Neurotransmitter Systems - Karius 3/22 Flashcards
What is the central location of NE?
Fx?
Metabotropic receptors?
Made from what?
Pons/Brainstem
Wakefulness
Alpha and beta adrenergics
Tyrosine
What is the central location of Epi?
Fx?
Metabotropic receptors?
Made from what?
Brainstem
Wakefulness
Alpha and beta adrenergics
Tyrosine
What is the central location of Serotonin?
Fx?
Metabotropic receptors?
Made from what?
Brainstem (Raphe nucleus)
Mood, wakefulness
5HT6 - mood
Trp
What is the central location of Histamine?
Fx?
Metabotropic receptors?
Made from what?
Hypothalamus
Waking
H1 and H2
Histidine
What ionotropic receptors does serotonin have?
Responsible for what?
5HT3
Vomiting
Where is Ach located?
Fx?
Pons, midbrain, striatum
Wakefulness, REM sleep, control voluntary motion
Where is Ach stored?
How is it moved?
How is it degraded?
Clear vesicles
VAchT
Acetylcholinesterase
What is M1 found in, what mechanism does it act through?
M2?
M3?
Neuronal, Gq
Cardiac, Gi
Smooth m. Of bronchi, vasculature, endothelial cells of vasculature, Gq
What is M4 found in, what mechanism does it act through?
M5?
glands, Gi
INC IP3/DAG
What kind of receptors does Ach bind to?
Where are they located?
What subunits?
Nicotinic
NMJ, autonomic ganglia, other parts of CNS
Alpha(1-9), beta(2-5), gamma(1), delta(1), epsilon(1)
What are the Metabotropic receptors for Ach?
Ionotropic?
Muscarinic
Nicotinic
Where is GABA located?
Fx?
Higher CNS - cerebellum, cortex, retina
Major inhibitory nt in higher CNS
Critical for consciousness and control voluntary motion
How is GABA made?
How is degraded?
GAD, derived from glutamate
Reuptake
Catabolism by GABA-transaminase
What kind of receptor is GABA(A)?
What else about it?
Ionotropic
Cl conductance
What kind of receptors is GABA(B)?
Acts through what mechanism?
Metabotropic GPCR
Heterotrimeric Gqi(DEC IP3 and DEC Ca influx) and Gi
What does benzodiazepine potentiate?
GABA (A)
Where is glycine found?
Fx?
Spinal cord and Brainstem (lower CNS)
Spinal inhibition of reflexes
Is the glycine receptor ionotropic or Metabotropic?
What mech?
What subunits and fxs do they have?
Ionotropic with Cl- going in
alpha-glycine binding
Beta-structural
What can block the glycine receptor?
Strychnine
What neurotransmitters are released from opioid family of peptides?
NEED Nociceptin Endorphins Enkephalins dynorphins
Where are the opioid peptides located?
Fx?
Basal ganglia, hypothalamus, parabrachial nuclei, Raphe nuclei
Modify nociceptive inputs and modify mood
What is proenkephalin a precursor molecule for?
What 2 forms?
Enkephalins
Met and Leu
What is Pro-opomelanocortinin (POMC) a precursor molecule for?
Beta-endorphins
What is prodynorphin a precursor molecule for?
3 molecules of Leu-enkephalins
Dynorphins (1-8 and 1-17)
What is Orphanin FQ a precursor molecule for?
Nociceptin
How are opioid peptides made?
Destroyed?
DNA/RNA protein synthesis
Enkephalinase A and B
Aminopeptidase
What do the mu receptors do?
Analgesia Respiratory depression Euphoria Sedation Constipation
CARES
What do the kappa receptors do?
Analgesia
Dysphoria
Diuresis
Miosis
What do the delta receptors do?
Analgesia
What do the opioid receptors inhibit?
What kind are they?
Adenylyl cyclase
Serpentine
What indirect ion effects do mu receptors have?
Kappa an Delta?
K+ effluent and hyperpolarize
Decrease calcium
What are the 2 endcocannabinoids?
Anandamide
2-Arachidonylglycerol
What makes up anandamide?
Arachidonic acid + ethanolamine
What makes up 2-Arachidonylglycerol?
Arachidonic acid esterified into middle position of glycerol
4 locations and associated functions of endocannabinoids?
Hippocampus - memory
Basal ganglia - affect/motor
Spinal cord - modulation of nociception
Neocortex - neuroprotective
CB-1 receptor is what kind of receptor?
What does it do?
Binds to what?
Gi of excitatory a.a. Or GABA
Reduces nt release
Both endocannabinoids
Where is CB-2 receptor found?
Fx?
Microglia in brain, immune system, and gut
Anti-inflammatory and in brain causes macrophages to remove B-amyloid
What is the central location of dopamine?
Fx?
Metabotropic receptors?
Made from what?
Basal Ganglia and VTA
Motor control, pleasure, consciousness
D1, D2, D3
Tyrosine
Do nts travel by slow or fast axon all transport?
Mitochondria?
Ion channels and receptors?
Fast
Slow
Slow
What is the RLS in catecholamines nt synthesis?
tyrosine -> L-dopa
Tyrosine hydroxylase
NE -> Epi with what enzyme?
PNMT
What are the 4 major pathways in the brain that utilize dopamine as their nt? And functions
Substantia nigra dopaminergic - motor control (Parkinson’s)
Mesolimbic - pleasure/reward and addiction
Mesocortical - consciousness, if fucked then schizophrenia
Tuberinfundibular - supress prolactin release
Where is NE stored?
Fx?
Nucleus ceruleus
Waking up
What releases Epi?
Adrenal medulla
What moves catecholamines into vesicles? Where are they found specifically?
VMAT1 - adrenal medulla
VMAT2 - neuronal form
What reduces the amount of mono amines that are packaged into vesicles?
Tx for what?
Reserpine
HTN
What dopamine receptors activate the Gs pathway?
D1 and D5 -> D1 like
What dopamine receptors activate the Gi pathway?
D2, D3, D4 -> D2-like
What are the true D1 and D2 receptors innervated by?
Involved in what?
Substantia nigra
Normal control of motion
D1 receptor activation fx?
D2?
D3?
Voluntary motion
Inhibits motion
Pleasure/reward
What enzymes will destroy catecholamines in the synaptic cleft?
What other mechanism of destruction?
MAO and COMT
Reuptake
What is the only ionotropic receptor of serotonin?
5-HT3
What is the 5-HT1 receptor?
5-HT2?
Gi
Gq
What receptors are associated with vomiting?
High affinity for anti-depressants?
Control normal body weight and prevent seizures?
5-HT3
5-HT6
5-HT2c
How is serotonin removed from the synaptic cleft?
MAO
What are the types of histamine receptors?
Which ones are found presynaptically?
H1, H2, H3
H3
What receptors mediate the neuronal effects of histamine?
H1 and H2
What degrades histamine?
Diamine oxidase
