autonomic nervous system 4 Flashcards
basic principles of Neurotransmission for cholinergic synapse
Ach synthesis from choline and acetyl coa using CAT
choline taken up by the terminal (limiting factor)
synthesis of ach determined by choline uptake
actively packaged
requires a proton gradient
synthesis of adrenergic nt noradrenaline and
rate limiting step =
ATP
conversion of tyrosine
drugs that affect Ach synthesis/packaging
Hemicholinium - inhibits choline uptake
vesamicol - inhibits Ach packaging
no clinical use
what can we uses drugs that affect Ach synthesis and packaging for
use them to dissect the transmission seeing the impact of the transmission in certain cells
ach release how much and how much is used
3 million released from 1 neurone of 300 vesicles
2 million released and act on 1 of the 30 million receptors
only 2ms then hydrolysed by AchE on the NMJ
drugs affecting Ach release
streptomycin/neomycin - inhibits Ca influx, reduces NT release
botulinum toxin and Beta bungrutoxin - cleaves protein involved in vesicle exocytosis
regulation of Ach release
what happens with the post ganglionic synapse
M2R found presynaptically
ach acts on it and inhibits Ach release
regulation of Ach release
at the NMJ terminals what happens
Ach acts presynaptically on nAchR to enhance further Ach release
regulation of Ach release
in the CNS terminal what happens
nAchRfound presynaptically to increase or decrease release of NT such as glutamate and Dopamine
Ach inactivation
what is it broken down by
AchE
or BuchE
ach inactivation
what does AchE do
it hydrolysis Ach within 2ms of interaction with receptor
tethered to cleft
inhibition of Ach what happens
allows more then one receptor to be bound and activated
helps in altzimers
drugs that affect breakdown (enhhance cholinergic transmission)
Neosigmine - inhibits AchE breakdown at NMJ
physostigmine - inhibits ACHE acting at post ganglionic cholinergic synapses
donezapil - inhibits ACHE at CNS cholinergic synapse
Nicotinic receptors where are they used
ganglionic - post
CNS - pre
NMJ - post
drugs that act at nicotinic
nicotine- ganglionic and CNS stimulant hexamethonium (antagonist) -autonomic ganglion blocker blood pressure lowering agent tubocurarine - NMJ blocker muscle relaxant