

slow EPSP

A
  • ACh binds to mACHr
  • IP3 pathway (a SU) - Gq protein
  • DAG produced (2nd messenger)
  • inhibits M-type K channels
  • less k efflux, reduced resting conductance to k (open without stimulation)
  • small depol due to leak Na channels
  • no AP fired initially
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10
Q

ACh release leads to

A

fast and slow EPSPs

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11
Q

No slow EPSP

A
  • M-type open
  • k efflux
  • reduced excitability
    . single AP only
  • difficult to reach vT
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12
Q

slow EPSP

A
  • M-T channels close (mACHr)
  • increased excitability of cell
  • now if stimulated by current
  • multiple Eps fire
  • repeated stimulation of same synapse enhances response
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13
Q

mACHr activation in ANS…

A

increases neuronal excitability

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