Flashcards in Neurotransmitter Systems Deck (45):
0
Ach - central locations
pons
midbrain
the striatum
1
Ach - General function
Crucial in producing consciousness, but not awareness
control of voluntary motion
initiation of REM sleep
2
Ach - vesicular storage
Ach stored in clear vesicles
Moved into vesicles by VAchT
3
Ach - Catabolism
Acetylcholinesterase bound to the POST synaptic cell membrane
4
Ach Receptors (2)
nicotinic (NAchR)
muscarinic (MAchR)
5
Muscarinic receptor properties
4 or 5 different types, all activated by muscarine
serpentine receptor
GPCR
6
M1 (neuronal) MAchR
Gq
increase IP3/DAG, Increase Ca++
7
M2 (cardiac) MAchR
Gi
decrease cAMP, increase K+ efflux
8
M3 (sm m. of bronchi, vasculature, endothelial cells of vasculature) MAchR
NO
Gq
IP3/DAG, increase Ca++
in the vasculature NO is the major effector (which wins)
9
Nicotinic receptors
located at NMJ (Na), autonomic ganglia, other parts of the CNS (Ca, Na)
5 subunits
IONOTROPIC
allow for Na entrance, allthough some neuronal forms allow for significant Ca influx
10
Amino acid NTs (list)
glutamate, aspartate, taurine (EAAS)
GABA, glycine (inhibitory amino acids)
11
GABA - location
cerebellum
cortex
retina
12
GABA - functional roles
major inhibitory NT in the higher CNS
critical for producing consciousness/awareness
control of voluntary motion
13
GABA - synthesis
glutamate decarboxylase (GAD)
derived from glutamate
14
GABA - how is action limited
reuptake
catabolism by GABA transaminase
15
GABA - what does it bind to
GABA-A and GABA-B receptors
16
GABA-A receptors
ionotropic/metabotropic
subunits
ion conductance (if ionotropic)/Gprotein if metabotropic
other important chemicals
IONOTROPIC
5 subunits
Cl- conductance
benzodiazapine site potentiates
17
GABA-B receptors
ionotropic/metabotropic
subunits
ion conductance (if ionotropic)/Gprotein if metabotropic
other important chemicals
Metabotropic
-
heterodimer G protein (Gq and Gi) decreases adenylyl cyclase, increases K+ efflux. AND decreases IP3/DAG, decreases Ca influx
-
18
Many general anesthetics are now postulated to produce anesthesia by activating what receptors?
GABA receptors, mostly GABA-A, at extra-synaptic locations throughout the cortex
19
Glycine - location
spinal cord
brainstem
forebrain (less than gaba)
20
glycine - function
mediates many spinal inhibitions
21
glycine - binds to
glycine receptors
22
glycine receptor
ionotropic/metabotropic
subunits
ion conductance (if ionotropic)/Gprotein if metabotropic
other important chemicals
ionotropic
a=glycine binding, b = structural
Cl-
blocked by strychnine
23
Peptide NT (2)
opiods
endocannabanoids
coded for by genes, originally thought to be neuromodulators
24
Opiods - location
basal ganglia
hypothalamus
parabrachial nuclei and raphe nuclei
25
opiods - general functions
modification of nociceptive inputs
modification of mood/affect
26
Opioid - 4 precursor molecules
proenkephalin
pro-opiomelanocortin
prodynorphin
orphanin FQ
27
proenkephalin - sequence and 2 major variants
tyr-gly-gly-phe-x
met-enkephalin
leu-enkephalin
28
pro-opiomelanocortin (POMC)
B endorphins
29
prodynorphin
When you cut up prodynophin, it gives rise to 4 opioid molecules
3 molecules of leu-enkephalin
dynorphins (8aa or 17aa) --> a smaller form OR the larger form
30
Orphanin FQ aka?
nociceptin
31
How are opioids made?
Since they are peptides, they are made through the usual protein synthetic machinery
32
How do we limit opioid action?
enzymatic activity, possibly after reuptake
enkephalinase A and B
aminopeptidase
33
What (3) receptors do opioids bind to?
mu, kappa, delta
34
Mu receptor
receptor type and effects
serpentine
ANALGESIA, RESPIRATORY DEPRESSION, EUPHORIA
sedation, constipation
35
Kappa receptor
receptor type and effects
serpentine receptor,
ANALGESIA, DYSPHORIA
diuresis, miosis
36
Delta receptor
receptor type and effects
serpentine
ANALGESIA
37
all opioid receptors are _______ and are ______ adenylyl cyclase
serpentine receptors
inhibit
Mu - increases K+ efflux and hyperpolarizes
Kappa and delta - decrease Ca
38
The two endocannabanoids are
anadaminde
2-AG (arachydonylglycerol)
39
Anadamide
"bliss"
arachidonic acid +ethanoloamine
40
2-Arachydonylglycerol
arachadonic acid esterified into the middle, #2 position of glycerol
41
Distribution of endocannabinoids in the CNS
broad distribution
hippocampus - memory formation
Basal Ganglia - affect, motor
spinal cord - modulation of nociception
neocortex - neuroprotective (?)
42
What type of receptors do the endocannabinoids bind to? (2)
CB-1 and CB-2
43
CB-1 receptor
where
what type
what it does
what it binds
axons and presynaptic terminals of EAA and GABA synapses
Gi protein coupled receptor
reduces NT release
binds to either anadamide or 2-AG equally
44