metabotropic receptors Flashcards
(13 cards)
pathways of GPCR include
indirect channel modulation
cAMP (a SU)- Gs/ Gi
PLC (a SU) - Gq - IP3
direct channel modulation
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
pre SN R
Post SN R
effect NT release at synapse
effect neuronal excitability and AP firing - mAChR (GIRK)
post-ganglionic SNS neurone (pre- SN)
- 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
regulation of pre- synaptic transmission can be via
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
receptors can be activated by
same
or different neurones in that chain
- CNS
- Nad release from neighbouring synapses can reduce the release of glutamate from glutaminergic neurones - a2 R
post SN modulation on..
autonomic ganglia
- ACh always
- post G neuron
- modulates AP firing in that cell
Fast EPSP
- ACh binds to nAChR
- single AP
- na influx
- large depol
(synapse not stimulated)- current stimulus only
slow EPSP
- 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
ACh release leads to
fast and slow EPSPs
No slow EPSP
- M-type open
- k efflux
- reduced excitability
. single AP only - difficult to reach vT
slow EPSP
- M-T channels close (mACHr)
- increased excitability of cell
- now if stimulated by current
- multiple Eps fire
- repeated stimulation of same synapse enhances response
mACHr activation in ANS…
increases neuronal excitability